Document Detail


A probe for octopamine receptors: synthesis of 2-[(4-azido-2,6-diethylphenyl)imino]imidazolidine and its tritiated derivative, a potent reversible-irreversible activator of octopamine-sensitive adenylate cyclase.
MedLine Citation:
PMID:  2502628     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
In order to develop an irreversible ligand for octopamine receptors, a highly potent azido-substituted 2-(phenyl-imino)imidazolidine (NC-5Z, 8) and its tritiated derivative (3H-NC-5Z, 11) have been designed and synthesized. Under reversible-binding conditions, NC-5Z is 50-100-fold more potent than octopamine in activating octopamine-sensitive adenylate cyclase in a variety of tissues. After photolysis, 3H-NC-5Z binds irreversibly to cell membranes, and this binding is reduced by preincubation with octopamine agonists and antagonists but not by norepinephrine, dopamine, serotonin, or histamine. NC-5Z should be useful both as a potent reversible octopamine agonist and as an affinity probe for characterizing and isolating octopamine-receptor proteins.
Authors:
J A Nathanson; G Kaugars
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't; Research Support, U.S. Gov't, Non-P.H.S.    
Journal Detail:
Title:  Journal of medicinal chemistry     Volume:  32     ISSN:  0022-2623     ISO Abbreviation:  J. Med. Chem.     Publication Date:  1989 Aug 
Date Detail:
Created Date:  1989-09-07     Completed Date:  1989-09-07     Revised Date:  2008-11-21    
Medline Journal Info:
Nlm Unique ID:  9716531     Medline TA:  J Med Chem     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  1795-9     Citation Subset:  IM    
Affiliation:
Department of Neurology, Harvard Medical School, Massachusetts General Hospital, Boston 02114.
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MeSH Terms
Descriptor/Qualifier:
Adenylate Cyclase / metabolism*
Azides / chemical synthesis*,  pharmacology
Chemical Phenomena
Chemistry
Enzyme Activation / drug effects
Imidazoles / chemical synthesis*,  pharmacology
Imidazolidines*
Octopamine / pharmacology
Receptors, Adrenergic / metabolism*
Receptors, Biogenic Amine*
Tritium / diagnostic use
Chemical
Reg. No./Substance:
0/Azides; 0/Imidazoles; 0/Imidazolidines; 0/Receptors, Adrenergic; 0/Receptors, Biogenic Amine; 0/norsynephrine receptor; 10028-17-8/Tritium; 104-14-3/Octopamine; 121158-53-0/NC 5Z; EC 4.6.1.1/Adenylate Cyclase

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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