Table 1

Assay conditions for radioligand binding experiments

ReceptorLigand (concentration)TissueIncubation ConditionsNonspecific Ligand (concentration)
5-HT1A[3H]5-HT (1 nM)human recombinant (3T3 cells)1 h/25°Cserotonin (10 μM)
5-HT1B[125I]CYP (0.1 nM) + isoprenaline (30 μM)rat cerebral cortex1.5 h/37°Cserotonin (10 μM)
5-HT1D[3H]LSD (2 nM)human recombinant (HEK 293 cells)1 h/25°Cserotonin (10 μM)
5-HT2A[3H]DOB (1 nM)human recombinant (3T3 cells)1 h/25°Cmethysergide (10 μM)
5-HT2C[3H]5-HT (1 nM)human recombinant (3T3 cells)1 h/25°Cserotonin (10 μM)
5-HT3[3H]BRL 43694 (1 nM)N1E-115 cells30 min/25°Cmetoclopramide (100 μM)
5-HT4[3H]GR 113808 (0.1 nM)guinea pig striatum1 h/37°Cserotonin (30 μM)
5-HT6[3H]LSD (1 nM)human recombinant (Hela cells)1 h/37°Cserotonin (10 μM)
5-HT7[3H]LSD (2 nM)human recombinant (CHO cells)1 h/37°CMethiothepin (10 μM)
Adenosine A1[3H]CCPA (0.5 nM)rat cerebral cortex2 h/25°CCPA (10 μM)
Adenosine A2[3H]CGS-21680 (6 nM)rat striatum1.5 h/27°CNECA (100 μM)
α-1 adrenergic[3H]prazosin (0.25 nM)rat cerebral cortex1 h/25°Cprazosin (0.5 μM)
α-2 adrenergic[3H]RX821002 (0.5 nM)rat cerebral cortex30 min/25°C(−)epinephrine (100 μM)
β-1 adrenergic[3H](−)CPG 12177 (1 nM)rat heart20 min/25°Calprenolol (50 μM)
β-2 adrenergic[3H](−)CPG 12177 (1 nM)guinea pig lung20 min/25°Calprenolol (50 μM)
[3H](−)CPG 12177 (0.15 nM)human recombinant (SF9 cells)20 min/25°Calprenolol (50 μM)
Dopamine D-1[3H]SCH 23390 (0.5 nM)human recombinant (GH4 cells)45 min/25°Cbutaclamol (10 μM)
Dopamine D-2 [long form][3H]spiperone (0.2 nM)human recombinant (CHO cells)1 h/25°Cbutaclamol (10 μM)
Dopamine D-3[3H]YM-09151-2 (0.1 nM)rat recombinant (CHO cells)1 h/27°Cbutaclamol (10 μM)
Dopamine D-4 [D4.4R isoform][3H]spiperone (0.2 nM)rat recombinant (CHO cells)1 h/25°Cbutaclamol (10 μM)
Dopamine D-5[3H]SCH 23390 (1 nM)rat recombinant (CHO cells)1 h/25°CSCH 23390 (10 μM)
Histamine H-1[3H]pyrilamine (0.5 nM)guinea pig cerebellum10 min/25°Ctriprolidine (100 μM)
Histamine H-2[3H]tiotidine (2 nM)guinea pig cerebral cortex30 min/25°Chistamine (5 μM)
Histamine H-3[3H](R)α-methylhistamine (0.5 nM)rat cerebral cortex1 h/25°C(R)α-methylhistamine (5 μM)
Muscarinic M-1[3H]pirenzepine (0.6 nM)rat cerebral cortex2 h/25°Catropine (1 μM)
[3H]pirenzepine (2 nM)human recombinant (CHO cells)1 h/25°Catropine (1 μM)
Muscarinic M-2[3H]AF-DX 384 (2 nM)rat heart1 h/25°Catropine (1 μM)
[3H]AF-DX 384 (3 nM)human recombinant (CHO cells)1 h/27°Catropine (1 μM)
Muscarinic M-3[3H]4-DAMP (0.2 nM)rat salivary gland45 min/25°Catropine (1 μM)
[3H]4-DAMP (0.1 nM)human recombinant (CHO cells)1 h/27°Catropine (1 μM)
Muscarinic M-4[3H]4-DAMP (0.2 nM)human recombinant (CHO cells)1 h/27°Catropine (1 μM)
Muscarinic M-5[3H]4-DAMP (0.5 nM)human recombinant (CHO cells)1 h/25°Catropine (1 μM)
Nicotinic[3H]cytisine (1 nM)rat cerebral cortex75 min/4°Cnicotine (10 μM)
Kainate[3H]kainate (5 nM)rat cerebral cortex1 h/4°C l-glutamate (1 μM)
AMPA[3H]AMPA (5 nM)rat cerebral cortex1 h/4°C l-glutamate (1 μM)
Mu opiate[3H]DAMGO (1 nM)rat cerebral cortex1 h/25°Cnaloxone (1 μM)
Delta opiate[3H]PCl-Phe-DPDPE (0.75 nM)rat cerebral cortex15 h/25°Cnaltrexone (10 μM)
Kappa opiate[3H]U-69593 (1.5 nM)guinea pig cerebellum1 h/25°Cnaloxone (10 μM)
BZD[3H]flumazenil (1 nM)rat cerebral cortex1 h/4°Cdiazepam (10 μM)