Astemizole
- CAS No.
- 68844-77-9
- Chemical Name:
- Astemizole
- Synonyms
- r45312;MJD-30;r42512;retolen;Waruzol;R 43512;Metodik;idazole;laridal;metodih
- CBNumber:
- CB6741448
- Molecular Formula:
- C28H31FN4O
- Molecular Weight:
- 458.57
- MOL File:
- 68844-77-9.mol
- Modify Date:
- 2023/6/30 15:45:59
| Melting point | 172.9°C |
|---|---|
| Boiling point | 627.3±65.0 °C(Predicted) |
| Density | 1.1587 (estimate) |
| storage temp. | 2-8°C |
| solubility | DMSO: >20mg/mL |
| pka | pKa 4.85(H2O t=25.0 I=0.025) (Uncertain);8.69(H2O t=25.0 I=0.025) (Uncertain) |
| form | powder |
| color | Crystals |
| Water Solubility | It is soluble in DMSO (25 mg/ml ), ethanol (25 mg/ml), chloroform, methanol, and water (partly miscible). |
| Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months. |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Warning | |||||||||
| Hazard statements | H315-H319-H335 | |||||||||
| Precautionary statements | P261-P264-P271-P280-P302+P352-P305+P351+P338 | |||||||||
| Hazard Codes | Xn | |||||||||
| Risk Statements | 22-36/37/38 | |||||||||
| Safety Statements | 26-36 | |||||||||
| RIDADR | UN 2811 6.1 / PGII | |||||||||
| WGK Germany | 3 | |||||||||
| RTECS | DD8968000 | |||||||||
| HS Code | 2933992600 | |||||||||
| Toxicity | LD50 orl-rat: >2560 mg/kg AIPTAK 251,39,81 | |||||||||
| NFPA 704 |
|
Astemizole price More Price(2)
Astemizole Chemical Properties,Uses,Production
Description
Astemizole belongs to the second-generation class of non-sedating, non-anticholinergic antihistamines. Its non-sedating properties appear to result from its poor penetration of the blood brain barrier. As a result it shows no potentiation of CNS depressants, including alcohol. Its long half-life allows once-daily dosing.
Chemical Properties
Crystalline Solid
Uses
Astemizole is used for preventing and treating severe seasonal and chronic allergic rhinitis, allergic conjunctivitis, hives, Quinke’s edema, other allergic conditions and dermatitis. Synonyms of this drug are hismanal, histazol, and others.
Definition
ChEBI: A piperidine compound having a 2-(4-methoxyphenyl)ethyl group at the 1-position and an N-[(4-fluorobenzyl)benzimidazol-2-yl]amino group at the 4-position.
World Health Organization (WHO)
The first clinically interesting histamine ti-antagonists were introduced in the late forties and early fifties. Several histamine ti-antagonists have a similar cardiac effect to that seen with astemizole and terfenadine. Serious cardiovascular adverse reactions have been reported when used concomitantly with imidazole antifungals and macrolide antibiotics.
Biological Activity
Orally active, potent histamine H 1 antagonist (IC 50 = 4 nM) that displays 20-fold, > 250-fold and > 250-fold selectivity over 5-HT, dopamine and muscarinic acetylcholine receptors respectively. Exhibits antimalarial activity in multidrug resistant strains in vitro (IC 50 = 227 - 734 nM). Also potent hERG K + channel blocker (IC 50 = 0.9 nM) that displays cardiotoxicity in vivo .
Safety Profile
Poison by subcutaneous andintravenous routes. Moderately toxic by ingestion. Humansystemic effects by ingestion: arrhythmias, coma, nauseaor vomiting, somnolence. When heated to decompositionit emits toxic fumes of F?? and NOx.
Astemizole Preparation Products And Raw materials
Raw materials
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chevron_rightPreparation Products
| Supplier | Tel | Country | ProdList | Advantage | Inquiry |
|---|---|---|---|---|---|
| Medkem Laboratories | 91-40-23700606 | Andhra Pradesh, India | 297 | 58 | Inquiry |
| Euroasia Trans Continental | +91 22 56349035-36 | New Delhi, India | 519 | 47 | Inquiry |
| Vishal Pharma (Agency) | 91-11-23874123 | Delhi, India | 89 | 58 | Inquiry |
| Megha Health Care Pvt., Ltd. | 91-22-61424444 | Maharashtra, India | 126 | 58 | Inquiry |
| Pharmaffiliates Analytics & Synthetics (P) Ltd. | 91-172-5066494 | Haryana, India | 631 | 58 | Inquiry |
| Shivam Pharma Chemicals | 91-22-26403900 | Maharashtra, India | 656 | 58 | Inquiry |
| OCEAN TRADING CORPORATION | +91(22) 24921669 | New Delhi, India | 6211 | 58 | Inquiry |
| Pharma Affiliates | 172-5066494 | Haryana, India | 6761 | 58 | Inquiry |
| Tradeimpex International | 91-22-22010843 | Maharashtra, India | 64 | 58 | Inquiry |
| Exim-Pharm International | 91-22-26191948 | Maharashtra, India | 112 | 58 | Inquiry |
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