Document Detail


Pharmacological characterization of histamine H3 receptors in isolated guinea pig pulmonary artery and ileum.
MedLine Citation:
PMID:  8788448     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
We characterized the histamine H3 receptors involved in the modulation of electrical field stimulated neurogenic contraction of guinea pig pulmonary artery sympathetic, and guinea pig ileum parasympathetic preparations. Simultaneous measures of electrical field stimulation-evoked 3H overflow and tension in [3H]norepinephrine-loaded pulmonary artery were sensitive to tetrodotoxin (300 nM) and insensitive to hexamethonium (100 microM). Only the contractile response was inhibited by prazosin (100 nM). (R)-alpha-Methylhistamine's inhibition of the pulmonary artery contraction and 3H overflow were dose-dependently antagonized by thioperamide (30-100 nM). (R)-alpha-Methylhistamine also inhibited the neurogenic contractions of the isolated ileum (pD2 = 8.2). In the pulmonary artery, the relative potency of the histamine H3 receptor antagonists vs. (R)-alpha-methylhistamine inhibition of neurogenic contractions (pD2 = 7.1) was thioperamide (pA2 = 8.6 +/- 0.1) > burimamide (pA2 = 7.6 +/- 0.2) > impromidine (pA2 = 6.9 +/- 0.02). Similarly, the relative potency of histamine H3 receptor antagonists in the isolated ileum was thioperamide > burimamide > or = impromidine, with pA2 estimates of 8.7 +/- 0.1, 7.3 +/- 0.1 and 7.1 +/- 0.1, respectively. Antagonist potencies suggest a predominant histamine H3A-like receptor population on postganglionic sympathetic neurons innervating the pulmonary artery and parasympathetic neurons innervating the ileum longitudinal muscle.
Authors:
C A Rizzo; S Tozzi; M E Monahan; J A Hey
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Publication Detail:
Type:  In Vitro; Journal Article    
Journal Detail:
Title:  European journal of pharmacology     Volume:  294     ISSN:  0014-2999     ISO Abbreviation:  Eur. J. Pharmacol.     Publication Date:  1995 Dec 
Date Detail:
Created Date:  1997-02-12     Completed Date:  1997-02-12     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  1254354     Medline TA:  Eur J Pharmacol     Country:  NETHERLANDS    
Other Details:
Languages:  eng     Pagination:  329-35     Citation Subset:  IM    
Affiliation:
Schering-Plough Research Institute, Kenilworth, NJ 07033, USA.
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MeSH Terms
Descriptor/Qualifier:
Animals
Brain Chemistry / drug effects
Electric Stimulation
Guinea Pigs
Histamine Agonists / pharmacology
Histamine Antagonists / pharmacology
Ileum / drug effects
Methylhistamines / pharmacology
Muscle Contraction / drug effects
Muscle, Smooth / drug effects*
Muscle, Smooth, Vascular / drug effects*
Norepinephrine / metabolism,  pharmacology
Piperidines / pharmacology
Pulmonary Artery / drug effects
Receptors, Histamine H3 / drug effects*
Vasoconstrictor Agents / metabolism,  pharmacology
Chemical
Reg. No./Substance:
0/Histamine Agonists; 0/Histamine Antagonists; 0/Methylhistamines; 0/Piperidines; 0/Receptors, Histamine H3; 0/Vasoconstrictor Agents; 106243-16-7/thioperamide; 51-41-2/Norepinephrine; 6986-90-9/alpha-methylhistamine

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


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