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BioAssay: AID 708697

Antagonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation counting analysis

In the search for opioid ligands with mixed functional activity, a series of 5'-(4-chlorophenyl)-4,5alpha-epoxypyridomorphinans possessing alkoxy or acyloxy groups at C-14 was synthesized and evaluated. In this series, the affinity and functional activity of the ligands were found to be influenced by the nature of the substituent at C-14 as well as by the substituent at N-17. Whereas the more ..
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 Tested Compounds
 Tested Compounds
All(15)
 
 
Active(6)
 
 
Inconclusive(9)
 
 
 Tested Substances
 Tested Substances
All(15)
 
 
Active(6)
 
 
Inconclusive(9)
 
 
AID: 708697
Data Source: ChEMBL (876440)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2013-06-29
Modify Date: 2014-05-25

Data Table ( Complete ):           View Active Data    View All Data
Target
Sequence: RecName: Full=Mu-type opioid receptor; Short=M-OR-1; Short=MOR-1; AltName: Full=Mu opiate receptor; AltName: Full=Mu opioid receptor; Short=MOP; Short=hMOP
Description ..   
Protein Family: Serpentine type 7TM GPCR chemoreceptor Srx
Comment ..   

Gene:OPRM1     Related Protein 3D Structures     More BioActivity Data..
BioActive Compounds: 6
Description:
Title: 14-Alkoxy- and 14-acyloxypyridomorphinans: mu agonist/delta antagonist opioid analgesics with diminished tolerance and dependence side effects.

Abstract: In the search for opioid ligands with mixed functional activity, a series of 5'-(4-chlorophenyl)-4,5alpha-epoxypyridomorphinans possessing alkoxy or acyloxy groups at C-14 was synthesized and evaluated. In this series, the affinity and functional activity of the ligands were found to be influenced by the nature of the substituent at C-14 as well as by the substituent at N-17. Whereas the incorporation of a 3-phenylpropoxy group at C-14 on N-methylpyridomorhinan gave a dual MOR agonist/DOR agonist 17h, its incorporation on N-cyclopropylmethylpyridomorphinan gave a MOR agonist/DOR antagonist 17d. Interestingly, 17d, in contrast to 17h, did not produce tolerance or dependence effects upon prolonged treatment in cells expressing MOR and DOR. Moreover, 17d displayed greatly diminished analgesic tolerance as compared to morphine upon repeated administration, thus supporting the hypothesis that ligands with MOR agonist/DOR antagonist functional activity could emerge as novel analgesics devoid of tolerance, dependence, and related side effects.
(PMID: 23016952)
Comment
Compounds with activity <= 50uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.

Categorized Comment
Assay Type: Binding

Assay Data Source: Scientific Literature

BAO: Assay Format: cell-based format

Assay Cell Type: CHO

Target Type: Target is a single protein chain

Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Ke activity commentKe activity commentString
2Ke standard flagKe standard flagInteger
3Ke qualifierKe qualifierString
4Ke published valueKe published valueFloatnM
5Ke standard valueKe standard valueFloatnM

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