TABLE 2

Cannabinoid receptor binding and in vivo effects of 1-(2,4-dichlorophenyl)-4-methyl-5-(4-chlorophenyl)-1H-pyrazoles with various 3-substituents

Compound	R	Receptor Affinities^{^a}			Effects in Mice^{^b}
Compound	R	[³H]CP55,940	[³H]SR144528	CB₂	SA	%MPE	RT	RI
O-4338		680	290	>10,000	2.5	6.1	9.3	16
		(78)	(23)		(2–5)	(1.7–23)	(5.7–15)	(5–47)
O-6668		68	45	>10,000	<2	6	∼2	12
		(7)	(4)			(5–10)		(7–21)
O-6730		83	89	5415	Inactive	Inactive	−2.6	Inactive
		(25)	(14)	(543)	(71)	(71)	(71)	(71)
O-6729		185	120	4573	Inactive	Inactive	Inactive	Inactive
		(42)	(11)	(456)	(71)	(71)	(71)	(71)
O-6731		117	247	5342	89	52	−4.4	16
		(12)	(25)	(516)	(72)	(72)	(72)	(72)
O-6740		159	265	>10,000	Inactive at 8.5 and 28 μg/kg
		(45)	(26)		Lethal at 85 μg/kg

↵a K_i values are nanomolar S.E.M. values for receptor affinities are shown in parentheses.
↵b Values shown are ED₅₀ (95% confidence intervals in parentheses). Single dose tests are indicated by magnitude of effect, with dose that was tested in parentheses. All doses are expressed as micromoles per kilogram.