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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
Chlorphentermine >10,000 451 ± 66 30.9 ± 5.4 388 ± 6 2,650 ± 273 3,940 ± 110
Phentermine 39.4 ± 6.6 244 ± 15 3,511 ± 253 13,900 ± 510 262 ± 21 1,580 ± 80
(+)Amphetamine 7.07 ± 0.95 38.9 ± 1.8 1,765 ± 94 3,830 ± 170 24.8 ± 3.5 34 ± 6
(-)Methamphetamine 28.5 ± 2.5 234 ± 14 4,640 ± 243 14,000 ± 644 416 ± 20 4,840 ± 178
(+)Methamphetamine 12.3 ± 0.7 48.0 ± 5.1 736 ± 45 2,137 ± 98 24.5 ± 2.1 114 ± 11
(+)Fenfluramine 302 ± 20 1,290 ± 152 51.7 ± 6.1 150 ± 5 >10,000 22,000 ± 1,100
(±)Fenfluramine 739 ± 57 1,987 ± 205 79.3 ± 11.5 269 ± 7 >10,000 23,700 ± 1,300
(-)Ephedrine 72.4 ± 10.2 225 ± 36 >10,000 >50,000 1,350 ± 124 4,398 ± 213
Tyramine 40.6 ± 3.5 72.5 ± 5.0 2,775 ± 234 1,556 ± 95 119 ± 11 106 ± 6.0
(±)MDMA 77.4 ± 3.4 462 ± 18 56.6 ± 2.1 238 ± 13 376 ± 16 1,572 ± 59
Norepinephrine 164 ± 13 63.9 ± 1.6 >10,000 >50,000 869 ± 51 357 ± 27
Dopamine 66.2 ± 5.4 40.3 ± 4.4 >10,000 6,489 ± 200 86.9 ± 9.7 38.3 ± 1.6
Serotonin >10,000 3,013 ± 266 44.4 ± 5.3 16.7 ± 0.9 >10,000 2,703 ± 79
GBR-12935 >10,000 277 ± 23 >10,000 289 ± 29 >10,000 3.70 ± 0.40
GBR-12909 >10,000 79.2 ± 4.9 >10,000 73.2 ± 1.5 >10,000 4.3 ± 0.3
Cocaïne >10,000 779 ± 30 >10,000 304 ± 10 >10,000 478 ± 25
Mazindol >10,000 2.88 ± 0.17 >10,000 272 ± 11 >10,000 25.9 ± 0.56
Desipramine >10,000 8.32 ± 1.19 >10,000 350 ± 13 >10,000 5.946 ± 193
Fluoxetine >10,000 688 ± 39 >10,000 9.58 ± 0.88 >10,000 >5,000
Citalopram >10,000 4,332 ± 295 >10,000 2.40 ± 0.09 >10,000 20,485 ± 923
RTI-55 >10,000 5.89 ± 0.53 >10,000 1.00 ± 0.03 >10,000 0.83 ± 0.09
RTI-229 >10,000 19.5 ± 0.6 >10,000 362 ± 13 >10,000 2.5 ± 0.24
Indatraline >10,000 12.6 ± 0.5 >10,000 3.10 ± 0.09 2,810 ± 777 1.90 ± 0.05

Source: Rothman RB, Baumann MH, Dersch CM, Romero DV, Rice KC, Carroll FI, Partilla JS. (2001) Amphetamine-Type Central Nervous System Stimulants Release Norepinephrine More Potently Than They Release Dopamine and Serotonin. Synapse. 39(1), 32-41. Pubmed Link PDF Link

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 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), 138-45. Pubmed Link, PDF Link.

Equilibrium Dissociation Constants for Antidepressants at Human Brain Receptors:

