ATIPAMEZOLE

Details

Stereochemistry	ACHIRAL
Molecular Formula	C14H16N2
Molecular Weight	212.2902
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

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

InChI

InChIKey=HSWPZIDYAHLZDD-UHFFFAOYSA-N

InChI=1S/C14H16N2/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)

HIDE SMILES / InChI

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
A comparative study of the reversal by different alpha 2-adrenoceptor antagonists of the central sympatho-inhibitory effect of clonidine.	1996 Feb	8821553

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 15:40:14 UTC 2023` Edited by `admin` on `Fri Dec 15 15:40:14 UTC 2023`
Record UNII	03N9U5JAF6
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

ATIPAMEZOLE

Official Name

English

ATIPAMEZOLE [MART.]

Common Name

English

ATIPAMEZOLE [USAN]

Common Name

English

4-(2-ETHYL-2-INDANYL)IMIDAZOLE.

Common Name

English

ATIPAMEZOLE [MI]

Common Name

English

ANTISEDAN

Brand Name

English

atipamezole [INN]

Common Name

English

1H-IMIDAZOLE, 4-(2-ETHYL-2,3-DIHYDRO-1H-INDEN-2-YL)-

Systematic Name

English

MPV-1248

Code

English

Classification Tree Code System Code

WHO-VATC

QV03AB90