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#1

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Pharmacological Profile of Selected Agents in the Dopamine, Norepinephrine and 5-HT Release and Uptake Inhibition Assays:

Test Drug Release NET
EC50 (nM ± SD)
NE Uptake
Ki (nM ± SD)
Release DAT
EC50 (nM ± SD)
DA Uptake
Ki (nM ± SD)
Release SERT
EC50 (nM ± SD)
5-HT Uptake
Ki (nM ± SD)
Appetite Suppressants and their Metabolites
Phentermine 39.4 ± 6.6 - 262 ± 21 - 3,511 ± 253 -
(+)-Amphetamine 7.07 ± 0.95 - 24.8 ± 3.5 - 1,765 ± 94 -
(–)-Ephedrine 43.1 ± 4.0 - 236 ± 9 - >10,000 >50,000
(+)-Ephedrine 218 ± 14 - 2,104 ± 68 - - -
Diethylpropion >10,000 >10,000 >10,000 >10,000 >10,000 >10,000
N-Ethylpropion 99.3 ± 6.6 - - 1,014 ± 80 2,118 ± 98 -
N,N-Diethylnorpseudoephedrine >10,000 >10,000 >10,000 >10,000 >10,000 >10,000
Phendimetrazine 8,300 ± 445 >10,000 19,000 ± 537 >10,000 >100,000 >100,000
Phenmetrazine 50.4 ± 5.4 - 131 ± 11 - 7,765 ± 610 -
(±)-Pseudophenmetrazine 514 ± 52 - - 2,630 ± 198 >10,000 >10,000
(+)-Pseudophenmetrazine 349 ± 28 - 1,457 ± 138 - >10,000 >10,000
(–)-Pseudophenmetrazine 2,511 ± 561 - - 2,691 ± 176 >10,000 >10,000
Appetite Suppressants Removed from Clinical Use
(±)-Fenfluramine 739 ± 57 - - 23,700 ± 1,300 79.3 ± 11.5 -
(+)-Fenfluramine 302 ± 20 - - 22,000 ± 1,100 51.7 ± 6.1 -
(–)-Fenfluramine - 7,187 ± 559 >10,000 >20,000 147 ± 19 -
(±)-Norfenfluramine 168 ± 17 - 1,925 ± 295 - 104 ± 5 -
(+)-Norfenfluramine 72.7 ± 5.4 - 924 ± 112 - 59.3 ± 2.4 -
(–)-Norfenfluramine 474 ± 40 - - 19,194 ± 1,048 287 ± 14 -
Aminorex 26.4 ± 2.8 - 49.4 ± 7.5 - 193 ± 23 -
Chlorphentermine - 451 ± 66 2,650 ± 273 - 30.9 ± 5.4 -
Abused Stimulants
(+)-Methamphetamine 12.3 ± 0.7 - 24.5 ± 2.1 - 736 ± 45 -
(–)-Methamphetamine 28.5 ± 2.5 - 416 ± 20 - 4,640 ± 243 -
(±)-MDMA 110 ± 10 - 278 ± 7 - 72 ± 3 -
(+)-MDMA 136 ± 9 - 142 ± 4 - 74 ± 3 -
(–)-MDMA 560 ± 4 - 3,700 ± 100 - 340 ± 20 -
(±)-MDA 108 ± 7 - 190 ± 6 - 160 ± 7 -
(+)-MDA 50 ± 5 - 98 ± 4 - 100 ± 4 -
(–)-MDA 290 ± 10 - 900 ± 30 - 310 ± 10 -
Benzylpiperazine 62 ± 6.5 - 175 ± 13 - 6,050 ± 835 -
Endogenous Substrates
Tyramine 40.6 ± 3.5 - 119 ± 11 - 2,775 ± 234 -
Norepinephrine 164 ± 13 - 869 ± 51 - >10,000 >50,000
Dopamine 66.2 ± 5.4 - 86.9 ± 9.7 - - 6,489 ± 200
Serotonin >10,000 3,013 ± 266 1,960 ± 147 - 44.4 ± 5.3 -
Transporter Inhibitors
GBR-12,935 - 277 ± 23 - 4.90 ± 0.30 - 289 ± 29
GBR-12,909 (Vanoxerine) - 79.2 ± 4.9 - 4.3 ± 0.3 - 73.2 ± 1.5
Cocaine - 779 ± 30 - 478 ± 25 - 304 ± 10
Mazindol 2.88 ± 0.17 - 25.9 ± 0.56 - 272 ± 11 -
Methylphenidate - 118 ± 12 - 90.2 ± 7.9 - -
Desipramine - 8.32 ± 1.19 - 5,946 ± 193 - 350 ± 13
Fluoxetine - 688 ± 39 - >5,000 - 9.58 ± 0.88
Citalopram - 4,332 ± 295 - 20,485 ± 923 - 2,40 ± 0.09
RTI-55 (β-CIT; Iometopane) - 5.89 ± 0.53 - 0.83 ± 0.09 - 1.00 ± 0.03
Indatraline - 12.6 ± 0.5 - 1.90 ± 0.05 - 3.10 ± 0.09
Miscellaneous Agents
Nantenine >10,000 >10,000 >10,000 >10,000 >10,000 >10,000
Tramadol >10,000 2,770 ± 250 >10,000 >10,000 >10,000 1,820 ± 100
JDTic >10,000 1,756 ± 100 >10,000 3,620 ± 230 >10,000 -

Source: Rothman RB, Baumann MH. (2006) Therapeutic Potential of Monoamine Transporter Substrates. Current Topics in Medicinal Chemistry. 6(17), 1845-1859. Pubmed Link.

#2

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Pharmacological Profile of Selected Agents in the DA, NE and 5-HT Release and Uptake Inhibition Assays:

Compound NE Release NE Reuptake 5-HT Release 5-HT Reuptake DA Release DA Reuptake
Aminorex 26.4 ± 2.8 54.5 ± 4.8 193 ± 23 1,244 ± 106 49.4 ± 7.5 216 ± 7
(+)-Amphetamine 7.07 ± 0.95 38.9 ± 1.8 1,765 ± 94 3,830 ± 170 24.8 ± 3.5 34 ± 6
Chlorphentermine >10,000 451 ± 66 30.9 ± 5.4 388 ± 6 2,650 ± 273 3,940 ± 110
Dopamine 66.2 ± 5.4 40.3 ± 4.4 >10,000 6,489 ± 200 86.9 ± 9.7 38.3 ± 1.6
(–)-Ephedrine 72.4 ± 10.2 225 ± 36 >10,000 >50,000 1,350 ± 124 4,398 ± 213
(±)-Fenfluramine 739 ± 57 1,987 ± 205 79.3 ± 11.5 269 ± 7 >10,000 23,700 ± 1,300
(+)-Fenfluramine 302 ± 20 1,290 ± 152 51.7 ± 6.1 150 ± 5 >10,000 22,000 ± 1,100
(-)-Fenfluramine >10,000 ? 147 ± 19 ? >10,000 ?
mCPP 38.1 ± 4.6 ? >10,000 ? >10,000 ?
MDMA 77.4 ± 3.4 462 ± 18 56.6 ± 2.1 238 ± 13 376 ± 16 1,572 ± 59
(+)-Methamphetamine 12.3 ± 0.7 48.0 ± 5.1 736 ± 45 2,137 ± 98 24.5 ± 2.1 114 ± 11
(–)-Methamphetamine 28.5 ± 2.5 234 ± 14 4,640 ± 243 14,000 ± 644 416 ± 20 4,840 ± 178
Norepinephrine 164 ± 13 63.9 ± 1.6 >10,000 >50,000 869 ± 51 357 ± 27
Phentermine 39.4 ± 6.6 244 ± 15 3,511 ± 253 13,900 ± 510 262 ± 21 1,580 ± 80
Serotonin >10,000 3,013 ± 266 44.4 ± 5.3 16.7 ± 0.9 >10,000 2,703 ± 79
Tyramine 40.6 ± 3.5 72.5 ± 5.0 2,775 ± 234 1,556 ± 95 119 ± 11 106 ± 6.0

