TABLE 1

Summary of assay conditions used for assessing activity at various receptor sites in competition for the specified radioligand

Further details can be found in the MDS Panlabs catalogue (MDS Panlabs Pharmacology Services).

Assay Target	Ligand	Nonspecific Binding	Tissue	Incubation
Adenosine A₁	1 nM [³H]DPCPX	100 μM R(−)-PIA	Human recombinant CHO cells	90 min at 25°C
Adenosine A_2A	0.05 μM [³H]CGS-21680	50 μM NECA	Human recombinant HEK-293 cells	90 min at 25°C
Adrenergic α₁, nonselective	0.25 nM [³H]prazosin	0.1 μM Prazosin	Rat brain	30 min at 25°C
Adrenergic α_1A	0.25 nM [³H]prazosin	10 μM Phentolamine	Rat submaxillary gland	60 min at 25°C
Adrenergic α_1B	0.25 nM [³H]prazosin	10 μM Phentolamine	Rat liver	60 min at 25°C
Adrenergic α₂, nonselective	0.7 nM [³H]rauwolscine	1 μM Yohimbine	Rat cortex	30 min at 25°C
Adrenergic α_2A	1 nM [³H]MK-912	10 μM WB-4101	Human recombinant insect Sf9 cells	60 min at 25°C
Adrenergic β, nonselective	0.25 nM [³H]dihydroalprenolol	1 μM S(−)-propranolol	Rat brain	20 min at 25°C
Adrenergic β₁	0.03 nM [¹²⁵I]-cyanopindolol	100 μM (S)- propranolol	Human recombinant Rex 16 cells	120 min at 25°C
Adrenergic β₂	0.2 nM [³H]CGP-12177	10 μM ICI-118551	Human recombinant CHO-NBR1 cells	60 min at 25°C
Ca⁺⁺ channel-L, dihydropyridine	0.1 nM [³H]nitrendipine	1 μM Nifedipine	Rat cortex	90 min at 25°C
Dopamine D₁	1.4 nM [³H]SCH 23390	10 μM (+)-Butaclamol	Human recombinant CHO cells	120 min at 37°C
Dopamine D₂	0.16 nM [³H]spiperone	10 μM Haloperidol	Human recombinant CHO cells	120 min at 25°C
GABA_A, agonist site (muscimol)	1 nM [³H]muscimol	100 nM Muscimol	Rat brain (minus cerebellum)	10 min at 4°C
GABA_A, benzodiazepine, central	1 nM [³H]flunitrazepam	10 μM Diazepam	Rat brain (minus cerebellum)	60 min at 25°C
GABA_A, chloride channel	3 nM [³H]TBOB	200 μM Picrotoxin	Rat cortex	20 min at 25°C
GABA_B, nonselective	0.6 nM [³H]CGP-54626	100 nM CGP-54626	Rat brain	20 min at 25°C
Glutamate, NMDA, phencyclidine	4 nM [³H]TCP	1 μM MK-801	Rat cortex	45 min at 25°C
Glutamate, nonselective	3.75 nM [³H]l-glutamic acid	50 μM L-Glutamic acid	Rat brain	30 min at 37°C
Glycine, strychnine-sensitive	10 nM [³H]strychnine	1 mM Glycine	Rat spinal cord	10 min at 4°C
Insulin	0.03 nM [¹²⁵I]insulin	1 μM Insulin	Rat liver	l6 h at 4°C
Muscarinic M₂	0.29 nM [³H]N-methylscopolamine (0.8 nM for JHW 013)	1 μM Atropine	Human recombinant insect sf9 cells (human recombinant CHO cells)	60 min at 25°C (120 min at 25°C)
Muscarinic M₃	0.29 nM [³H]N-methylscopolamine (0.8 nM for JHW 013)	1 μM Atropine	Human recombinant insect sf9 cells (human recombinant CHO cells)	60 min at 25°C (120 min at 25°C)
Nicotinic acetylcholine	0.1 nM [¹²⁵I]epibatidine	300 μM (−)-Nicotine	Human IMR-32 cells	60 min at 25°C
Opiate, nonselective	1.0 nM [³H]naloxone	1 μM Naloxone	Rat brain	40 min at 25°C
Opiate-δ	0.9 nm [³H]naltrindole	10 μM Naloxone	Human recombinant CHO cells	120 min at 25°C
Opiate-κ	0.6 nM [³H]diprenorphine	1 μM Naloxone	Human recombinant HEK-293 cells	60 min at 25°C
Opiate-μ	0.6 nM [³H]diprenorphine	10 μM Naloxone	Human recombinant CHO cells	60 min at 25°C
Phorbol ester	3 nM [³H]PDBu	1 μM PDBu	Mouse brain	60 min at 25°C
K⁺ channel [K_ATP]	5 nM [³H]glyburide	1 μM Glyburide	Hamster pancreatic β cells HIT-T15	120 min at 25°C
K⁺ channel hERG	1.5 nM [³H]astemizole	10 μM Astemizole	Human recombinant HEK-293 cells	60 min at 25°C
Progesterone	2 nM [³H]R-5020	0.41 μM Progesterone	Bovine uterus	16 h at 4°C
5-HT₁, nonselective	2 nM [³H]5-HT	10 μM 5-HT	Rat cortex	10 min at 37°C
5-HT₂, nonselective	0.5 nM [³H]ketanserin	1 μM Ketanserin	Rat brain	40 min at 25°C
Na⁺ Channel, site 2	5 nM [³H]batrachotoxin A 20-α-benzoate	100 μM Veratridine	Rat brain	60 min at 37°C

NMDA, N-methyl-d-aspartate; CGP-12177, 4-[3-[(1,1-dimethylethyl)amino]-2-hydroxypropoxy]-1,3-dihydro-2H-benzimidazol-2-one; CGP-54626, [S-(R*,R*)]-[3-[[1-(3,4-dichlorophenyl)ethyl]amino]-2-hydroxypropyl](cyclohexylmethyl) phosphinic acid; CGS 21680, 2-[p-(2-carboxyethyl)phenethylamino]-5′-N-ethylcarboxamidoadenosine; DPCPX, 8-cyclopentyl-1,3-dipropylxanthine; ICI 118551, (±)-1-[2,3-(dihydro-7-methyl-1H-inden-4-yl)oxy]-3-[(1-methylethyl)amino]-2-butanol; MK801, (5R,10S)-(+)-5-methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imine hydrogen; MK-912, l-657,743, (2S-trans)-1,3,4,5′,6,6′,7,12b-octahydro-1′,3′-dimethyl-spiro[2H-benzofuro[2,3-a]quinolizine-2,4′(1′H)-pyrimidin]-2′(3′H)-one hydrochloride hydrate; NECA, 5′-N-ethylcarboxamidoadenosine; PDBu, phorbol-12,13-dibutyrate; PIA, N⁶-phenylisopropyladenosine; R-5020, 17α,21-dimethyl-19-nor-4,9-pregnadiene-3,20-dione; SCH 23390, R-(+)-7-chloro-8-hydroxy-3-methyl-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine; TBOB, t-butylbicycloorthobenzoate; TCP, thienyl cyclohexylpiperidine; WB-4101, 2-(2,6-dimethoxyphenoxyethyl)aminomethyl-1,4-benzodioxane hydrochloride.