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BioAssay: AID 60245

Antiarrhythmic effect in coronary artery ligated dogs model at a dose of 5 mg/kg, administered intravenously and value noted at 20 min

A series of alpha,alpha-diaryl-1-piperidinebutanols was evaluated for antiarrhythmic activity in the coronary ligated dog model. Structure-activity relationship studies indicated that the 2,6-dimethylpiperidine group yielded compounds with the best antiarrhythmic profiles in this series. The length of the methylene chain separating the diarylcarbinol and the amino group was not crucial. more ..
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 Tested Compounds
 Tested Compounds
All(28)
 
 
Unspecified(28)
 
 
 Tested Substances
 Tested Substances
All(28)
 
 
Unspecified(28)
 
 
 Related BioAssays
 Related BioAssays
AID: 60245
Data Source: ChEMBL (57392)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-05-21
Modify Date: 2014-05-19

Data Table ( Complete ):           View All Data
Tested Compounds:
Description:
Title: Synthesis and antiarrhythmic activity of cis-2,6-dimethyl-alpha,alpha-diaryl-1-piperidinebutanols.

Abstract: A series of alpha,alpha-diaryl-1-piperidinebutanols was evaluated for antiarrhythmic activity in the coronary ligated dog model. Structure-activity relationship studies indicated that the 2,6-dimethylpiperidine group yielded compounds with the best antiarrhythmic profiles in this series. The length of the methylene chain separating the diarylcarbinol and the amino group was not crucial. Substitution of a hydrogen or a number of functional groups for the hydroxyl group had little effect on efficacy or duration but yielded compounds that produced severe tachycardias. Replacement of one of the aryl groups by hydrogen or a pyridinyl or cyclohexyl group had little effect on efficacy but decreased the duration of action. Compound 18 (pirmenol) was ultimately chosen for further studies and is now being investigated in man.
(PMID: 1992110)
Comment
Putative Target:
ChEMBL Target ID: 50588
Target Type: ORGANISM
Pref Name: Canis familiaris
Organism: Canis lupus familiaris
Tax ID: 9615
Confidence: Target assigned is non-molecular
Relationship Type: Non-molecular target assigned
Categorized Comment - additional comments and annotations
From ChEMBL:
Assay Type: Functional
Assay Data Source: Scientific Literature
BAO: Assay Format: organism-based format
Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Normal beats activity commentNormal beats activity commentString
2Normal beats standard flagNormal beats standard flagInteger
3Normal beats qualifierNormal beats qualifierString
4Normal beats published valueNormal beats published valueFloat%
5Normal beats standard valueNormal beats standard valueFloat%

Data Table (Concise)
Data Table ( Complete ):     View All Data
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