Astemizole

Astemizole__Herg channel blocker LY2801653 (dihydrochloride)

Product Name	Astemizole
Description	Herg channel blocker
Purity	>98%
CAS No.	68844-77-9
Molecular Formula	C28H31FN4O
Molecular Weight	458.57

Storage Temperature	-20ºC
Shipping Temperature	Shipped Ambient
Product Type	Inhibitor
Solubility	Soluble to 100 mM in DMSO and to 25 mM in ethanol
Source	Synthetic
Appearance	White solid
SMILES	COC1=CC=C(C=C1)CCN2CCC(CC2)NC3=NC4=CC=CC=C4N3CC5=CC=C(C=C5)F
InChI	InChI=1S/C28H31FN4O/c1-34-25-12-8-21(9-13-25)14-17-32-18-15-24(16-19-32)30-28-31-26-4-2-3-5-27(26)33(28)20-22-6-10-23(29)11-7-22/h2-13,24H,14-2
InChIKey	GXDALQBWZGODGZ-UHFFFAOYSA-N
Safety Phrases	Classification: Caution: Substance not yet fully tested. Safety Phrases: S22 – Do not breathe dust S24/25 – Avoid contact with skin and eyes S36/37/39 – Wear suitable protective clothing, gloves and eye/face protection Risk Phrases: R62 – Possible risk of impaired fertility Hazard Phrases: H315-H319-H335 Precautionary Phrases: P261-P305 + P351 + P338
Cite This Product	Astemizole (StressMarq Biosciences Inc., Victoria BC CANADA, Catalog # SIH-302)

References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19114965

Alternative Names	1-(4-Fluorobenzyl)-N-{1-[2-(4-methoxyphenyl)ethyl]-4-piperidinyl}-1H-benzimidazol-2-amine, Hismanal
Research Areas	Ion Channels, Neuroscience
PubChem ID	2247
Scientific Background	Astemizole is a second generation antihistamine drug which has a long duration of action. It binds to histamine H1-receptor sites in the gastrointestinal tract, uterus, blood vessels and bronchial muscle. It does not cross the blood-brain barrier, and the binding is primarily in the peripheral nervous system (1). It is metabolized by CYP3A4 (2).
References	1. Laduron P.M., Janssen P.F., Commeren W. and Leysen J.E. (1982) Mol Pharmacol. 21(2): 294-300. 2. Maysumoto S., Yamazoe Y. (2001) Br. J Clin Pharamcol. 51(2): 133-142.