CAS NO: | 156727-74-1 |
包装 | 价格(元) |
5mg | 电议 |
25mg | 电议 |
Physical Appearance | A white to off- |
Storage | Store at RT |
M.Wt | 449.64 |
Cas No. | 156727-74-1 |
Formula | C28H39N3O2 |
Solubility | Soluble in DMSO |
Chemical Name | 4-((R)-((2S,5R)-4-allyl-2,5-dimethylpiperazin-1-yl)(3-methoxyphenyl)methyl)-N,N-diethylbenzamide |
Canonical SMILES | O=C(C1=CC=C(C=C1)[C@H](C2=CC=CC(OC)=C2)N3[C@@H](C)CN(CC=C)[C@H](C)C3)N(CC)CC |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
SNC 80 is a highly selective and potent nonpeptide agonist of the δ-opioid receptor, with an IC50 value of 2.73 nM. The δ-opioid receptor, most heavily expressed in the basal ganglia and neocortical regions of the brain in human, participates not solely in the control of pain but also of mood disorders such as anxiety and depression. Selective δ-opioid receptor agonists may serve as potential therapeutic agents for chronic pain with ancillary anxiolytic- and antidepressant-like effects. Moreover, compared to μ-opioid receptor agonists, molecules acting on δ-opioid receptors typically show reduced adverse effects.
References:
1. Calderon SN, Rothman RB, Porreca F, 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 agonist. Journal of Medicinal Chemistry, 1994, 37(14): 2125-2128.
2. Quirion B, Bergeron F, Blais V, et al. The Delta-Opioid Receptor; a Target for the Treatment of Pain. Frontiers in Molecular Neuroscience, 2020, 13: 52.
3. Bilsky EJ, Calderon SN, Wang T, et al. SNC 80, a selective, nonpeptidic and systemically active opioid delta agonist. Journal of Pharmacology and Experimental Therapeutics, 1995, 273(1): 359-366.
Cell experiment:[3] | |
Cell lines | Mouse vas deferens |
Reaction Conditions | 2.73 nM SNC 80 |
Applications | SNC 80 was potent in producing inhibition of electrically induced contractions of mouse vas deferens, but not in inhibiting contractions of the guinea pig isolated ileum (IC50 values of 2.73 and 5457 nM, respectively). |
Animal experiment:[3] | |
Animal models | Mice |
Dosage form | 104.9 nmol, 69 nmol, and 57 mg/kg Intracerebroventricular (i.c.v), intrathecal (i.th.) and intraperitoneal (i.p.) administration |
Applications | SNC 80 produced dose- and time-related antinociception in the mouse warm-water tail-flick test after i.c.v., i.th. and i.p. administration. The calculated A50 values (and 95% C.I.) for SNC 80 administered i.c.v., i.th. and i.p. were 104.9 (63.7-172.7) nmol, 69 (51.8-92.1) nmol and 57 (44.5-73.1) mg/kg, respectively. The i.c.v. administration of SNC 80 also produced dose- and time-related antinociception in the hot-plate test, with a calculated A50 value (and 95% C.I.) of 91.9 (60.3-140.0) nmol. |
Note | The technical data provided above is for reference only. |
References: 1. Calderon SN, Rothman RB, Porreca F, 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 agonist. Journal of Medicinal Chemistry, 1994, 37(14): 2125-2128. 2. Quirion B, Bergeron F, Blais V, et al. The Delta-Opioid Receptor; a Target for the Treatment of Pain. Frontiers in Molecular Neuroscience, 2020, 13: 52. 3. Bilsky EJ, Calderon SN, Wang T, et al. SNC 80, a selective, nonpeptidic and systemically active opioid delta agonist. Journal of Pharmacology and Experimental Therapeutics, 1995, 273(1): 359-366. |