Source(s):

  • Rothman RB, Baumann MH, Dersch CM; et al. (January 2001). "Amphetamine-type central nervous system stimulants release norepinephrine more potently than they release dopamine and serotonin". Synapse (New York, N.Y.). 39 (1): 32–41. doi:10.1002/1098-2396(20010101)39:1<32::AID-SYN5>3.0.CO;2-3. PMID 11071707. {{cite journal}}: Explicit use of et al. in: |author= (help)CS1 maint: date and year (link) CS1 maint: multiple names: authors list (link) PDF

#3

[edit]

Effect of Test Agents on Biogenic Amine Release or Uptake [EC50 (nM ± S.D.)]:

Compound NE Release DA Release 5-HT Release
(+)-Amphetamine 7.07 ± 0.95 24.8 ± 3.5 1,765 ± 94
(+)-Methamphetamine 12.3 ± 0.7 24.5 ± 2.1 736 ± 45
(–)-Cathinone 12.4 ± 0.7 18.5 ± 0.3 2,366 ± 138
(–)-Methcathinone 13.1 ± 0.6 14.8 ± 0.4 1772 ± 160
(–)-Ephedrine 43.1 ± 4.0 236 ± 9 -
(+)-Ephedrine 218 ± 14 2,104 ± 68 -
(–)-Norephedrine 42.1 ± 4.3 302 ± 10 -
(+)-Norephedrine 137 ± 8.9 1,371 ± 50 -
(–)-Pseudoephedrine 4,092 ± 432 9,125 ± 480 -
(+)-Pseudoephedrine 224 ± 14 1,988 ± 50 -
(–)-Pseudonorephedrine 30.1 ± 2.2 294 ± 8 -
(+)-Pseudonorephedrine (Cathine) 15.0 ± 4.7 68.3 ± 2.4 -

Source: Rothman RB, Vu N, Partilla JS, Roth BL, Hufeisen SJ, Compton-Toth BA, Birkes J, Young R, Glennon RA. (2003) In vitro characterization of ephedrine-related stereoisomers at biogenic amine transporters and the receptorome reveals selective actions as norepinephrine transporter substrates. J Pharmacol Exp Ther. 307(1), 138-145. Pubmed Link, PDF Link.

#4

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In Vitro Potency as Releasers of Monoamine Neurotransmitters:

Compound [3H]NE [3H]DA [3H]5-HT
d-Amphetamine 7.2 ± 0.44 8.0 ± 0.43 1756 ± 94
3-Fluoroamphetamine (PAL-353) 16.1 ± 1.7 24.2 ± 1.1 1,937 ± 202
4-Fluoroamphetamine (PAL-303) 28.0 ± 1.8 51.5 ± 1.7 939 ± 76
3-Methylamphetamine (PAL-314) 18.3 ± 1.4 33.3 ± 1.3 218 ± 22
4-Methylamphetamine (PAL-313) 22.2 ± 1.3 44.1 ± 2.6 53.4 ± 0.83

Source: Wee S, Anderson KG, Baumann MH, Rothman RB, Blough BE, Woolverton WL. (2005) Relationship between the serotonergic activity and reinforcing effects of a series of amphetamine analogs. J Pharmacol Exp Ther. 313(2), 848-854. 15677348 Pubmed Link, PDF Link.

#5

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Comparison of the Ki (μM) Values of Five Psychostimulants to Inhibit Human and Mouse Monoamine Transporters:

Transporter Cocaine Methylphenidate d-Amphetamine d-Methamphetamine MDMA
Human
hDAT 0.23 ± 0.03 0.06 ± 0.01 0.64 ± 0.14 0.46 ± 0.06 8.29 ± 1.67
hNET 0.48 ± 0.05 0.10 ± 0.01 0.07 ± 0.01 0.11 ± 0.01 1.19 ± 0.13
hSERT 0.74 ± 0.03 132.43 ± 10.71 38.46 ± 3.84 31.74 ± 2.40 2.41 ± 0.73
Mouse
mDAT 0.49 ± 0.04 0.26 ± 0.03 0.56 ± 0.11 0.47 ± 0.08 4.87 ± 0.65
mNET 0.46 ± 0.06 0.17 ± 0.03 0.12 ± 0.02 0.19 ± 0.05 1.75 ± 0.51
mSERT 0.73 ± 0.12 114.37 ± 7.61 23.82 ± 1.71 9.28 ± 0.86 0.64 ± 0.05

Source: Han DD, Gu HH. (2006) Comparison of the monoamine transporters from human and mouse in their sensitivities to psychostimulant drugs. BMC Pharmacol. 6(6). Pubmed Link, PDF Link.

#6

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Antidepressants: Equilibrium Dissociation Constants (KD (nM) ± S.E.M.) for the Receptors of Human Brain Frontal Cortex or Caudate Nucleus:

