SNC 80 is a selective nonpeptide agonist of the δ-opioid receptor (Ki = 0.18 nM, IC50 = 2.73 nM) that is over 2,000-fold less effective at the μ-opioid receptor.[1],[2],[3] It effectively activates µ/δ receptor heteromers (EC50 = 52.8 nM) but not κ/δ or μ/κ heteromers.[4] SNC 80 has antinociceptive as well as pro-convulsant effects in vivo.[1],[2],[5]
Reference:
[1]. Bilsky, E.J., Calderon, S.N., Wang, T., et al. SNC 80, a selective, nonpeptidic and systemically active opioid delta agonist. Journal of Pharmacology and Experimental Therapeutics 273(1), 359-366 (1995).
[2]. Calderon, S.N., Rothman, R.B., Porreca, F., et al. Probes for narcotic receptor mediated phenomena. 19. Synthesis of (+)-4-[(αR)-α-((2S,5R)-4-allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl]-N,N-diethylbenzamide (SNC 80): A highly selective, nonpeptide δ opioid receptor agonist. Journal of Medicinal Chemistry 37(14), 2125-2128 (1994).
[3]. Knapp, R.J., Santoro, G., De Leon, I.A., et al. Structure-activity relationships for SNC80 and related compounds at cloned human delta and mu opioid receptors. Journal of Pharmacology and Experimental Therapeutics 277(3), 1284-1291 (1996).
[4]. Metcalf, M.D., Yekkirala, A.S., Powers, M.D., et al. The δ opioid receptor agonist SNC80 selectively activates heteromeric μ-δ opioid receptors. ACS Chem.Neurosci. 3(7), 505-509 (2012).
[5]. Danielsson, I., Gasior, M., Stevenson, G.W., et al. Electroencephalographic and convulsant effects of the delta opioid agonist SNC80 in rhesus monkeys. Pharmacology, Biochemistry, and Behavior 85(2), 428-434 (2006).