ATIPAMEZOLE HYDROCHLORIDE

Details

Stereochemistry	ACHIRAL
Molecular Formula	C14H16N2.ClH
Molecular Weight	248.751
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

Cl.CCC1(CC2=C(C1)C=CC=C2)C3=CN=CN3

InChI

InChIKey=PCCVCJAQMHDWJY-UHFFFAOYSA-N

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

HIDE SMILES / InChI

Molecular Formula	ClH
Molecular Weight	36.461
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Molecular Formula	C14H16N2
Molecular Weight	212.2902
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=403065e1-4c1a-433c-bb1b-6a2951946297
Curator's Comment: description was created based on several sources, including: http://www.fda.gov/downloads/AnimalVeterinary/Products/ApprovedAnimalDrugProducts/FOIADrugSummaries/ucm116099.pdf https://www.zoetisus.com/products/dogs/antisedan-_atipamezole_.aspx

Atipamezole is a synthetic α2-adrenergic antagonist. It competitively inhibits α2-adrenergic receptors. Atipamezole is indicated for the reversal of the sedative and analgesic effects of Dexdomitor and Domitor in dogs. Adverse reactions: occasional vomiting may occur. At times, a period of excitement or apprehensiveness may be seen in dogs treated with atipamezole. Other effects of atipamezole include hypersalivation, diarrhea, and tremors.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Adrenergic receptor alpha-2 113 Target ID: CHEMBL2095158 Sources: http://www.ncbi.nlm.nih.gov/pubmed/9402036 \| https://www.ncbi.nlm.nih.gov/pubmed/16389294	Antagonist 2778		1.6 nM [Ki]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Sedative and analgesic effects of Dexdomitor and Domitor 2 Sources: http://www.fda.gov/downloads/AnimalVeterinary/Products/ApprovedAnimalDrugProducts/FOIADrugSummaries/ucm116099.pdf	Primary		Approved 8429	Antisedan Approved Use It is indicated for the reversal of the clinical effects of the sedative and analgesic agents. Launch Date 8.3920323E11

PubMed

Title	Date	PubMed
Systemic administration of atipamezole, an alpha 2-antagonist, can reduce scopolamine-induced hyperactivity in rats.	1997 Oct	9832985
Alpha(2A) adrenoceptors contribute to feedback inhibition of capsaicin-induced hyperalgesia.	2004 Jul	15220790
Seizures during medetomindine sedation and local anaesthesia in two dogs undergoing skin biopsy.	2009 May	19382926

Patents

Sample Use Guides

In Vivo Use Guide

The atipamezole dose for the reversal of Dexdomitor or Domitor is 3750 ug/m2 (intravenous) or 5000 ug/m2 (intramuscular).

Route of Administration: Other

In Vitro Use Guide

Affinity of atipamezole to a1- and a2-adrenoceptors in rat brain membranes is 13,300 and 1.6 nM respectively.

Substance Class	Chemical Created by `admin` on `Fri Dec 15 17:35:48 UTC 2023` Edited by `admin` on `Fri Dec 15 17:35:48 UTC 2023`
Record UNII	2W4279571X
Record Status	`Validated (UNII)`
Record Version

Download

Name

Type

Language

ATIPAMEZOLE HYDROCHLORIDE

Common Name

English

ATIPAMEZOLE HYDROCHLORIDE [GREEN BOOK]

Common Name

English

ATIPAMEZOLE HYDROCHLORIDE [MI]

Common Name

English

ATIPAMEZOLE HYDROCHLORIDE [MART.]

Common Name

English

ATIPAMEZOLE HCL

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C29713