Compound 5-HT1A 5-HT2A D2 α1-adrenergic α2-adrenergic H1 mACh
Amitriptyline 190 ± 40 29 ± 8 1,000 ± 100 27 ± 4 940 ± 320 1.1 ± 0.4 18 ± 1
Amoxapine 220 ± 50 0.6 ± 0.2 160 ± 60 50 ± 3 2,600 ± 150 25 ± 3 1,000 ± 150
Bupropion 170,000 ± 50,000 90,000 ± 20,000 ? 4,600 ± 500 81,000 ± 8,000 6,600 ± 400 48,000 ± 9,000
Butriptyline 7,000 ± 2,000 380 ± 80 ? 570 ± 110 4,800 ± 910 1.1 ± 0.1 35 ± 6
Clomipramine 7,000 ± 2,000 27 ± 7 190 ± 30 38 ± 6 3,200 ± 310 31 ± 6 37 ± 4
Clovoxamine 21,000 ± 5,000 4,000 ± 1,000 ? 2,200 ± 20 11,000 ± 1,300 16,000 ± 1,000 26,000 ± 5,000
Desipramine 10,000 ± 3,000 280 ± 20 3,300 ± 300 130 ± 40 7,200 ± 1,400 110 ± 30 198 ± 14
Dothiepin 2,300 ± 800 258 ± 8 ? 470 ± 20 2,400 ± 500 3.6 ± 0.2 25 ± 4
Doxepin 290 ± 50 25 ± 8 2,400 ± 300 24 ± 7 1,100 ± 200 0.24 ± 0.02 80 ± 6
Fluoxetine 24,000 ± 4,000 210 ± 40 ? 5,900 ± 400 13,000 ± 700 6,200 ± 600 2,000 ± 400
Fluvoxamine 16,000 ± 2,000 5,600 ± 900 ? 7,500 ± 1,000 15,000 ± 3,500 109,000 ± 20,000 24,000 ± 4,000
Imipramine 9,500 ± 800 80 ± 20 2,000 ± 200 90 ± 30 3200 ± 240 11 ± 1 90 ± 3
Iprindole 2,800 ± 700 280 ± 60 ? 2,300 ± 400 8,600 ± 120 130 ± 20 2,100 ± 350
Maprotiline 12,000 ± 4,000 120 ± 20 350 ± 10 90 ± 20 9,400 ± 140 2.0 ± 0.4 570 ± 120
Mianserin 190 ± 20 7 ± 2 2,100 ± 200 34 ± 7 73 ± 6 0.40 ± 0.10 820 ± 110
Nisoxetine 20,500 ± 900 400 ± 100 ? 5,300 ± 500 6,700 ± 550 4,200 ± 200 3,200 ± 50
Nomifensine 800 ± 200 900 ± 100 ? 850 ± 80 6,500 ± 700 21,000 ± 2,000 250,000
Nortriptyline 310 ± 20 44 ± 8 1,200 ± 100 60 ± 10 2,500 ± 200 10 ± 2 150 ± 30
Oxaprotiline 67,000 ± 9,000 2,400 ± 600 ? 620 ± 80 42,000 ± 7,000 21 ± 1 2,900 ± 600
Protriptyline 3,800 ± 500 70 ± 10 2,300 ± 600 130 ± 40 6,600 ± 390 25 ± 5 25 ± 1
Trazodone 60 ± 20 7 ± 2 3,800 ± 1,000 36 ± 2 490 ± 110 350 ± 60 324,000
Trimipramine 8,000 ± 2,000 32 ± 2 180 ± 50 24 ± 2 680 ± 120 0.27 ± 0.04 58 ± 12
Viloxazine 11,000 ± 2,000 31,000 ± 8,000 ? 14,000 ± 2,000 44,000 ± 7,000 18,000 ± 2,000 54,000 ± 7,000
Zimelidine 18,000 ± 3,000 800 ± 200 ? 1,500 ± 50 790 ± 40 4,000 ± 300 13,000 ± 2,500

Source(s):

  • Wander TJ, Nelson A, Okazaki H, Richelson E (December 1986). "Antagonism by antidepressants of serotonin S1 and S2 receptors of normal human brain in vitro". European Journal of Pharmacology. 132 (2–3): 115–21. doi:10.1016/0014-2999(86)90596-0. PMID 3816971.{{cite journal}}: CS1 maint: date and year (link) CS1 maint: multiple names: authors list (link)

#7

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Equilibrium Dissociation Constants (KD (nM) ± S.E.M.) for Antidepressants at Human Brain Receptors:

Compound 5-HT1A 5-HT2A D2 α1-adrenergic α2-adrenergic H1 mACh
Adinazolam >35,000 17,400 ± 500 >35,000 >35,000 >35,000 >35,000 >35,000
Amitriptyline 450 ± 20 18 ± 1 1,460 ± 90 24 ± 2 690 ± 20 0.95 ± 0.03 9.6 ± 0.3
Bupropion >35,000 >35,000 >35,000 4,200 ± 300 >35,000 11,800 ± 600 >35,000
Desipramine 6,400 ± 300 350 ± 20 3,500 ± 200 100 ± 10 5,500 ± 200 60 ± 1 66 ± 2
Desmethylsertraline >35,000 4,800 ± 300 11,000 ± 2,000 1,200 ± 100 7,800 ± 200 9,000 ± 2,000 1,430 ± 30
Doxepin 276 ± 4 27 ± 4 360 ± 60 23.5 ± 0.9 1,270 ± 40 0.17 ± 0.03 23 ± 2
Etoperidone 85 ± 2 36 ± 3 2,300 ± 400 38 ± 1 570 ± 10 3,100 ± 400 >35,000
Femoxetine 2,285 ± 4 130 ± 10 590 ± 30 650 ± 30 1,970 ± 60 4,200 ± 200 184 ± 4
Fluoxetine 32,400 ± 900 280 ± 50 12,000 ± 1,000 3,800 ± 300 13,900 ± 200 5,400 ± 500 5,90 ± 70
Imipramine 5,800 ± 500 150 ± 2 620 ± 90 32 ± 5 3,100 ± 100 37 ± 4 46 ± 2
Lofepramine 4,600 ± 200 200 ± 40 2,000 ± 400 100 ± 3 2,700 ± 100 360 ± 40 67 ± 1
Nefazodone 80 ± 20 26 ± 2 910 ± 40 48 ± 2 640 ± 30 24,000 ± 1,000 11,000 ± 2,000
Norfluoxetine 13,700 ± 400 600 ± 60 16,000 ± 1,000 3,900 ± 300 19,000 ± 700 11,000 ± 1,000 810 ± 40
Nortriptyline 294 ± 4 41 ± 4 2,570 ± 50 55 ± 2 2,030 ± 30 6.3 ± 0.9 37 ± 1
Paroxetine >35,000 19,000 ± 1,000 32,000 ± 4,000 4,600 ± 500 17,000 ± 400 22,000 ± 4,000 108 ± 5
Sertraline >35,000 9,900 ± 1,000 10,700 ± 800 380 ± 50 4,100 ± 200 24,000 ± 5,000 630 ± 30
Tomoxetine 10,900 ± 100 940 ± 70 >35,000 3,800 ± 200 8,800 ± 100 5,500 ± 900 2,060 ± 50
Trazodone 96 ± 5 25 ± 0.7 3,500 ± 600 42 ± 3 320 ± 10 1,100 ± 200 >35,000
Venlafaxine >35,000 >35,000 >35,000 >35,000 >35,000 >35,000 >35,000

Source:

#8

[edit]

Affinities (Ki (nM) ± S.E.M.) of Typical and Atypical Antidepressants for the Cloned Rat 5-HT2A and 5-HT2C Receptors (and SERT for comparison):

Compound 5-HT2A 5-HT2C SERT
Amitriptyline 4.3 ± 2.4 4.3 ± 0.8 17.6
Amoxapine 1.0 ± 0.5 2.0 ± 0.3 290
Citalopram >1,000 269 ± 57 0.65
Clomipramine 15 ± 1 22 ± 7 0.14
Clorgyline >1,000 >1,000 ?
Desipramine 121 ± 9 244 ± 59 152
Doxepin 26 ± 10 8.8 ± 2.0 126
Fluoxetine 708 ± 6 42.6 ± 4.2 1.96
Imipramine 160 ± 7 94 ± 26 14.2
Iprindole 217 ± 8 206 ± 14 >1,000
Maprotiline 51 ± 11 122 ± 24 >1,000
Mianserin 1.0 ± 0.2 0.4 ± 0.1 >1,000
Nomifensine >1,000 >1,000 >1,000
Norfluoxetine >1,000 157 ± 19 3.15
Nortriptyline 5.0 ± 0.3 8.5 ± 3.7 60.8
Sertraline >1,000 >1,000 0.047
Trazodone 6.0 ± 0.8 192 ± 64 243
Zimelidine >1,000 >1,000 67.6

