SNC 80

A selective δ-opioid receptor agonist

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5mg

￥1162.00

930.00

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25mg

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货号: ajci6952
CAS: 156727-74-1
别名: (+)-4-[(ΑR)-Α-((2S,5R)-4-烯丙基-2,5-二甲基-1-哌嗪基)-3-甲氧基苄基]-N,N-二乙基苯酰胺,NIH 10815
分子式: C28H39N3O2
分子量: 449.64
纯度: >98%
溶解度: 0.2 mg/ml in DMSO, 0.2 mg/ml in DMF
储存: Store at -20°C
库存: 现货

Background

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).