Table 1 Affinities for Aripiprazole and Reference Compounds at Various Receptors, Channels and Transporters

From: Aripiprazole, A Novel Atypical Antipsychotic Drug with a Unique and Robust Pharmacology

Receptor Cold ligand 3H-ligand KD (nM) Assay conc. (nM) Aripiprazole Ki (nM)
5-HT1A WAY 100,635 8-OH-DPAT 1 0.5 5.6±0.8
5-HT1B Ergotamine GR125743 0.3 0.3 830±260
5-HT1D Ergotamine GR125743 0.3 0.3 68±11
5-HT1E 5-HT 5-HT 7.2 3 8000±5000
r5-HT2A Chlorpromazine Ketanserin 0.8 0.5 22±4
5-HT2A Chlorpromazine Ketanserin 2 1 8.7±2.0
5-HT2A Chlorpromazine [125I]DOI 2.5 0.2 35±4
5-HT2B Norfenfluramine LSD 10 5 0.36±0.11
r5-HT2C Chlorpromazine Mesulergine 1.2 0.5 76±8
5-HT2C VGIa Chlorpromazine Mesulergine 1.7 1 180±37
5-HT2C INIa Chlorpromazine Mesulergine 1.7 1 75±14
5-HT2C VGIa Chlorpromazine [125I]DOI 3 0.2 97±100.0
5-HT2C INIa Chlorpromazine [125I]DOI 3 0.2 22±11
r5-HT3 LY-278,584 Zacopride 0.3 0.3 630±110
5-HT5A Ergotamine LSD 1.6 1 1240±280
5-HT6 Chlorpromazine LSD 1.5 1 570±95
5-HT7 Chlorpromazine LSD 2 1 10.3±3.7
D1 SKF38393/Fluphenazine SCH23390 0.35 0.2 1960±670
D2L Haloperidol N-methylspiperone 0.5 0.2 0.74±0.09
D2 Haloperidol N-methylspiperone 0.4 0.2 3.3±1.1
D3 Chlorpromazine N-methylspiperone 0.4 0.2 9.7±5.4
D3 Chlorpromazine N-methylspiperone 0.4 0.2 1.0±0.40
rD4 Chlorpromazine N-methylspiperone 0.5 0.2 510±93
D5 SKF38393/Olanzapine SCH23390 0.3 0.2 2590±1350
MOR Naloxone Diprenorphine 0.2 0.2 >10 000
DOR Naltrindole Diprenorphine 0.2 0.2 >10 000
KOR Naloxone Bremazocine 4 2 >10 000
SERT Fluoxetine Citalopram 0.8 0.5 1080±180
NET Nortriptyline/imipramine Nisoxetine 1.2 0.5 2090±750
DAT 4′,4′-Diflouro-3a (diphenyl-methoxy) tropane HCl GBR12935 1 0.5 3220±660
H1 Chlorpheniramine Pyrilamine 3.6 1 25.1±2.6
H2 Me-histamine Tiotidine 10 0.5 >10 000
gpH3 Histamine Me-histamine 1 0.5 224±164
H4 Clozapine Histamine 10 5 >10 000
rBZP Diazepam RO 15-1788 0.8 0.4 >10 000
rGABA-A GABA Muscimol   3 >10 000
rGABA-B GABA Baclofen   15 >10 000
α-PKC PMA PDBU 1 0.5 >10 000
γ-PKC PMA PDBu 1 0.5 8000±2600
rNMDA (PCP site) PCP/ketamine TCP 1 0.5 4001±2177
α1A Urapidil Prazosin 0.2 0.2 25.7±5.0
α1B Corynanthine Prazosin 0.2 0.2 34.8±5.8
α2A Oxymetazoline Clonidine 2 2 74.3±11.7
α2B Prazosin Clonidine 2.0 2.0 103±10.6
α2C Prazosin Clonidine 2.0 2.0 37.9±3.3
hβ1 Atenolol Pindolol 0.1 0.1 141±4.2
hβ2 ICI-118,551 Pindolol 0.1 0.1 163±15.0
M1 Pirenzepine QNB 0.2 0.5 6780±570
M2 Methoctramine QNB 0.2 0.5 3510±620
M3 4-DAMP QNB 0.2 0.5 4680±440
M4 Tropicamine QNB 0.2 0.5 1520±230
M5 Pirenzepine QNB 0.2 0.5 2330±383
Prostaglandin Ep3 PGE2 PGE2 2 1 >10 000
Prostaglandin Ep4 PGE2 PGE2 2 1 >10 000
  1. Experiments were performed as described in Methods using the radioligands and unlabeled reference ligands listed above. Data represent mean±SEM of at least four separate experiments. All studies were performed with human cloned cDNAs expect where specified; r=rat; gp=guinea-pig.
  2. aRefers to mRNA editing isoform.