Document Detail


Affinities of pirenzepine for muscarinic cholinergic receptors in membranes isolated from bovine tracheal mucosa and smooth muscle.
MedLine Citation:
PMID:  3826897     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Muscarinic cholinergic receptors have been classified into subtypes based on their high (M-1 subtype) or low (M-2 subtype) affinities for the nonclassic antagonist pirenzepine, and this classification has important experimental and therapeutic implications. Because muscarinic receptors are abundant in the airways where they mediate several different cellular responses, the goal of this study was to characterize the affinities of pirenzepine for the muscarinic receptors in bovine tracheal mucosa and smooth muscle. After isolating membrane particulates from mucosa and smooth muscle, as well as from bovine cerebral cortex (a known source of M-1 receptors), we used 3H-quinuclidinyl benzilate to label muscarinic receptors in the particulates and performed competition radioligand binding assays in the presence of either atropine or pirenzepine. Receptors from all 3 tissues (mucosa, smooth muscle, and cerebral cortex) were of a relatively uniform affinity for atropine (range of KI values: 0.8 +/- 0.4 X 10(-9) to 2.4 +/- 1.7 X 10(-9) M), as would be predicted for this classic muscarinic antagonist. By contrast, affinities for pirenzepine differed depending on the tissue. In cerebral cortex, the majority of receptors were of high affinity for pirenzepine (KI = 1.8 +/- 1.4 X 10(-8) M). In both mucosa and smooth muscle, receptors were of low affinity for pirenzepine (Kl = 4.8 +/- 0.4 to 6.9 +/- 3.8 X 10(-7) M). We conclude that muscarinic cholinergic receptors in bovine tracheal mucosa and smooth muscle are predominantly of the M-2 subtype.
Authors:
J M Madison; C A Jones; M Tom-Moy; J K Brown
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Publication Detail:
Type:  In Vitro; Journal Article; Research Support, Non-U.S. Gov't; Research Support, U.S. Gov't, Non-P.H.S.; Research Support, U.S. Gov't, P.H.S.    
Journal Detail:
Title:  The American review of respiratory disease     Volume:  135     ISSN:  0003-0805     ISO Abbreviation:  Am. Rev. Respir. Dis.     Publication Date:  1987 Mar 
Date Detail:
Created Date:  1987-04-14     Completed Date:  1987-04-14     Revised Date:  2007-11-14    
Medline Journal Info:
Nlm Unique ID:  0370523     Medline TA:  Am Rev Respir Dis     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  719-24     Citation Subset:  AIM; IM    
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MeSH Terms
Descriptor/Qualifier:
Animals
Binding, Competitive
Cattle
Mucous Membrane / metabolism
Muscle, Smooth / metabolism*
Pirenzepine / metabolism*
Quinuclidinyl Benzilate / metabolism
Receptors, Muscarinic / metabolism*
Trachea / metabolism*
Tritium / diagnostic use
Grant Support
ID/Acronym/Agency:
HL-0643/HL/NHLBI NIH HHS; HL-27669/HL/NHLBI NIH HHS
Chemical
Reg. No./Substance:
0/Receptors, Muscarinic; 10028-17-8/Tritium; 28797-61-7/Pirenzepine; 6581-06-2/Quinuclidinyl Benzilate

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


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