Document Detail


Guanine nucleotides decrease the affinity of substance P binding to its receptor.
MedLine Citation:
PMID:  1694776     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
The inhibitory effect of guanine nucleotides on the binding of 125I-Bolton-Hunter conjugated substance P (125I-BHSP) to rat submaxillary gland membranes has been confirmed and further explored. The evidence presented here indicates that this is due to a marked loss of binding affinity. In the presence of 5'-guanylyl imidodiphosphate (GppNHp) there is (1) a greater than or equal to 20-fold increase in the Kd as determined by Scatchard analysis and (2) the concentration of SP required to inhibit half of the 125I-BHSP binding (IC50) increased approximately 30-fold. Consistent with a marked decrease in affinity is an approximately 100-fold increase in the rate of dissociation of 125I-BHSP following addition of GppNHp. Complete restoration of high-affinity binding was achieved by removal of the guanine nucleotide.
Authors:
J Luber-Narod; N D Boyd; S E Leeman
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Publication Detail:
Type:  Journal Article; Research Support, U.S. Gov't, P.H.S.    
Journal Detail:
Title:  European journal of pharmacology     Volume:  188     ISSN:  0014-2999     ISO Abbreviation:  Eur. J. Pharmacol.     Publication Date:  1990 Apr 
Date Detail:
Created Date:  1990-08-13     Completed Date:  1990-08-13     Revised Date:  2007-11-14    
Medline Journal Info:
Nlm Unique ID:  1254354     Medline TA:  Eur J Pharmacol     Country:  NETHERLANDS    
Other Details:
Languages:  eng     Pagination:  185-91     Citation Subset:  IM    
Affiliation:
Department of Physiology, University of Massachusetts Medical School, Worcester 01655.
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MeSH Terms
Descriptor/Qualifier:
Guanine Nucleotides / pharmacology*
Guanylyl Imidodiphosphate / pharmacology
Indicators and Reagents
Iodine Radioisotopes / diagnostic use
Kinetics
Membranes / drug effects,  metabolism
Receptors, Neurokinin-1
Receptors, Neurotransmitter / metabolism*
Submandibular Gland / drug effects,  metabolism
Substance P / diagnostic use,  metabolism*
Succinimides / diagnostic use
Grant Support
ID/Acronym/Agency:
DK29876/DK/NIDDK NIH HHS; NS25151/NS/NINDS NIH HHS
Chemical
Reg. No./Substance:
0/Bolton Hunter reagent-substance P conjugate; 0/Guanine Nucleotides; 0/Indicators and Reagents; 0/Iodine Radioisotopes; 0/Receptors, Neurokinin-1; 0/Receptors, Neurotransmitter; 0/Succinimides; 33507-63-0/Substance P; 34273-04-6/Guanylyl Imidodiphosphate

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


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