SMILES string
Cl.Cl.Oc1ccc2C[C@H]3N(CC[C@@]45[C@@H](Oc1c24)[C@@H](CC[C@@]35O)N(CCCl)CCCl)CC6CC6
InChI
1S/C24H32Cl2N2O3.2ClH/c25-8-11-27(12-9-26)17-5-6-24(30)19-13-16-3-4-18(29)21-20(16)23(24,22(17)31-21)7-10-28(19)14-15-1-2-15;;/h3-4,15,17,19,22,29-30H,1-2,5-14H2;2*1H/t17-,19-,22+,23+,24-;;/m1../s1
InChI key
JJZDLJGFHABVOM-QNWHWJQFSA-N
form
solid
drug control
regulated under CDSA - not available from Sigma-Aldrich Canada
color
white
solubility
H2O: soluble (use aqueous solutions immediately.), ethanol: soluble (is stable for ca. 1 month in the freezer.), polar organic solvents: soluble
storage temp.
−20°C
Quality Level
Biochem/physiol Actions
Irreversible μ, δ and κ opioid receptor antagonist.
Features and Benefits
This compound is featured on the Opioid Receptors page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
Disclaimer
Hygroscopic, photosensitive.
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)
法规信息
新产品
此项目有
R M Quock et al.
Brain research, 549(1), 162-164 (1991-05-17)
Nitrous oxide antinociception in the abdominal constriction test was significantly reduced in mice pretreated intracerebroventricularly (i.c.v.) with beta-chlornaltrexamine (beta-CNA). However, this antagonism was reversed when the beta-CNA was co-administered i.c.v. with the kappa-opioid ligand U-50,488H but not the mu-opioid ligand
J R Nicholson et al.
Canadian journal of physiology and pharmacology, 76(3), 304-313 (1998-07-23)
We have exploited the availability of the "orphan" opioid receptor (referred to here as ORL1) in its "natural state" to investigate the effect of nociceptin (orphanin FQ), the endogenous agonist for the ORL1 receptor in the brain, vas deferens, and
R B Raffa et al.
European journal of pharmacology, 244(3), 231-238 (1993-02-15)
Dissociation constants (KA) for [D-Pen2,5]enkephalin (DPDPE) inhibition of the electrically evoked twitch of the mouse isolated vas deferens preparation (MVD) were calculated at five temperatures (25, 30, 34, 37 and 40 degrees C). These values were determined from the equiactive
Agonist-specific regulation of mu-opioid receptor desensitization and recovery from desensitization.
Michael S Virk et al.
Molecular pharmacology, 73(4), 1301-1308 (2008-01-17)
Agonist-selective actions of opioids on the desensitization of mu-opioid receptors (MORs) have been well characterized, but few if any studies have examined agonist-dependent recovery from desensitization. The outward potassium current induced by several opioids was studied using whole-cell voltage-clamp recordings
T A Macey et al.
Neuroscience, 168(2), 543-550 (2010-04-17)
Microinjection of opioids into the ventrolateral periaqueductal gray (vlPAG) produces antinociception in part by binding to mu-opioid receptors (MOPrs). Although both high and low efficacy agonists produce antinociception, low efficacy agonists such as morphine produce limited MOPr internalization suggesting that
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