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Clemastine fumarate

Clemastine fumarate structure

CAS No:
14976-57-9
Formula:
C21H26ClNO.C4H4O4
Chemical Name:
Clemastine fumarate
Synonyms:
Pyrrolidine,2-[2-[(1R)-1-(4-chlorophenyl)-1-phenylethoxy]ethyl]-1-methyl-,(2R)-,(2E)-2-butenedioate (1:1);Pyrrolidine,2-[2-[(p-chloro-α-methyl-α-phenylbenzyl)oxy]ethyl]-1-methyl-,(+)-,fumarate (1:1);Pyrrolidine,2-[2-[1-(4-chlorophenyl)-1-phenylethoxy]ethyl]-1-methyl-,[R-(R*,R*)]-,(E)-2-butenedioate (1:1);HS 592;Tavegil;(+)-2-[2-[(p-Chloro-α-methyl-α-phenylbenzyl)oxy]ethyl]-1-methylpyrrolidine fumarate;Clemastine fumarate;Clemastine hydrogen fumarate;Tavegyl;Agasten;Tavist;Meclastine fumarate;Mecloprodine;Telgin G;Lacretin;Kinotomin;Marsthine;Masletine;Inbestan;Lecasol;Maikohis;Piloral;Alphamin;Fuluminol;Mallermin F;Trabest;Xolamin;Anhistan;Aloginan;Reconin;Bravegyl;Telgin;52205-67-1
Categories:
Active Pharmaceutical Ingredients > Antiallergic Drugs

Description

Clemastine Fumarate is a selective histamine H1 receptor antagonist with IC50 of 3 nM.Target: Histamine H1 ReceptorClemastine Fumarate inhibits histamine induced rise in [Ca2+]i in HL-60 cells with an IC50 of 3 nM as compared with that of chlorpheniramine or diphenhydramine with IC50 values of 20 nM and 100 nM, respectively [1]. Clemastine showed a first-pass reduction in the extent of absorption, with oral bioavailability calculated as 39.2 +/- 12.4%. Extravascular distribution of drug

Clemastine fumarate Basic Attributes

Molecular Weight：

459.96

Exact Mass：

459.181244

EC Number：

239-055-2

HScode：

2933990090

Characteristics

PSA：

87.1

XLogP3：

4.75410

Appearance：

white to beige

Density：

1.097 g/cm3

Melting Point：

177-178 °C

Boiling Point：

154 °C @ Press: 0.02 Torr

Flash Point：

211ºC

Refractive Index：

1.553

Water Solubility：

DMSO: soluble 5mg/mL (clear solution; warmed)

Storage Conditions：

Store at RT

Vapor Pressure：

1.94E-07mmHg at 25°C

Specific rotation：

D21 +16.9° (methanol)

Odor：

Odorless

Safety Information

Transport codes：

NONH for all modes of transport

RTECS Number：

UY0704600

Precautionary statement(s)：

P261, P264, P270, P271, P273, P280, P301+P310, P302+P352, P304+P340, P311, P312, P321, P322, P330, P361, P363, P391, P403+P233, P405, P501

Hazard Statements：

H301

Clemastine fumarate Use and Manufacturing

Clemastine is a selective histamine H1 receptor antagonist (Ki = 0.26 nM) that also displays high affinity for muscarinic receptors (Ki = 16 nM). It has also recently been identified as a positive allosteric modulator of P2X7 receptor signaling. Clemastine has long been used to inhibit histamine-induced bronchoconstriction in asthma and airway hyperresponsive studies.

Drug Function and Efficacy

Not yet clear

This ingredient has been used in drugs with the following functions (note: it does not mean that the ingredient itself has the following health functions)

Related Drugs

Clemastine Fumarate Oral Solution
Ingredients	The main ingredient of this product is clemastine fumarate.
Indication	It can enhance the effects of ethanol, CNS depressants and anticholinergics.
Specifications	60ml:8.04mg
Manufacturer	Guangdong Zhongsheng Pharmaceutical Co., Ltd.

Paracetamol and pseudoephedrine tablets
Ingredients	Fengyuan Paracetamol Pseudoephedrine Tablets are compound preparations, each tablet contains 0.335mg of clemastine fumarate, 500mg of acetaminophen, and 30mg of pseudoephedrine sulfate. Excipients are: hydroxypropyl cellulose, lactose, polyvinyl pyrrolidone, and magnesium stearate.
Specifications	Each tablet contains 0.335 mg of clemastine fumarate, 500 mg of acetaminophen, and 30 mg of pseudoephedrine sulfate.
Manufacturer	Bengbu Fengyuan Pharmaceutical Co., Ltd.

Clemastine Fumarate Oral Solution
Ingredients	The main ingredient of this product and its chemical name are: [R-(R, R)]-1-methyl-2-[2-[1-(4-chlorophenyl)-1-phenethoxy]ethyl]-pyrrolidine (E)-2-butenedioate.
Indication	It can enhance the effects of ethanol, CNS depressants and anticholinergics.
Specifications	60 ml: 8.04 mg

See More Related Drugs

Registered Holders

Yuanda Life Sciences (Shandong) Co., Ltd.

China
Active
Shandong Keyuan Pharmaceutical Co., Ltd.

China
Active
Jinan Gaohua Pharmaceutical Co., Ltd.

China
Active

See More Registered Holders

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