TABLE 1

Binding affinity and potency and efficacy for stimulation of [³⁵S]GTPγ turnover at hCB₁ and hCB₂ receptors

For each measure in all columns, n is shown in italics below the S.E.M.

Compound	CB₁K_i^{^a}	[³⁵S]GTPγ Turnover		CB₂K_i^{^a}	[³⁵S]GTPγ Turnover
Compound	CB₁K_i^{^a}	CB₁ EC₅₀^{^b}	CB₁E_max^{^c}	CB₂K_i^{^a}	CB₂ EC₅₀^{^b}	CB₂E_max^{^c}
CP55,940	0.59	23.3	124	0.30	2.1	63
	(0.06)	(4.7)	(9)	(0.04)	(0.8)	(4)
	7	12	12	6	10	10
AB-CHMINACA	0.78	7.4	205	0.45	232.4	35
	(0.11)	(1.5)	(14)	(0.03)	(231.2)	(2)
	3	6	6	3	4	4
AB-PINACA	2.87	71	192	0.88	14.9	41
	(0.69)	(20.9)	(25)	(0.00)	(8.4)	(1)
	3	6	6	3	4	4
FUBIMINA	296.1	2466.3	122	23.45	1269.3	56
	(33.5)	(1037.2)	(7)	(3.21)	(557.1)	(9)
	4	6	6	3	6	6

↵^a Values represent K_i (±S.E.M.) in nM for [³H]CP55,940 displacement at specified (hCB₁ or hCB₂) receptor.
↵^b Values represent EC₅₀ (±S.E.M.) in nM for [³⁵S]GTPγS binding at specified (hCB₁ or hCB₂) receptor.
↵^c Values represent percentage of maximal increase (±S.E.M.) for [³⁵S]GTPγS binding over basal at specified (hCB₁ or hCB₂) receptor.