Compound H1 Muscarinic α1-adrenergic α2-adrenergic 5-HT1A 5-HT2 D2
Adinazolam >35,000 >35,000 >35,000 >35,000 >35,000 17,400 ± 500 >35,000
Amitriptyline 0.95 ± 0.03 9.6 ± 0.3 24 ± 2 690 ± 20 450 ± 20 18 ± 1 1,460 ± 90
Bupropion 11,800 ± 600 >35,000 4,200 ± 300 >35,000 >35,000 >35,000 >35,000
Desipramine 60 ± 1 66 ± 2 100 ± 10 5,500 ± 200 6,400 ± 300 350 ± 20 3,500 ± 200
Desmethylsertraline 9,000 ± 2,000 1,430 ± 30 1,200 ± 100 7,800 ± 200 >35,000 4,800 ± 300 11,000 ± 2000
Doxepin 0.17 ± 0.03 23 ± 2 23.5 ± 0.9 1,270 ± 40 276 ± 4 27 ± 4 360 ± 60
Etoperidone 3,100 ± 400 >35,000 38 ± 1 570 ± 10 85 ± 2 36 ± 3 2,300 ± 400
Femoxetine 4,200 ± 200 184 ± 4 650 ± 30 1,970 ± 60 2,285 ± 4 130 ± 10 590 ± 30
Fluoxetine 5,400 ± 500 5,90 ± 70 3,800 ± 300 13,900 ± 200 32,400 ± 900 280 ± 50 12,000 ± 1,000
Imipramine 37 ± 4 46 ± 2 32 ± 5 3,100 ± 100 5,800 ± 500 150 ± 2 620 ± 90
Lofepramine 360 ± 40 67 ± 1 100 ± 3 2,700 ± 100 4,600 ± 200 200 ± 40 2,000 ± 400
Nefazodone 24,000 ± 1,000 11,000 ± 2,000 48 ± 2 640 ± 30 80 ± 20 26 ± 2 910 ± 40
Norfluoxetine 11,000 ± 1,000 810 ± 40 3,900 ± 300 19,000 ± 700 13,700 ± 400 600 ± 60 16,000 ± 1,000
Nortriptyline 6.3 ± 0.9 37 ± 1 55 ± 2 2,030 ± 30 294 ± 4 41 ± 4 2,570 ± 50
Paroxetine 22,000 ± 4,000 108 ± 5 4,600 ± 500 17,000 ± 400 >35,000 19,000 ± 1,000 32,000 ± 4,000
Sertraline 24,000 ± 5,000 630 ± 30 380 ± 50 4,100 ± 200 >35,000 9,900 ± 1,000 10,700 ± 800
Tomoxetine 5,500 ± 900 2,060 ± 50 3,800 ± 200 8,800 ± 100 10,900 ± 100 940 ± 70 >35,000
Trazodone 1,100 ± 200 >35,000 42 ± 3 320 ± 10 96 ± 5 25 ± 0.7 3,500 ± 600
Venlafaxine >35,000 >35,000 >35,000 >35,000 >35,000 >35,000 >35,000

Source: Cusack B, Nelson A, Richelson E (1994) Binding of Antidepressants to Human Brain Receptors: Focus on Newer Generation Compounds. Psychopharmacology (Berl). 114(4), 559-565. Pubmed Link PDF Link

Antidepressants: Equilibrium Dissociation Constants (KD's) and Selectivity for the Human Serotonin, Norepinephrine and Dopamine Transporters:

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

Source: Tatsumi M, Groshan K, Blakely RD, Richelson E. (1997) Pharmacological Profile of Antidepressants and Related Compounds at Human Monoamine Transporters. Eur J Pharmacol. 340(2-3), 249-258. Pubmed Link PDF Link

Affinty of Antipsychotic Drugs at 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 M1
Aripiprazole 410 0.52 9.1 260  ?  ? 20  ? 160 15 57  ?  ?  ?
Clozapine 290 130 240 47 140 1,700 9.9 17 11 66 4 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 1.4 5.1 19 2,800
Ziprasidone 130 3.1 7.2 32 2.5 2 0.39 0.72 76 9.3 13 310 47 5,100

Source: Davis K, Charney D, American College of Neuropsychopharmacology, Coyle J, Nemeroff C. (2002) Neuropsychopharmacology: The Fifth Generation of Progress. 778. Preview Link (Google Books)

Equilibrium Dissociation Constants for Antipsychotic Drugs at Human Brain Receptors:

Compound α1-adrenegic α2-adrenergic D2 H1 Muscarinic 5-HT1A 5-HT1D 5-HT2A 5-HT2C
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
ORG 5222 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
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
9-OH-Risperdone 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
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: Richelson E, Souder T. (2000) Binding of Antipsychotic Drugs to Human Brain Receptors: Focus on Newer Generation Compounds. Life Sci. 68(1), 29-39. Pubmed Link PDF Link

Neuroleptics: Equilibrium Dissociation Constants (KD) 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
cis-Thiothixene 3,190 ± 40 30,000 ± 2000 3,600 ± 100
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
Haloperidol meta2 6,300 ± 300 >10,000 >10,000
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
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. (1999) Pharmacological Profile of Neuroleptics at Human Monoamine Transporters. Eur J Pharmacol. 368(2-3), 277-83. Pubmed Link PDF Link

bron: http://en.wikipedia.org/wiki/User:Rocknroll714/affinities