Clemastine fumarate
- CAS No.
- 14976-57-9
- Chemical Name:
- Clemastine fumarate
- Synonyms
- hs592;tavist;Alagyl;agasten;lecasol;piloral;reconin;tavegil;tavegyl;trabest
- CBNumber:
- CB0376055
- Molecular Formula:
- C25H30ClNO5
- Molecular Weight:
- 459.96
- MOL File:
- 14976-57-9.mol
- MSDS File:
- SDS
- Modify Date:
- 2024/7/22 15:01:55
Melting point | 158-162°C |
---|---|
alpha | D21 +16.9° (methanol) |
Boiling point | 154°C (rough estimate) |
Density | 1.0247 (rough estimate) |
refractive index | 1.5790 (estimate) |
storage temp. | 2-8°C |
solubility | DMSO: soluble5mg/mL (clear solution; warmed) |
form | powder |
color | white to beige |
optical activity | [α]/D +15 to +25°, c = 1 in methanol |
InChIKey | PMGQWSIVQFOFOQ-YKVZVUFRSA-N |
CAS DataBase Reference | 14976-57-9(CAS DataBase Reference) |
SAFETY
Risk and Safety Statements
Symbol(GHS) | GHS07 |
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Signal word | Warning | |||||||||
Hazard statements | H302 | |||||||||
Precautionary statements | P280-P305+P351+P338 | |||||||||
WGK Germany | 3 | |||||||||
RTECS | UY0704600 | |||||||||
HS Code | 2933992600 | |||||||||
Toxicity | LD50 in mice, rats (mg/kg): 730, 3550 orally; 43, 82 i.v. (Weimann) | |||||||||
NFPA 704 |
|
Clemastine fumarate Chemical Properties,Uses,Production
Chemical Properties
White Solid
Uses
Clemastine fumarate 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 fumarate has long been used to inhibit histamine-induced bronchoconstriction in asthma and airway hyperresponsive studies.
Definition
ChEBI: The fumaric acid salt of clemastine. An antihistamine with antimuscarinic and moderate sedative properties, it is used for the symptomatic relief of allergic conditions such as rhinitis, urticaria, conjunctivitis and in pruritic (severe itching) skin condi ions.
General Description
Dextrorotatory clemastine, R,R-2[2[1-(4-chlorophenyl)-1-phenylethoxy]ethyl]-1- methylpyrrolidine hydrogen furnarate (1:1) (Tavist), has two chiral centers, each of which has the (R) absolute configuration. A comparison of the activities of the enantiomers indicates that the asymmetric center close to the terminal side chain nitrogen is of lesser importance to antihistaminic activity.
? This member of the ethanolamine series is characterized by a long duration of action, with an activity that reaches a maximum in 5 to 7 hours and persists for 10 to 12 hours. It is well absorbed when administered orally, and it is excreted primarily in the urine. The side effects are those usually encountered with this series of antihistamines. Clemastine is closely related to chlorphenoxamine, which is used for its central cholinergic-blocking activity. Therefore, it is not surprising that clemastine has significant antimuscarinic activity.
Biological Activity
H 1 -receptor antagonist. Clinically-used antihistamine.
Clemastine fumarate Preparation Products And Raw materials
Supplier | Tel | Country | ProdList | Advantage | Inquiry |
---|---|---|---|---|---|
SynZeal Research Pvt Ltd | +1 226-802-2078 | Gujarat, India | 6522 | 58 | Inquiry |
Pharmaffiliates Analytics and Synthetics P. Ltd | +91-172-5066494 | Haryana, India | 6773 | 58 | Inquiry |
Pharma Affiliates | 172-5066494 | Haryana, India | 6761 | 58 | Inquiry |
Clearsynth Labs | 91-22-45045900 | Maharashtra, India | 3889 | 58 | Inquiry |
A.J Chemicals | 91-9810153283 | New Delhi, India | 6124 | 58 | Inquiry |
CLEARSYNTH LABS LTD. | +91-22-45045900 | Hyderabad, India | 6351 | 58 | Inquiry |
Hebei Mojin Biotechnology Co., Ltd | +8613288715578 | China | 12458 | 58 | Inquiry |
Henan Bao Enluo International TradeCo.,LTD | +86-17331933971 +86-17331933971 | China | 2503 | 58 | Inquiry |
Hebei Mojin Biotechnology Co.,Ltd | +8613288715578 | China | 619 | 58 | Inquiry |
Capot Chemical Co.,Ltd. | 571-85586718 +8613336195806 | China | 29798 | 60 | Inquiry |
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