Source:

#9

[edit]

Antidepressants: Equilibrium Dissociation Constants (KD (nM) ± S.E.M.) and Selectivity for the Human Serotonin, Norepinephrine and Dopamine Transporters:

Antidepressants
Compound SERT NET DAT
Amitriptyline 4.30 ± 0.12 35 ± 2 3,250 ± 20
Amoxapine 58 ± 2 16.0 ± 0.3 4,310 ± 10
Bupropion 9,100 ± 300 52,000 ± 1,000 520 ± 20
Butriptyline 1,360 ± 50 5,100 ± 400 3,940 ± 40
Citalopram 1.16 ± 0.01 4,070 ± 80 28,100 ± 700
Clomipramine 0.28 ± 0.01 38 ± 1 2,190 ± 40
Desipramine 17.6 ± 0.7 0.83 ± 0.05 3,190 ± 40
Desmethylcitalopram 3.6 ± 0.2 1,820 ± 40 18,300 ± 500
Desmethylsertraline 3.0 ± 0.2 390 ± 10 129 ± 2
Dothiepin 8.6 ± 0.4 46 ± 1 5,310 ± 30
Doxepin 68 ± 1 29.5 ± 0.8 12,100 ± 400
Etoperidone 890 ± 40 20,000 ± 2,000 52,000 ± 4,000
Femoxetine 11.0 ± 0.3 760 ± 40 2,050 ± 40
Fluoxetine 0.81 ± 0.02 240 ± 10 3,600 ± 100
Fluvoxamine 2.2 ± 0.2 1,300 ± 30 9,200 ± 200
Imipramine 1.40 ± 0.03 37 ± 2 8,500 ± 100
Iprindole 1,620 ± 40 1,262 ± 7 6,530 ± 20
Iproniazid >100,000 >100,000 >100,000
Lofepramine 70 ± 4 5.4 ± 0.4 18,000 ± 1,000
Maprotiline 5,800 ± 200 11.1 ± 0.3 1,000 ± 20
Mianserin 4,000 ± 300 71 ± 2 9,400 ± 200
Mirtazapine, (±)- >100,000 4,600 ± 300 >100,000
Mirtazapine, (+)- >100,000 2,900 ± 200 >100,000
Mirtazapine, (-)- >100,000 26,000 ± 3,000 >100,000
Nefazodone 200 ± 20 360 ± 40 360 ± 10
Nomifensine 1,010 ± 30 15.6 ± 0.4 56 ± 3
Norfluoxetine 1.47 ± 0.06 1,426 ± 9 420 ± 20
Nortriptyline 18 ± 1 4.37 ± 0.07 1,140 ± 30
Oxaprotiline 3,900 ± 100 4.9 ± 0.2 4,340 ± 30
Paroxetine 0.13 ± 0.01 40 ± 2 490 ± 20
Phenelzine >100,000 49,000 ± 5,000 8,400 ± 200
Protriptyline 19.6 ± 0.5 1.41 ± 0.02 2,100 ± 60
Sertraline 0.29 ± 0.01 420 ± 20 25 ± 2
Tomoxetine 8.9 ± 0.3 2.03 ± 0.06 1,080 ± 50
Tranylcypromine 39,000 ± 2,000 5,900 ± 200 5,100 ± 200
Trazodone 160 ± 20 8,500 ± 300 7,400 ± 300
Trimipramine 149 ± 6 2,450 ± 30 3,780 ± 10
Venlafaxine 8.9 ± 0.3 1,060 ± 40 9,300 ± 50
Viloxazine 17,300 ± 500 155 ± 8 >100,000
Zimelidine 152 ± 6 9,400 ± 100 11,700 ± 400

The Related Compounds: Equilibrium Dissociation Constants (KD (nM) ± S.E.M.) for the Human Serotonin, Norepinephrine and Dopamine Transporters:

Benzodiazepines
Compound SERT NET DAT
Alprazolam >100,000 >100,000 >100,000
Clonazepam >100,000 >100,000 >100,000
Mood Stabilizers
Compound SERT NET DAT
Acetazolamide >100,000 >100,000 >100,000
Carbamazepine 32,000 ± 500 >100,000 >100,000
Lithium Carbonate >100,000 >100,000 >100,000
Valproic Acid >100,000 >100,000 >100,000
Hormones
Compound SERT NET DAT
Estrone 50,000 ± 3,000 >100,000 13,500 ± 600
T3 >100,000 >100,000 81,000 ± 300
Calcium Channel Blockers
Compound SERT NET DAT
Nifedipine >100,000 >100,000 >100,000
Verapamil 246 ± 6 48,000 ± 1,000 20,000 ± 300
Antihypertensives
Compound SERT NET DAT
Reserpine 1,460 ± 60 15,200 ± 900 41,000 ± 2,000
Psychostimulants
Compound SERT NET DAT
Amfonelic Acid ? ? 207 ± 5
Amphetamine, (+)- >100,000 530 ± 40 2,900 ± 200
Cocaine 340 ± 20 1,420 ± 50 220 ± 9
Mazindol 39 ± 1 0.45 ± 0.03 8.1 ± 0.4
Methamphetamine, (+)- >100,000 660 ± 20 2,800 ± 100
Methylphenidate 44,000 ± 1,000 234 ± 9 24 ± 1
Vanoxerine 940 ± 20 310 ± 10 27.2 ± 0.2
Antihistamines
Compound SERT NET DAT
Chlorpheniramine 15.2 ± 0.8 1,440 ± 50 1,060 ± 4
Diphenhydramine 3,800 ± 400 960 ± 30 2,200 ± 100
Neurotransmitters
Compound SERT NET DAT
Dopamine >100,000 32,000 ± 3,000 2,400 ± 100
Norepinephrine >100,000 2,200 ± 30 16,200 ± 500
Serotonin 2,100 ± 100 >100,000 >100,000

Source:

#10

[edit]

Affinty of Antipsychotic Drugs for Human Neurotransmitter Receptors (Ki, nM):

Compound D1 D2 D3 D4 5-HT1A 5-HT1D* 5-HT2A 5-HT2C 5-HT6 5-HT7 α1-adrenegic α2-adrenergic H1 mACh
Aripiprazole 410 0.52 9.1 260 ? ? 20 ? 160 15 57 ? ? ?
Clozapine 290 130 240 47 140 1,700 8.9 17 11 66 4.0 33 1.8 1.8
Haloperidol 120 1.4 2.5 3.3 3,600 >5,000 120 4,700 6,000 1,100 4.7 1,200 440 1,600
Iloperidone 320 6.3 7.1 25 93 ? 5.6 43 63 110 1.4 160 470 ?
Olanzapine 52 20 50 50 2,100 530 3.3 10 10 250 54 170 2.8 4.7
Quetiapine 1,300 180 940 2,200 230 >5,100 220 1,400 4,100 1,800 15 1,000 8.7 100
Risperidone 580 2.2 9.6 8.5 210 170 0.29 10 2,000 3.0 1.4 5.1 19 2,800
Volinanserin 1,800 1,800 ? ? >4,700 >5,100 0.3 68 7,400 2,000 68 2,200 83 ?
Ziprasidone 130 3.1 7.2 32 2.5 2.0 0.39 0.72 76 9.3 13 310 47 5,100
  • Note: 5-HT1D values are for bovine tissue.

