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BioAssay: AID 145933

50% Inhibition of stereospecific [3H]-naltrexone (10e-9 M) binding towards opiate receptor in rat brain homogenate

A series of novel 2- and 3-acylmorphinans (8-14) was synthesized in our search for a potent analgesic agent with low addiction potential. The compounds were evaluated for antinociceptive potency and receptor binding affinity. Among these compounds, the levorotatory 3-acetyl-N-(cyclopropylmethyl)morphinan (12) was found to be an orally active analgesic, comparable in potency to morphine (1), yet only weakly able to substitute for morphine (1) in morphine-dependent rats. ..more
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 Tested Compounds
 Tested Compounds
All(7)
 
 
Active(7)
 
 
 Tested Substances
 Tested Substances
All(7)
 
 
Active(7)
 
 
 Related BioAssays
 Related BioAssays
AID: 145933
Data Source: ChEMBL (143177)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-05-21
Modify Date: 2014-05-19

Data Table ( Complete ):           View Active Data    View All Data
BioActive Compounds: 7
Description:
Title: Acylmorphinans. A novel class of potent analgesic agents.

Abstract: A series of novel 2- and 3-acylmorphinans (8-14) was synthesized in our search for a potent analgesic agent with low addiction potential. The compounds were evaluated for antinociceptive potency and receptor binding affinity. Among these compounds, the levorotatory 3-acetyl-N-(cyclopropylmethyl)morphinan (12) was found to be an orally active analgesic, comparable in potency to morphine (1), yet only weakly able to substitute for morphine (1) in morphine-dependent rats.
(PMID: 2863378)
Comment
Compounds with activity <= 50uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.
Putative Target:
ChEMBL Target ID: 104711
Target Type: PROTEIN FAMILY
Pref Name: Opioid receptor
Synonyms: D-OR-1;Delta-type opioid receptor;DOR-1;Opioid receptor A;K-OR-1;Kappa-type opioid receptor;KOR-1;M-OR-1;MOR-1;Mu-type opioid receptor;Opioid receptor B;Sigma 1-type opioid receptor;Sigma non-opioid intracellular receptor 1;Sigma1-receptor;Sigma1R;
Gene Name: Oprd1;Ror-a;Oprk1;Ror-d;Oprm1;Ror-b;Oprs1;Sigmar1;
Protein Accession: P33533;P34975;P33535;Q9R0C9;
Protein GI: 464311;464313;464314;81882051;
Organism: Rattus norvegicus
Tax ID: 10116
Target Classification 1: membrane receptor
Target Classification 2: membrane receptor 7tm1 peptide short peptide opioid receptor
Confidence: Multiple homologous protein targets may be assigned
Relationship Type: Homologous protein target assigned
Categorized Comment - additional comments and annotations
From ChEMBL:
Assay Type: Binding
Assay Data Source: Scientific Literature
BAO: Assay Format: tissue-based format
Assay Tissue: Brain
Result Definitions
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TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1IC50*IC50 PubChem standard valueFloatμM
3BEIBinding Efficiency Index(nM)Float
2SEISurface Efficiency Index(nM)Float
4LELigand EfficiencyFloat
5LLELipophilic Ligand EfficiencyFloat
6IC50 activity commentIC50 activity commentString
7IC50 standard flagIC50 standard flagInteger
8IC50 qualifierIC50 qualifierString
9IC50 published valueIC50 published valueFloatM
10IC50 standard valueIC50 standard valueFloatnM
11IC50 data validityIC50 data validityString

* Activity Concentration.

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