| Bioactivity | SNC80 (NIH 10815) is a potent, highly selective and non-peptide δ-opioid receptor agonist with a Ki of 1.78 nM and an IC50 of 2.73 nM. SNC80 also selectively activates μ-δ heteromer in HEK293 cells with an EC50 of 52.8 nM. SNC80 shows antinociceptive, antihyperalgesic and antidepressant‐like effects. SNC80 has the potential for multiple headache disorders treatment[1][2][3][4][5][6]. | ||||||||||||
| Target | IC50: 2.73 nM (δ-opioid receptor), 5457 nM (μ-opioid receptor) Ki: 1.78 nM (δ-opioid receptor), 881.5 nM (μ-opioid receptor) and 441.8 nM (κ-opioid receptor) | ||||||||||||
| Invitro | SNC80 selectively activates μ-δ heteromer in HEK293 cells with an EC50 of 52.8 nM. SNC80 exhibits substantially greater activity in cells coexpressing μ- and δ-opioid receptors than in cells either singly expressing δ-opioid receptors or coexpressing δ- and κ-opioid receptors[4]. | ||||||||||||
| In Vivo | SNC80 (10 mg/kg; intraperitoneal injection; once; C57BL6/J mice) treatment significantly attenuated this allodynia caused by overuse of Sumatriptan[1]. Animal Model: | ||||||||||||
| Name | SNC80 | ||||||||||||
| CAS | 156727-74-1 | ||||||||||||
| Formula | C28H39N3O2 | ||||||||||||
| Molar Mass | 449.63 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Moye LS, et al. Delta opioid receptor agonists are effective for multiple types of headache disorders. Neuropharmacology. 2019 Apr;148:77-86. [2]. Bilsky EJ, et al. SNC 80, a selective, nonpeptidic and systemically active opioid delta agonist. J Pharmacol Exp Ther. 1995 Apr;273(1):359-66. [3]. Calderon SN, et al. Probes for narcotic receptor mediated phenomena. 19. Synthesis of (+)-4-[(alpha R)-alpha-((2S,5R)-4-allyl-2,5-dimethyl-1-piperazinyl)-3- methoxybenzyl]-N,N-diethylbenzamide (SNC 80): a highly selective, nonpeptide delta opioid receptor [4]. Metcalf MD, et al. The δ opioid receptor agonist SNC80 selectively activates heteromeric μ-δ opioid receptors. ACS Chem Neurosci. 2012 Jul 18;3(7):505-9. [5]. Vicente-Sanchez A, et al. The delta opioid receptor tool box. Neuroscience. 2016 Dec 3;338:145-159. [6]. Dripps IJ, et al. Role of signalling molecules in behaviours mediated by the δ opioid receptor agonist SNC80. Br J Pharmacol. 2018 Mar;175(6):891-901. |