U105
U-62066
solid
别名:
(±)-(5α,7α,8β)-3,4-Dichloro-N-methyl-N-[7-(1-pyrrolidinyl)-1-oxaspiro[4.5]dec-8-yl]benzeneacetamide mesylate salt, Spiradoline mesylate salt
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关于此项目
线性分子式:
C22H30Cl2N2O2 · CH3SO3H
化学文摘社编号:
分子量:
521.50
MDL编号:
UNSPSC代码:
12352200
PubChem化学物质编号:
NACRES:
NA.77
表单
solid
颜色
white
溶解性
H2O: 14 mg/mL
methanol: insoluble
储存温度
2-8°C
SMILES字符串
CS(O)(=O)=O.CN([C@H]1CC[C@@]2(CCCO2)C[C@@H]1N3CCCC3)C(=O)Cc4ccc(Cl)c(Cl)c4
InChI
1S/C22H30Cl2N2O2.CH4O3S/c1-25(21(27)14-16-5-6-17(23)18(24)13-16)19-7-9-22(8-4-12-28-22)15-20(19)26-10-2-3-11-26;1-5(2,3)4/h5-6,13,19-20H,2-4,7-12,14-15H2,1H3;1H3,(H,2,3,4)/t19-,20-,22-;/m0./s1
InChI key
FHEZDPDAYTVKKG-JLBKCEDKSA-N
基因信息
human ... OPRK1(4986)
生化/生理作用
U-62066, also known as spiradoline, is a highly selective κ opioid receptor agonist. It exhibits analgesic and diuretic effects. Antitussive property of U-62066 is observed in rats.
制备说明
U-62066 is soluble in water at 14 mg/ml, but is insoluble in methanol.
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
个人防护装备
Eyeshields, Gloves, type N95 (US)
U-47700 and Its Analogs: Non-Fentanyl Synthetic Opioids Impacting the Recreational Drug Market.
Baumann, et al.
Brain sciences, 10 (2020)
Diana T McCloskey et al.
American journal of physiology. Heart and circulatory physiology, 294(1), H205-H212 (2007-10-30)
Increased signaling by G(i)-coupled receptors has been implicated in dilated cardiomyopathy. To investigate the mechanisms, we used transgenic mice that develop dilated cardiomyopathy after conditional expression of a cardiac-targeted G(i)-coupled receptor (Ro1). Activation of G(i) signaling by the Ro1 agonist
Kimberly Scearce-Levie et al.
BMC biology, 3, 3-3 (2005-02-15)
The physiological regulation of G protein-coupled receptors, through desensitization and internalization, modulates the length of the receptor signal and may influence the development of tolerance and dependence in response to chronic drug treatment. To explore the importance of receptor regulation
M F Piercey et al.
The Journal of pharmacology and experimental therapeutics, 251(1), 267-271 (1989-10-01)
Administered i.p. to mice, the selective kappa receptor agonists U-50488H and spiradoline (U-62066) were more potent on the tail-flick than on the hot-plate analgesic assay. Both were more potent after i.s. rather than i.c. administration, a result consistent with earlier
A M Peiró et al.
Pharmacological research, 64(1), 80-84 (2011-03-23)
How can we treat patients with reduced morphine doses without loosing the pain killing effect or morphine antinociceptive effects (MAE)? To address this question, we hypothesized that serotonin (5-HT2) receptor antagonism could enhance MAE mediated by kappa-opioid receptors. We pretreated
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