Source(s):

  • Duncan GE, Zorn S, Lieberman JA (September 1999). "Mechanisms of typical and atypical antipsychotic drug action in relation to dopamine and NMDA receptor hypofunction hypotheses of schizophrenia". Molecular Psychiatry. 4 (5): 418–28. doi:10.1038/sj.mp.4000581. PMID 10523814.{{cite journal}}: CS1 maint: date and year (link) CS1 maint: multiple names: authors list (link) PDF

#11

[edit]

Neuroleptics: Equilibrium Dissociation Constants (KD (nM) ± S.E.M.) for the Receptors of Human Brain Frontal Cortex or Caudate Nucleus:

Compound 5-HT1A 5-HT2A D2 α1-adrenergic α2-adrenergic H1 mACh
Butaclamol 800 ± 300 0.4 ± 0.1 0.86 ± 0.06 56 ± 8 310 ± 40 390 ± 70 12,000 ± 3,000
Chlorpromazine 3,200 ± 800 1.4 ± 0.4 19 ± 2 2.6 ± 0.3 750 ± 50 9 ± 3 70 ± 6
Chlorprothixene 230 ± 20 0.43 ± 0.08 8 ± 2 ? ? ? ?
Clozapine 1,800 ± 300 1.6 ± 0.4 180 ± 5 9 ± 3 160 ± 20 2.8 ± 0.8 12 ± 4
Fluphenazine 40,000 ± 10,000 19 ± 5 0.8 ± 0.1 9 ± 2 1,550 ± 20 21 ± 4 1,900 ± 500
Haloperidol 2,800 ± 600 36 ± 5 4 ± 1 6.1 ± 0.8 3,800 ± 400 1,900 ± 300 24,000 ± 9,000
Loxapine 2,900 ± 400 1.7 ± 0.4 70 ± 10 28 ± 6 2,400 ± 600 4.9 ± 0.8 450 ± 80
Mesoridazine 500 ± 100 4.8 ± 0.3 19 ± 3 2.0 ± 0.5 1,600 ± 100 1.8 ± 0.1 69 ± 2
Molindone 1,200 ± 300 5,000 ± 1,000 120 ± 40 2,500 ± 600 640 ± 100 124,000 ± 12,000 390,000 ± 90,000
Perphenazine 3,600 ± 400 5.6 ± 0.6 1.4 ± 0.2 10 ± 2 510 ± 20 8 ± 1 1,500 ± 30
Prochlorperazine 5,900 ± 700 15 ± 2 7 ± 1 24 ± 7 1,700 ± 100 19 ± 0.2 540 ± 120
Promazine 12,000 ± 2,000 16 ± 4 160 ± 5 6 ± 2 900 ± 100 2.0 ± 0.1 150 ± 30
Spiperone 320 ± 90 0.38 ± 0.05 0.16 ± 0.02 1.2 ± 0.2 660 ± 20 480 ± 70 2,700 ± 800
Thioridazine 350 ± 70 22 ± 8 26 ± 8 5 ± 1 800 ± 100 16 ± 3 18 ± 1
Thiothixene 1,400 ± 400 130 ± 30 0.45 ± 0.08 11 ± 1 200 ± 20 6 ± 2 2,900 ± 100
Trifluoperazine 23,000 ± 1,000 14 ± 1 2.6 ± 0.3 24 ± 3 2,600 ± 200 62 ± 7 660 ± 40
Triflupromazine 23,000 ± 5,000 4 ± 1 2.8 ± 0.5 ? ? ? ?

Source(s):

#12

[edit]

Binding Data (Ki (nM)) for Typical and Atypical Antipsychotic Drugs as Used in This Study:

Compound 5-HT1A 5-HT2A 5-HT2C 5-HT6 5-HT7 D2 α1A-adrenergic α2A-adrenergic α2B-adrenergic α2C-adrenergic H1 M3
Aripiprazole 5.57 8.7 22.4 783.2 9.6 26 74 102 37 0.66 29.7 4677
Chlorpromazine 116.4 8 25 20.1 35.8 0.28 184 27 46 4 6 47
Clozapine 104.8 5.4 17 17 17.9 1.64 142 26 34 256 1.2 25
Fluphenazine 145.7 30 1386 38 8 6.5 314.1 81.6 28.8 0.54 21 1441
Haloperidol 1202 53 >10000 3666 377.2 12 1130 480 550 4 1800 >10000
Loxapine 2456 7.7 9.5 32.9 87.2 31 150.8 107.6 79.9 12 7 122
Molindone 3797 320 >10000 1008 3053 2612 1097 557.8 172.6 63 2130 >10000
Olanzapine 2063 2 6.8 6.28 105.4 115 314.1 81.6 28.8 34 2 105
Perphenazine 421 5.6 132 17 23 10 810.5 104.9 85.2 1.4 8 1848
Pimozide 650 19 3350 71 0.5 197.7 1593 821.1 376.5 0.65 692 1955
Quetiapine 431.6 101 2502 1865 307.2 22 3630 746.6 28.7 245 11 >10000
Risperidone 427.5 0.17 35 1188 6.6 5 150.8 107.6 1.3 6.5 15 >10000
Sertindole 280 0.58 0.9 5.4 28 1.8 640 450 450 9.1 130 2692
Thioridazine 180.7 10 60 57.1 99 5 134.3 341.3 74.8 11 19 43
Thiothixene 410.4 50 1400 208.4 15.5 11 79.9 50.2 51.9 0.63 4 >10000
Trifluoperazine 950 13 378 118 290.8 24 653.7 163.6 391.5 1.3 63 1001
Ziprasidone 76 0.3 13 60.9 6.62 18 160 48 59 9.7 43 >10000

Source:

#13

[edit]

Equilibrium Dissociation Constants (KD (nM) ± S.E.M.) for Antipsychotic Drugs at Human Brain Receptors:

