TABLE 2.

Stimulation of [³⁵S]GTPγS binding by BU08028, compared with buprenorphine, morphine, and other prototypical agonists at NOP and opioid receptors

Data show mean ± S.D. for at least two experiments conducted in triplicate. SR16435 data are from Khroyan et al., 2007.

	NOP		μ		δ		κ
	EC50	%Stimulated	EC50 (nM)	%Stimulated	EC50	%Stimulated	EC50	%Stimulated
	nM		nM		nM		nM
Buprenorphine	251 ± 94	15.5 ± 5.8	10.2 ± 2.2	28.7 ± 1.0	>10,000		>10,000
N/OFQ	8.11 ± 1.4	100
DAMGO			35.3 ± 0.5	100
DPDPE					6.90 ± 0.4	100
U69593							78.5 ± 8.8	100
SR16435	28.7 ± 0.6	45.0 ± 5.1	2.73 ± 0.01	29.5 ± 10	N.D.		>10,000
BU08028	78.6 ± 49	48 ± 13	6.03 ± 2.1	21.1 ± 8.7	—*	10.8 ± 6.8	>10,000

N.D., not determined.

^*Stimulation was too low to accurately determine EC₅₀ value.