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BioAssay: AID 128307

Agonistic activity by mouse acetic acid writhing test.

A series of 7-alkanoyl-substituted hydromorphone derivatives were prepared by acylation of the morpholine enamines. The most potent compound (6i) of the series was found to have agonist activity of the same order of magnitude as that of buprenorphine. The N-cyclopropylmethyl-substituted series was found to exhibit structure-activity relationships for analgesia and narcotic antagonism similar to those of the endo-ethanotetrahydrooripavines. ..more
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 Tested Compounds
 Tested Compounds
All(26)
 
 
Unspecified(26)
 
 
 Tested Substances
 Tested Substances
All(26)
 
 
Unspecified(26)
 
 
 Related BioAssays
 Related BioAssays
AID: 128307
Data Source: ChEMBL (125539)
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: Novel opiates and antagonists. 4. 7-Alkanoylhydromorphones.

Abstract: A series of 7-alkanoyl-substituted hydromorphone derivatives were prepared by acylation of the morpholine enamines. The most potent compound (6i) of the series was found to have agonist activity of the same order of magnitude as that of buprenorphine. The N-cyclopropylmethyl-substituted series was found to exhibit structure-activity relationships for analgesia and narcotic antagonism similar to those of the endo-ethanotetrahydrooripavines.
(PMID: 6181259)
Comment
Putative Target:

ChEMBL Target ID: 50594
Target Type: ORGANISM
Pref Name: Mus musculus
Organism: Mus musculus
Tax ID: 10090
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
1ED50 activity commentED50 activity commentString
2ED50 standard flagED50 standard flagInteger
3ED50 qualifierED50 qualifierString
4ED50 published valueED50 published valueFloatmg kg-1
5ED50 standard valueED50 standard valueFloatmg.kg-1

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