156727-74-1
中文名稱
(+)-4-[(ΑR)-Α-((2S,5R)-4-烯丙基-2,5-二甲基-1-哌嗪基)-3-甲氧基芐基]-N,N-二乙基苯酰胺
英文名稱
SNC 80
CAS
156727-74-1
分子式
C28H39N3O2
分子量
449.63
MOL 文件
156727-74-1.mol
更新日期
2023/03/20 15:41:23
156727-74-1 結(jié)構(gòu)式
基本信息
中文別名
(+)-4-[(ΑR)-Α-((2S,5R)-4-烯丙基-2,5-二甲基-1-哌嗪基)-3-甲氧基芐基]-N,N-二乙基苯酰胺4-[(R)-[(2S,5R)-2,5-二甲基-4-(2-丙烯-1-基)-1-哌嗪基](3-甲氧基苯基)甲基]-N,N-二乙基苯甲酰胺
英文別名
SNC 80NIH 10815
(+)-4-[(Ar)-alpha-((2s,5r)-4-allyl-2,5-dimethyl-1-piperazinyl)-3
4-(alpha-(4-allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl)-N,N-diethylbenzamide
(+)-4-[(AR)-A-((2S,5R)-4-ALLYL-2,5-DIMETHYL-1-PIPERAZINYL)-3-METHOXYBENZYL]-N,N-DIETHYLBENZAM
(+)-4-[(aR)-α-((2S,5R)-4-Allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl]-N,N-diethylbenzamide
(+)-4-[(αr)-α-((2s,5r)-4-allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl]-n,n-diethylbenzamide
(+)-4-[(AR)-A-((2S,5R)-4-ALLYL-2,5-DIMETHYL-1-PIPERAZINYL)-3-METHOXYBENZYL]-N,N-DIETHYLBENZAMIDE
(+)-4-[(AR)-ALPHA-((2S,5R)-4-ALLYL-2,5-DIMETHYL-1-PIPERAZINYL)-3-METHOXYBENZYL]-N,N-DIETHYLBENZAMIDE
(+)-4-[(alphaR)-alpha-((2S,5R)-4-Allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl]-N,N-diethylbenzamide
物理化學性質(zhì)
熔點122-123°C
沸點564.8±50.0 °C(Predicted)
密度1.040
儲存條件Store at RT
溶解度DMSO: soluble
溶解度可溶于DMSO
酸度系數(shù)(pKa)7.29±0.10(Predicted)
形態(tài)solid
顏色off-white
穩(wěn)定性冷凍儲存
InChIKeyKQWVAUSXZDRQPZ-UMTXDNHDSA-N
SMILESC(N(CC)CC)(=O)C1=CC=C([C@@H](N2C[C@@H](C)N(CC=C)C[C@@H]2C)C2=CC=CC(OC)=C2)C=C1
應(yīng)用領(lǐng)域
用途1
A highly selective and potent non-peptide 鈭?agonist, 2000-fold selective over u-receptors.常見問題列表
生物活性
SNC80 (NIH 10815) 是一種有效的，高度選擇性的非肽類 δ 阿片 (δ-opioid) 受體激動劑，Ki 為1.78 nM，IC50 為 2.73 nM。SNC80 還以 EC50 為 52.8 nM 來選擇性激活 HEK293 細胞中的 μ-δ 異聚體。SNC80 具有抗傷害性，抗痛覺過敏和抗抑郁樣作用，并可用于多種頭痛癥的研究。靶點
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)
體外研究
SNC80 selectively activates μ-δ heteromer in HEK293 cells with an EC 50 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.
體內(nèi)研究
SNC80 (10 mg/kg; intraperitoneal injection; once; C57BL6/J mice) treatment significantly attenuated this allodynia caused by overuse of Sumatriptan.
| Animal Model: | Male and female C57BL6/J mice (20-30g) injected with Sumatriptan |
| Dosage: | 10 mg/kg |
| Administration: | Intraperitoneal injection; once |
| Result: | Significantly attenuated allodynia. |