Atipamezole hydrochloride Chemical Properties

Melting point:

211-215°

storage temp. 

Sealed in dry,Room Temperature

solubility 

DMSO (Slightly), Methanol (Slightly)

form 

Solid

color 

White to Off-White

Merck 

14,861

InChI

InChI=1S/C14H16N2.ClH/c1-2-14(13-9-15-10-16-13)7-11-5-3-4-6-12(11)8-14;/h3-6,9-10H,2,7-8H2,1H3,(H,15,16);1H

InChIKey

PCCVCJAQMHDWJY-UHFFFAOYSA-N

SMILES

C1(CC)(CC2=C(C=CC=C2)C1)C1=CNC=N1.Cl

CAS DataBase Reference

104075-48-1(CAS DataBase Reference)

Safety Information

RTECS 

NI6139000

HS Code 

2933.29.2000

Toxicity

LD50 in male, female rats (mg/kg): >50, 44 s.c. (Scheinin)

Atipamezole hydrochloride Usage And Synthesis

Uses

Atipamezole Hydrochloride, is the a synthetic α2-adrenergic antagonist, usually used to reverse the sedative and analgesic effects of dexmedetomidine and medetomidine in dogs. It has also been shown to be used as possible anti-Parkinsonian drug in humans.

Biological Activity

Selective α 2 -adrenergic receptor antagonist (K i values are 1.1, 1.0, 0.89, 1300 and 6500 nM for α 2A , α 2B , α 2C , α 1A and α 1B receptors respectively). Brain penetrant.

Side effects

A transient hypotensive effect has been observed during the first 10 minutes post-injection of atipamezole hydrochloride. In rare cases, hyperactivity, tachycardia, salivation, atypical vocalization, muscle tremor, vomiting, increased respiratory rate, uncontrolled urination, and defecation may occur. In very rare cases, recurrence of sedation may occur, or the recovery time may not be shortened after administration of atipamezole. In cats, when using low doses to reverse the effects of medetomidine or dexmedetomidine partially, the possibility of hypothermia (even when aroused from sedation) should be guarded against.

Veterinary Drugs and Treatments

Atipamezole is labeled for use as a reversal agent for medetomidine and dexmedetomidine. It potentially could be useful for reversal of other alpha2-adrenergic agonists as well (e.g., amitraz, xylazine, clonidine, tizanidine, brimonidine).

storage

Desiccate at RT

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