Compound α1-adrenegic α2-adrenergic D2 H1 mACh 5-HT1A 5-HT1D 5-HT2A 5-HT2C
Asenapine 1.1 ± 0.1 16 ± 1 2.0 ± 0.3 9.3 ± 0.8 7,000 ± 300 15 ± 2 10.2 ± 0.7 0.77 ± 0.03 0.27 ± 0.03
Clozapine 6.8 ± 0.8 15.0 ± 0.6 210 ± 30 3.1 ± 0.5 9 ± 1 160 ± 20 130 ± 10 2.59 ± 0.01 4.8 ± 0.4
Haloperidol 17 ± 1 600 ± 100 2.6 ± 0.5 260 ± 20 >10,000 1,800 ± 300 40 ± 4 61 ± 3 4,700 ± 400
Iloperidone 0.31 ± 0.02 3.0 ± 0.2 3.3 ± 0.1 12.3 ± 0.9 6,000 ± 300 33 ± 2 15 ± 2 0.20 ± 0.02 14 ± 1
Melperone 180 ± 20 150 ± 20 180 ± 20 580 ± 50 >10,000 2,200 ± 200 3,400 ± 100 102 ± 3 2,100 ± 200
Olanzapine 44 ± 4 280 ± 30 20 ± 3 0.087 ± 0.005 36 ± 5 610 ± 80 150 ± 20 1.48 ± 0.05 4.1 ± 0.2
Paliperidone 10.1 ± 0.8 80 ± 10 2.8 ± 0.3 3.4 ± 0.4 8,800 ± 600 480 ± 40 19 ± 1 1.21 ± 0.06 48 ± 5
Pimozide 76 ± 5 650 ± 40 29 ± 4 25 ± 3 800 ± 100 88 ± 6 3,100 ± 300 14.3 ± 0.1 570 ± 40
Quetiapine 8.1 ± 0.9 80 ± 10 770 ± 30 19 ± 1 1,400 ± 200 300 ± 20 560 ± 90 31 ± 4 3,500 ± 500
Risperidone 2.7 ± 0.3 8 ± 1 3.77 ± 0.04 5.2 ± 0.5 34,000 ± 3,000 190 ± 20 3.9 ± 0.5 0.15 ± 0.02 32 ± 4
Sertindole 3.9 ± 0.2 190 ± 30 2.7 ± 0.2 320 ± 30 5,000 ± 1,000 1,050 ± 40 20 ± 1 0.14 ± 0.01 6 ± 1
Ziprasidone 2.6 ± 0.3 154 ± 9 2.6 ± 0.1 4.6 ± 0.4 2,440 ± 80 1.9 ± 0.1 2.4 ± 0.1 0.12 ± 0.01 0.9 ± 0.1
Zotepine 7.3 ± 0.3 180 ± 8 8.1 ± 1 3.3 ± 0.4 330 ± 80 280 ± 20 80 ± 10 2.6 ± 0.1 3.2 ± 0.3

Source:

#14

[edit]

Neuroleptics: Equilibrium Dissociation Constants (KD (nM) ± S.E.M.) for the Human Serotonin, Norepinephrine, and Dopamine Transporters:

Compound SERT NET DAT
Bromperidol 2,200 ± 100 8,600 ± 400 1,660 ± 60
Carpipramine 1,370 ± 30 5,100 ± 200 1,300 ± 100
Chlorpromazine 30 ± 2 19 ± 2 1,750 ± 40
Chlorprothixene 110 ± 10 21 ± 1 1,690 ± 50
Clocapramine 560 ± 10 3,200 ± 200 370 ± 30
Clozapine 1,330 ± 50 2,700 ± 300 >10,000
Fluperlapine 30 ± 4 128 ± 3 >100,000
Fluphenazine 400 ± 30 4,600 ± 100 1,690 ± 20
Haloperidol 3,000 ± 100 6,500 ± 300 2,400 ± 70
Levomepromazine 2,800 ± 100 >10,000 4,100 ± 200
Loxapine 2,400 ± 100 380 ± 30 9,000 ± 200
Melperone >10,000 >10,000 >10,000
Mesoridazine >100,000 >10,000 >10,000
Molindone >100,000 >100,000 >100,000
Moperone 2,680 ± 80 7,690 ± 60 >10,000
Olanzapine 1,310 ± 40 4,500 ± 100 >10,000
Oxypertine >10,000 4,000 ± 200 630 ± 320
Perazine 3,200 ± 100 1,540 ± 80 5,800 ± 100
Perphenazine 610 ± 30 740 ± 20 1,290 ± 30
Pimozide 74 ± 8 370 ± 10 69 ± 3
Prochlorperazine 940 ± 30 510 ± 10 590 ± 20
Promazine 190 ± 20 25 ± 2 8,400 ± 100
Quetiapine >10,000 >10,000 >10,000
Risperidone >10,000 >10,000 >10,000
Sertindole 1,200 ± 200 640 ± 40 200 ± 20
Spiperone 7,500 ± 300 >10,000 4,200 ± 300
Sulpiride >100,000 >100,000 >10,000
Sultopride >100,000 >100,000 >10,000
Thioridazine 650 ± 30 1,620 ± 70 1,130 ± 30
Thiothixene 3,190 ± 40 30,000 ± 2000 3,600 ± 100
Tiapride >100,000 >100,000 >10,000
Timiperone >100,000 >10,000 5,400 ± 300
Tiospirone 2,200 ± 200 1,900 ± 300 460 ± 20
Trifluoperazine 810 ± 10 3,000 ± 100 570 ± 50
Triflupromazine 24 ± 1 110 ± 4 1,830 ± 40
Ziprasidone 39 ± 3 59 ± 7 76 ± 5
Zotepine 45 ± 3 20 ± 3 2,350 ± 80

Source:

  • Tatsumi M, Jansen K, Blakely RD, Richelson E (March 1999). "Pharmacological profile of neuroleptics at human monoamine transporters". European Journal of Pharmacology. 368 (2–3): 277–83. doi:10.1016/s0014-2999(99)00005-9. PMID 10193665.{{cite journal}}: CS1 maint: date and year (link) CS1 maint: multiple names: authors list (link) PDF

#15

[edit]

Inhibition of Opioid Binding and Neurotransmitter Uptake:

Compound μ-OR δ-OR κ-OR SERT NET
DAMGO 0.365 85 210 >100,000 >100,000
DPDPE 380 4.45 11,700 >100,000 >100,000
U-69,593 1,000 3,750 6.65 >100,000 >100,000
Codeine 160 5,130 5,970 >100,000 >100,000
Oxycodone 8.69 901 1,350 >100,000 >100,000
Hydrocodone 11.1 962 501 >300,000 >300,000
Morphine, (-)- 1.24 145 23.4 >100,000 >100,000
Morphine, (+)- >10,000 >100,000 >300,000 >300,000 >300,000
Buprenorphine 4.18 25.8 12.9 >100,000 >100,000
Naloxone, (-)- 0.559 36.5 4.91 >100,000 >100,000
Naloxone, (+)- 3,550 122,000 8,950 >100,000 >100,000
Naltrexone 0.0825 8.02 0.509 >100,000 >100,000
Levorphanol 0.42 3.61 4.2 86.3 1,210
Dextrorphan 420 34,700 5,950 401 340
Levomethorphan 11.2 249 225 35.8 179
Dextromethorphan 1,280 11,500 7,000 23 240
Levallorphan 0.213 2.18 1,100 7,950 19,100
Dextrallorphan 1,140 2,600 34.6 27,700 804
Methadone, (±)- 1.7 435 405 ? ?
Methadone, (R)-(-)- 0.945 371 1,860 14.1 702
Methadone, (S)-(+)- 19.7 960 1,370 992 12,700
Levacetylmethadol 9.86 169 1,020 1,440 67,400
Dextropropoxyphene 34.5 380 1,220 30,000 10,000
Tramadol, (±)- 2,120 57,700 42,700 992 785
Tramadol, (+)- 1,330 62,400 54,000 528 2,510
Tramadol, (-)- 24,800 213,000 53,500 2,350 432

