TABLE 3

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

Compound	R	Receptor Affinities^{^a}			Effects in Mice^{^b}
Compound	R	[³H]CP55,940	[³H]SR144528	CB₂	SA	%MPE	RT	RI
O-4424		169	45	>10,000	N.T.	N.T.	N.T.	N.T.
		(0.4)	(3)
O-6211		138	52	>10,000	2	6	4	12
		(3)	(3)		(1–4)	(4–10)	(2–4)	(8–16)
O-6212		86	41	>10,000	81	100	−3.7	Ataxia
		(6)	(1)		(59)	(59)	(59)	(59)
O-6617		85	43	>10,000	12	8	19	Ataxia
		(3)	(1)		(6–17)	(6–12)	(13–25)	(58)
O-6618		89	44	>10,000	9	13	13	36
		(10)	(2)		(4–15)	(9–17)	(9–15)	(22–52)
O-6213		182	91	>10,000	<17	9	10	10
		(18)	(6)			(5–14)	(7–14)	(7–15)
O-6215		332	221	>10,000	9	13	7	Ataxia
		(52)	(12)		(5–13)	(9–18)	(5–11)	(54)
O-6214		88	56	>10,000	42	100	−2.7	Ataxia
		(4)	(2)		(59)	(59)	(59)	(59)
O-6629		24	20	>10,000	<2	1.5	1.3	4
		(5)	(1)			(0.6–4)	(0.6–2)	(2–6)
O-6658		57	46	>10,000	1	2	2	12
		(11)	(2)		(0.4–2)	(0.9–4)	(1–4)	(6–24)
O-6659		109	128	>10,000	6	16	12	∼59
		(7)	(6)		(4–12)	(10–26)	(6–18)

N.T., not tested.
↵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.