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
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
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
SMILES string
CS(O)(=O)=O.CN([C@H]1CC[C@@]2(CCCO2)C[C@@H]1N3CCCC3)C(=O)Cc4ccc(Cl)c(Cl)c4
InChI key
FHEZDPDAYTVKKG-JLBKCEDKSA-N
form
solid
color
white
solubility
H2O: 14 mg/mL, methanol: insoluble
storage temp.
2-8°C
Quality Level
Gene Information
human ... OPRK1(4986)
Biochem/physiol Actions
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.
Preparation Note
U-62066 is soluble in water at 14 mg/ml, but is insoluble in methanol.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
Eyeshields, Gloves, type N95 (US)
M A Smith et al.
Behavioural pharmacology, 14(8), 641-647 (2003-12-11)
The purpose of the present study was to examine sensitivity to the antinociceptive effects of kappa opioids during chronic treatment with the nonselective opioid antagonist naltrexone. In a warm-water tail-withdrawal procedure, rats were restrained and the latencies to remove their
Shannon L Briggs et al.
Pharmacology, biochemistry, and behavior, 92(2), 343-350 (2009-04-09)
Interactions of opioid agonists, fentanyl and oxymorphone (micro-selective) and spiradoline and enadoline(kappa-selective), were examined for additive, sub-additive, or supra-additive antinociception in the colorectal distension (CRD) assay. Single-dose values (mg/kg, 0.006-0.016 for fentanyl, 0.25-1.26 forspiradoline, etc.) were summed to formulate theoretical
Glenn R Valdez et al.
The Journal of pharmacology and experimental therapeutics, 323(2), 525-533 (2007-08-19)
Kappa opioid agonists were at one time proposed as candidate pharmacotherapies for cocaine addiction, mainly because of their ability to decrease dopamine neurotransmission and attenuate the behavioral effects of cocaine in laboratory animals. Recent studies, however, suggest that kappa agonists
S G Holtzman
Pharmacology, biochemistry, and behavior, 66(3), 517-522 (2000-07-19)
The results of a previous study in rats indicated that spiradoline has pharmacologically selective discriminative effects that are mediated by kappa-opioid receptors. However, the training dose, 3.0 mg/kg, increased response latencies, suggesting that it was relatively high. The current study
J Kamei et al.
European journal of pharmacology, 187(2), 281-286 (1990-10-09)
The effects of highly selective agonists of kappa-opioid receptors, namely U-50,488H and U-62,066E, on the capsaicin-induced cough reflex in rats were studied. Intracisternal (i.cist.) injection of U-50,488H and of U-62,066E significantly decreased the number of coughs in a dose-dependent manner.
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