Source:

#16

[edit]

The Ki Values of Drugs for Sigma-1, Sigma-2 and NMDA (PCP site) Receptors in Rat Brain Membranes:

Compound σ1 σ2 NMDA (PCP)
Alazocine 45 ± 4 13,694 ± 4,849 587 ± 108
Dextromethorphan 205 ± 42 11,060 ± 1,320 7,253 ± 302
Dextrorphan 144 ± 37 11,325 ± 1,395 906 ± 77
Dimemorfan 151 ± 17 4,421 ± 277 16,978 ± 488
Dizocilpine 33,756 ± 1,999 51,111 ± 7,630 8.2 ± 1.6
Haloperidol 13 ± 4 148 ± 31 63,951 ± 3,858
Tenocyclidine ? ? 36.3 ± 0.2

Source:

#17

[edit]
Antiparkinsonian Agents at Dopamine Receptors
Compound D1 D2S D2L D3 D4 D5
Apomorphine 372 35 83 26 4.4 15
Bromocriptine 692 5.0 15 6.8 372 537
Cabergoline 214 0.62 0.95 0.80 56 22
Lisuride 65 0.34 0.66 0.28 4.6 3.5
Pergolide 339 32 26 5.5 59 33
Piribedil >10,000 132 174 234 302 >10,000
Pramipexole >10,000 955 1,698 10 129 >10,000
Quinelorane >10,000 316 708 5.4 19 >10,000
Quinpirole >10,000 891 1,445 42 34 >10,000
Ropinirole >10,000 676 933 37 851 >10,000
Roxindole 468 2.8 4.4 1.2 5.9 191
Talipexole >10,000 617 977 68 331 3,467
Terguride 28 0.81 1.1 1.0 8.1 23
TL99 2,692 7.2 68 2.5 58 78
Antiparkinsonian Agents at Serotonin Receptors
Compound 5-HT1A 5-HT1B 5-HT1D 5-HT2A 5-HT2B 5-HT2C
Apomorphine 117 2,951 1,230 120 132 102
Bromocriptine 13 355 11 107 56 741
Cabergoline 20 479 8.7 6.2 1.2 692
Lisuride 0.15 19 0.98 2.8 1.3 6.6
Pergolide 1.9 282 13 8.3 7.1 295
Piribedil 447 >10,000 >10,000 >10,000 1,202 >10,000
Pramipexole 692 8,318 1,660 >10,000 >10,000 >10,000
Quinelorane >10,000 >10,000 >10,000 >10,000 >10,000 2,630
Quinpirole 1,698 >10,000 >10,000 >10,000 >10,000 >10,000
Ropinirole 288 >10,000 1,380 >10,000 3,802 >10,000
Roxindole 0.11 1,445 63 6.6 31 309
Talipexole 1,698 >10,000 >10,000 >10,000 >10,000 >10,000
Terguride 3.5 257 16 4.8 7.1 48
TL99 3,802 >10,000 1,950 2,344 2,042 2,291
Ropinirole at Additional Serotonin Receptors
Compound 5-HT3 5-HT4 5-HT5A 5-HT6 5-HT7
Ropinirole >10,000 >10,000 >10,000 >10,000 1,514
Antiparkinsonian Agents at Adrenergic Receptors
Compound α1A α1B α1D α2A α2B α2C α2D β1 β2
Apomorphine 1,995 676 65 141 66 36 324 >10,000 >10,000
Bromocriptine 4.2 1.4 1.1 11 35 28 68 589 741
Cabergoline 288 60 166 12 72 22 3.6 >10,000 >10,000
Lisuride 5.5 17 3.0 0.055 0.13 0.13 0.79 68 7.9
Pergolide 1,047 692 295 50 32 68 692 >10,000 >10,000
Piribedil 813 6,166 219 89 288 69 437 >10,000 >10,000
Pramipexole >10,000 >10,000 >10,000 1,698 631 >10,000 5,495 >10,000 >10,000
Quinelorane >10,000 >10,000 >10,000 >10,000 >10,000 >10,000 >10,000 >10,000 >10,000
Quinpirole >10,000 >10,000 >10,000 >10,000 2,512 >10,000 >10,000 >10,000 >10,000
Ropinirole >10,000 >10,000 >10,000 1,862 759 1,202 4,467 >10,000 >10,000
Roxindole 2.6 2.8 1.3 6.2 4.6 1.8 28 2,692 933
Talipexole >10,000 3,890 1,259 37 81 43 162 >10,000 >10,000
Terguride 3.5 35 3.9 0.30 0.45 0.76 1.5 661 20
TL99 >10,000 >10,000 >10,000 42 52 6.0 47 >10,000 >10,000
Antiparkinsonian Agents at Histamine and Muscarinic Acetylcholine Receptors
Compound H1 M1
Apomorphine >10,000 >10,000
Bromocriptine >10,000 >10,000
Cabergoline 1,380 >10,000
Lisuride 35 >10,000
Pergolide 1,698 >10,000
Piribedil >10,000 >10,000
Pramipexole >10,000 >10,000
Quinelorane 1,047 >10,000
Quinpirole 1,047 >10,000
Ropinirole 2,951 >10,000
Roxindole 129 >10,000
Talipexole >10,000 >10,000
Terguride 339 >10,000
TL99 776 >10,000

All values are for human receptors except for α2D-adrenergic which is for the rat receptor (due to this receptor not being present in humans and only in rodents). Also the ropinirole values for 5-HT3 and 5-HT4 are for house and guinea pig receptors, respectively.

Source(s):

#18

[edit]

Affinities of Tandospirone, Buspirone, Ipsapirone, and Gepirone for Neurotransmitter Receptor Binding Sites:

Receptor Buspirone Gepirone Ipsapirone Tandospirone
5-HT1A 20 ± 3 70 ± 10 7.9 ± 2 27 ± 5
5-HT1B > 100,000 > 100,000 > 100,000 > 100,000
5-HT1D > 100,000 > 100,000 33,000 ± 8,000 > 100,000
5-HT2A 1,300 ± 400 3,000 ± 50 6,400 ± 4,000 1,300 ± 200
5-HT2C 1,100 ± 200 5,000 ± 700 5,000 ± 1,000 2,600 ± 60
SERT > 100,000
α1-Adrenergic 1,000 ± 400 2,300 ± 300 40 ± 7 1,600 ± 80
α2-Adrenergic 6,000 ± 700 1,600 ± 200 1,900 ± 500 1,900 ± 400
β-Adrenergic 8,800 ± 1,000 > 100,000 > 100,000 > 100,000
D1 33,000 ± 1,000 > 100,000 15,000 ± 2,000 41,000 ± 10,000
D2 240 ± 50 2,200 ± 200 1,900 ± 200 1,700 ± 300
BDZ > 100,000 > 100,000 > 100,000 > 100,000
mACh 38,000 ± 5,000 > 100,000 49,000 ± 5,000 > 100,000

Source: Hamik A, Oksenberg D, Fischette C, Peroutka SJ. (1990) Analysis of Tandospirone (SM-3997) Interactions With Neurotransmitter Receptor Binding Sites. Biol Psychiatry. 28(2), 99-109. Pubmed Link

#19

[edit]

Ki Values of Test Drugs at 5-HT2 Receptors:

Compound 5-HT2A (rat) 5-HT2B (human) 5-HT2C (rat)
(±)-Fenfluramine 5216 ± 2.5 4134 ± 753 3183 ± 374
(+)-Fenfluramine 11107 ± 1354 5099 ± 690 6245 ± 514
(-)-Fenfluramine 5463 ± 352 5713 ± 1344 3415 ± 542
(±)-Norfenfluramine 2316 ± 163 52.1 ± 12.3 557 ± 36
(+)-Norfenfluramine 1516 ± 88 11.2 ± 4.3 324 ± 7.1
(-)-Norfenfluramine 3841 ± 361 47.8 ± 18.0 814 ± 58

Values are mean ± SEM (n=3). Units are nanomolar (nM).

