Document Detail

Differences in the effects of tachykinin NK1 receptor antagonists: neuronal versus smooth muscle tissues.
MedLine Citation:
PMID:  7509748     Owner:  NLM     Status:  MEDLINE    
The effects of three tachykinin NK1 receptor antagonists (L-668,169, (+/-)-RP 67580, and (+/-)-CP 96.345) were examined for their ability to antagonise responses evoked by substance P O-methyl ester (a selective NK1 receptor agonist) in isolated neuronal tissue (rat superior cervical ganglia and guinea-pig locus coeruleus) and smooth muscle tissues (rat urinary bladder and guinea-pig ileum longitudinal muscle/myenteric plexus). (+/-)-RP 67580 was similarly effective in antagonising responses in both rat superior cervical ganglia and urinary bladder (estimated pKa value = 7.4 for both tissues); however, (+/-)-CP 96,345 was 50-fold less effective in antagonising responses in guinea-pig locus coeruleus than in ileum longitudinal muscle/myenteric plexus (estimated pKa values = 7.6 and 9.3 respectively). It is suggested that the differential effects of (+/-)-CP 96,345 may reflect the existence of a population of NK1 receptors within guinea-pig locus coeruleus that are less sensitive to the effects of this NK1 receptor antagonist.
G R Seabrook; M J Main; Z Razzaque; J Longmore
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Publication Detail:
Type:  Comparative Study; In Vitro; Journal Article    
Journal Detail:
Title:  European journal of pharmacology     Volume:  250     ISSN:  0014-2999     ISO Abbreviation:  Eur. J. Pharmacol.     Publication Date:  1993 Nov 
Date Detail:
Created Date:  1994-04-04     Completed Date:  1994-04-04     Revised Date:  2013-06-05    
Medline Journal Info:
Nlm Unique ID:  1254354     Medline TA:  Eur J Pharmacol     Country:  NETHERLANDS    
Other Details:
Languages:  eng     Pagination:  125-31     Citation Subset:  IM    
Department of Pharmacology, Merck Sharp & Dohme Research Laboratories, Harlow, Essex, UK.
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MeSH Terms
Biphenyl Compounds / pharmacology
Guinea Pigs
Ileum / drug effects
Indoles / pharmacology
Locus Coeruleus / drug effects*
Muscle, Smooth / drug effects*
Myenteric Plexus / drug effects
Neurons / drug effects
Peptides, Cyclic / pharmacology
Rats, Sprague-Dawley
Receptors, Neurokinin-1 / antagonists & inhibitors*
Substance P / analogs & derivatives*,  pharmacology
Superior Cervical Ganglion / drug effects*
Urinary Bladder / drug effects
Reg. No./Substance:
0/Biphenyl Compounds; 0/Indoles; 0/Isoindoles; 0/Peptides, Cyclic; 0/Receptors, Neurokinin-1; 132746-60-2/CP 96345; 135911-02-3/7,7-diphenyl-2-(1-imino-2-(2-methoxyphenyl)ethyl)perhydroisoindol-4-one; 137012-28-3/L 668169; 33507-63-0/Substance P; 76260-78-1/substance P, methyl ester-

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

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