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Merck

U105

Sigma-Aldrich

U-62066

solid

Synonim(y):

(±)-(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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About This Item

Wzór liniowy:
C22H30Cl2N2O2 · CH3SO3H
Numer CAS:
Masa cząsteczkowa:
521.50
Numer MDL:
Kod UNSPSC:
12352200
Identyfikator substancji w PubChem:
NACRES:
NA.77

Postać

solid

kolor

white

rozpuszczalność

H2O: 14 mg/mL
methanol: insoluble

temp. przechowywania

2-8°C

ciąg SMILES

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

Klucz InChI

FHEZDPDAYTVKKG-JLBKCEDKSA-N

informacje o genach

human ... OPRK1(4986)

Działania biochem./fizjol.

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.

Uwaga dotycząca przygotowania

U-62066 is soluble in water at 14 mg/ml, but is insoluble in methanol.
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Kod klasy składowania

11 - Combustible Solids

Klasa zagrożenia wodnego (WGK)

WGK 3

Temperatura zapłonu (°F)

Not applicable

Temperatura zapłonu (°C)

Not applicable

Środki ochrony indywidualnej

Eyeshields, Gloves, type N95 (US)


Certyfikaty analizy (CoA)

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Dokumenty związane z niedawno zakupionymi produktami zostały zamieszczone w Bibliotece dokumentów.

Odwiedź Bibliotekę dokumentów

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
M-L G Wadenberg
CNS drug reviews, 9(2), 187-198 (2003-07-09)
The selective kappa-opioid receptor agonist spiradoline mesylate (U62,066E), an arylacetamide, was synthesized with the intention of creating an analgesic that, while still retaining its analgesic properties, would be devoid of the, mainly mu receptor mediated, side effects such as physical
X Wang et al.
Neuroscience, 129(1), 235-241 (2004-10-19)
Both enkephalin and dynorphin containing fibers are in close proximity to neurons in the nucleus ambiguus, including cardiac vagal neurons. Microinjection of Delta and kappa agonists into the nucleus ambiguus have been shown to evoke decreases in heart rate. Yet
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
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

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