Source: Rothman RB, Baumann MH, Savage JE; et al. (December 2000). "Evidence for possible involvement of 5-HT(2B) receptors in the cardiac valvulopathy associated with fenfluramine and other serotonergic medications". Circulation. 102 (23): 2836–41. doi:10.1161/01.cir.102.23.2836. PMID 11104741. {{cite journal}}: Explicit use of et al. in: |author= (help)CS1 maint: date and year (link) CS1 maint: multiple names: authors list (link)

#20

[edit]
Binding profiles of opioids (Codd et al., 1995)
Drug MORTooltip mu-Opioid receptor DORTooltip delta-Opioid receptor KORTooltip kappa-Opioid receptor SERTTooltip Serotonin transporter NETTooltip Norepinephrine transporter
Buprenorphine 4.18 25.8 12.9 >100,000 >100,000
Codeine 160 5,130 5,970 >100,000 >100,000
DAMGO 0.365 85 210 >100,000 >100,000
Dextropropoxyphene 34.5 380 1,220 30,000 10,000
DPDPE 380 4.45 11,700 >100,000 >100,000
Hydrocodone 11.1 962 501 >300,000 >300,000
Levacetylmethadol 9.86 169 1,020 1,440 67,400
Levallorphan 0.213 2.18 1,100 7,950 19,100
Levomethorphan 11.2 249 225 35.8 179
Levorphanol 0.42 3.61 4.2 86.3 1,210
Methadone 1.7 435 405 ND ND
  Dextromethadone 19.7 960 1,370 992 12,700
  Levomethadone 0.945 371 1,860 14.1 702
Morphine, (–)- 1.24 145 23.4 >100,000 >100,000
Morphine, (+)- >10,000 >100,000 >300,000 >300,000 >300,000
Naloxone, (–)- 0.559 36.5 4.91 >100,000 >100,000
Naloxone, (+)- 3,550 122,000 8,950 >100,000 >100,000
Naltrexone 0.0825 8.02 0.509 >100,000 >100,000
Oxycodone 8.69 901 1,350 >100,000 >100,000
Tramadol 2,120 57,700 42,700 992 785
U-69,593 1,000 3,750 6.65 >100,000 >100,000
Values are Ki (nM). The smaller the value, the more strongly the drug binds
to the site. Assays were done with rat brain membranes.

Source: Codd EE, Shank RP, Schupsky JJ, Raffa RB (1995). "Serotonin and norepinephrine uptake inhibiting activity of centrally acting analgesics: structural determinants and role in antinociception". J. Pharmacol. Exp. Ther. 274 (3): 1263–70. PMID 7562497.

#21

[edit]
Binding profiles of opioids (Tam, 1985)
Drug MORTooltip mu-Opioid receptor DORTooltip delta-Opioid receptor KORTooltip kappa-Opioid receptor σ1
(–)-Alazocine 3.0 15 4.7 1,800–2,400
(+)-Alazocine 1,900 19,000 1,600 48–66
Bremazocine 0.9 2.9 0.67 195
Butorphanol 1.7 13 7.4 2,300
Cyclazocine 0.45 6.3 5.9 36–42
DADLE 150 1.8 >10,000 >100,000
Dynorphin 31 12 0.98 >10,000
(–)-Ethylketazocine 2.3 5.2 2.2 15,000–19,000
(+)-Ethylketazocine 2,500 >10,000 1,600 55–76
Morphine 38 510 1,900 >100,000
Nalbuphine 6.3 163 61 >100,000
Nalorphine 4.5 49 31 80,000
Naloxone 1.1 16 12 >100,000
Oxymorphone 15 145 725 >100,000
Pentazocine 39 467 87 18–29
Sufentanil 5.3 41 140 94
Tifluadom 32 189 2.1 6,600
U-50488H 825 21,000 15 696
Values are Ki (nM). The smaller the value, the more strongly the drug
binds to the site. Assays were done with guinea pig brain membranes.

Source: Tam SW (1985). "(+)-[3H]SKF 10,047, (+)-[3H]ethylketocyclazocine, mu, kappa, delta and phencyclidine binding sites in guinea pig brain membranes". Eur. J. Pharmacol. 109 (1): 33–41. doi:10.1016/0014-2999(85)90536-9. PMID 2986989.

#22

[edit]
Binding and activation profiles of opioids (Gharagozlou et al., 2002, 2003, 2006)
Drug MORTooltip mu-Opioid receptor DORTooltip delta-Opioid receptor KORTooltip kappa-Opioid receptor
Ki IC50 Imax Ki IC50 Imax Ki EC50 Imax IA
β-Endorphin ND 526 71% ND ND ND ND ND ND ND
Alazocine 1.15 ANT ND 184 68% 0.4 24 38% 0.66
Butorphanol ND 3 58% ND 61 64% 2.5 57 33% 0.57
Cyclazocine 0.22 21 37% ND 6 53% 0.1 2 39% 0.67
DAMGO 2.65 35 58% ND ND ND ND ND ND ND
Dezocine ND 1.3 43% ND 477 39% 24.5 ANT ANT
Etorphine ND 0.6 60% ND 0.2 67% ND 0.4 52% 0.90
Fentanyl ND 8.4 69% 242.5 2,039 71% 233 1,677 58% 1.00
Hydromorphone ND 0.8 67% ND 54 65% 55 279 55% 0.95
Lofentanil ND 3.8 56% ND 0.8 62% 8.2 153 58% 1.00
Met-enkephalin ND ND ND ND 22 49% ND ND ND ND
Metazocine ND 2.0 41% ND 159 77% 24 56 47% 0.81
Morphine 2.2 17 48% 68.5 1,101 39% 26 213 55% 0.95
Nalbuphine ND 11 49% 77 545 55% 6 2,550 27% 0.47
Nalorphine ND 2.7 50% 38.5 ANT 1.6 483 55% 0.95
Naltrexone 0.74 ANT ND ANT 0.3 ANT ANT
Quadazocine 0.99 ANT 2.6 40 54% 0.5 ANT ANT
Xorphanol 0.25 3.4 29% 1.0 8 76% 0.4 3.3 49% 0.84
Values are nM. The smaller the value (aside from the percentages), the more strongly the drug inter-
acts with the site. Assays were done with cloned mouse receptors transfected in HEK293 cells.

Sources: