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. Author manuscript; available in PMC: 2007 Sep 27.

Published in final edited form as: J Med Chem. 2006 Jun 15;49(12):3653–3658. doi: 10.1021/jm060343t

Table 1.

Receptor binding and functional bioactivity.

		Receptor affinity ^a(nM)				Functional bioactivity (nM)
No.	Structure	K_i^δ	K_i^μ	μ/δ	δ/μ	MVD IC^b₅₀	MVD K^c_e	GPI IC^b₅₀
		0.035 ^d	152 ^d	4370 ^d			Irreversible antagonist ^d	>1000 ^d
1		0.158±0.027 (3)	41.3±1.09 (3)	261			Irreversible antagonist > 0.3 nM	244±35
2	H-Dmt-Tic-Glu-Dap(6DMN)-NH₂	7.80±0.29 (4)	7880±1139 (4)	1010			Irreversible antagonist > 10 nM	Partial agonist (max 40%) IC₅₀ = 100 nM
3		668.4 ±123 (6)	251.7±90 (6)		2.7	Partial agonist (max 20%) IC₅₀ = 200 nM		120±8
4		5937±1396 (4)	244.5±14 (5)		24	Partial agonist (max 29%) IC₅₀ = 300 nM		253±15
5	H-Tyr-Pro-Dap(6DMN)-Phe-NH₂	839±38 (3)	3420±817 (3)	4.1		Partial agonist (max 22%) IC₅₀ = 500nM		389±12