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
Y Pak et al.
Molecular pharmacology, 50(5), 1214-1222 (1996-11-01)
The effects of acute exposure of the opioid peptide [D-Ala2,N-MePhe4, Gly-ol5]enkephalin (DAMGO) on the mu-opioid receptor were examined in Chinese hamster ovary (CHO) K-1 and baby hamster kidney stable transfectants. In the CHO cell line, acute 1-hr treatment with DAMGO
C S Konkoy et al.
Biochemical pharmacology, 45(1), 207-216 (1993-01-07)
Previously, we showed that kappa-selective ligands inhibit adenylyl cyclase in guinea pig cerebellar membranes. The present studies explore the relationship between kappa 1 binding sites (as determined with [3H]U-69,593 binding) and kappa 1-inhibition of adenylyl cyclase (using U-50,488H) in guinea
W Kozak et al.
Physiology & behavior, 58(2), 353-362 (1995-08-01)
The effects of an irreversible long term opioid antagonism on circadian rhythms in body temperature (Tb), locomotor activity (Act) and feeding under normal conditions and following lipopolysaccharide administration (LPS; 2.5 mg/kg) have been investigated in unrestrained mice housed at their
Michael S Virk et al.
The Journal of neuroscience : the official journal of the Society for Neuroscience, 29(22), 7341-7348 (2009-06-06)
Buprenorphine is a weak partial agonist at mu-opioid receptors that is used for treatment of pain and addiction. Intracellular and whole-cell recordings were made from locus ceruleus neurons in rat brain slices to characterize the actions of buprenorphine. Acute application
Leon W Fyfe et al.
The Journal of pharmacology and experimental therapeutics, 335(3), 674-680 (2010-08-27)
Opioids activate the descending antinociceptive pathway from the ventrolateral periaqueductal gray (vlPAG) by both pre- and postsynaptic inhibition of tonically active GABAergic neurons (i.e., disinhibition). Previous research has shown that short-term desensitization of postsynaptic μ-opioid receptors (MOPrs) in the vlPAG
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