152658-17-8 Usage
Description
Pruritus (chronic itching) is a common symptom seen in 25-90% of
uremic patients, especially those with chronic renal failure requiring
hemodialysis.
Nalfurafine hydrochloride
is a new member of this class that exhibits an improved safety profile as
compared with its predecessors in preclinical studies. It is a potent
agonist for the κ-opioid receptor (Ki = 0.24 nM, EC50 = 0.008 nM, Imax =
91%), with substantially lower binding and agonism of the - or d-opioid
receptors (Ki = 2.24 and 484 nM, EC50 = 1.66 and 21.3 nM, Imax = 53 and
78%, respectively). In vivo, nalfurafine hydrochloride demonstrates
potent antipruritic activity against histamine-sensitive as well as histamine-resistant itch in mouse pruritogen-induced scratching models. The most common adverse event associated with nalfurafine hydrochloride was insomnia or sleep disturbance, seen in 10% of the treated patients. Nalfurafine is structurally related to naltrexone (Revia ), an opioid receptor antagonist marketed for treating
alcohol dependence. Nalfurafine is synthesized in two steps starting from
naltrexone, via reductive amination with methylamine under catalytic
hydrogenation conditions, and subsequent acylation with 3(E)-(3-furyl)
acryloyl chloride.
Originator
Toray industries (Japan)
Uses
Nalfurafine hydrochloride was launched on March of 2009 in Japan as the first in class non-narcotic opioid drug for intractable itch caused by hemodialysis. It showed significant opioid κ-agonist activity and induced neither aversion nor preference in rats on the CPP (Conditioned Place Preference) test.
A new therapeutic agent for the treatment of uremic pruritus in hemodialysis patients.
Brand name
Remitch
Check Digit Verification of cas no
The CAS Registry Mumber 152658-17-8 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,5,2,6,5 and 8 respectively; the second part has 2 digits, 1 and 7 respectively.
Calculate Digit Verification of CAS Registry Number 152658-17:
(8*1)+(7*5)+(6*2)+(5*6)+(4*5)+(3*8)+(2*1)+(1*7)=138
138 % 10 = 8
So 152658-17-8 is a valid CAS Registry Number.
152658-17-8Relevant articles and documents
Crystals of morphinan derivative, manufacturing method thereof, and pharmaceutical composition using the same
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, (2014/09/03)
The present invention relates to a X-form crystal of 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6β-[N-methyl-trans-3-(3-furyl)acrylamido]morphinan hydrochloride and the manufacturing method thereof, wherein the X-form crystal of the compound has char
CRYSTALS OF MORPHINAN DERIVATIVE AND PROCESS FOR PRODUCING THE SAME
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Page/Page column 5; 6, (2008/06/13)
The present invention is directed to provide 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6β-[N-methyl-trans-3-(3-furyl)acrylamido]morphinan hydrochloride consistent in quality after production and having high purity. A crystal of 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6β-[N-methyl-trans-3-(3-furyl)acrylamido]morphinan hydrochloride including a A-form, B-form or C-form crystal thereof, and a process for producing the same are provided.
