Source:http://linkedlifedata.com/resource/pubmed/id/10323493
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
4
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pubmed:dateCreated |
1999-6-29
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pubmed:abstractText |
The specific binding of [3H]QNB to rat duodenum smooth muscle membranes was a saturable process and Scatchard transformation of the saturation curves indicated a linear plot (nH = 1.017+/-0.071). The K(D) and Bmax values were 0.168+/-0.025 nM and 46.7+/-8.6 fmol/mg protein, respectively. Analyses of competition curves using pirenzepine and guanylpirenzepine indicated more than one class of binding site. A minor population of muscarinic binding sites showed high affinity (M1) for both pirenzepine (19.3+/-1.2%; pKi = 8.29+/-0.36) and guanylpirenzepine (29.4+/-2.0%; pKi = 7.28+/-0.11). The antagonistic affinity values of pirenzepine and guanylpirenzepine for the remaining low affinity binding sites, and that of methoctramine indicated the presence of both M2 and M3 subtypes. McN-A-343 produced relaxations in rat duodenum and inhibited twitch contractions of rabbit vas deferens induced by electrical stimulation in a concentration dependent manner. Carbachol (Cch) exerted concentration-dependent negative inotropic effect in rat atria and contractile effects in guinea-pig gallbladder and ileum longitudinal muscle-myenteric plexus preparation. Imperaline displaced the concentration-response curves to McN-A-343 and Cch to the right in parallel, without affecting the maximum responses in all tissues studied. The rank order of the pA2 values was rabbit vas deferens > rat atria > guinea-pig gallbladder = guinea-pig ileum > rat duodenum. The presynaptic muscarinic receptors at the rat duodenum and rabbit vas deferens were concluded to be of M1 and M4 subtypes, respectively.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Cevanes,
http://linkedlifedata.com/resource/pubmed/chemical/Diamines,
http://linkedlifedata.com/resource/pubmed/chemical/Muscarinic Antagonists,
http://linkedlifedata.com/resource/pubmed/chemical/Quinuclidinyl Benzilate,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Muscarinic,
http://linkedlifedata.com/resource/pubmed/chemical/methoctramine,
http://linkedlifedata.com/resource/pubmed/chemical/peiminine
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pubmed:status |
MEDLINE
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pubmed:month |
Apr
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pubmed:issn |
0306-3623
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
32
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
505-11
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:10323493-Animals,
pubmed-meshheading:10323493-Binding, Competitive,
pubmed-meshheading:10323493-Binding Sites,
pubmed-meshheading:10323493-Cevanes,
pubmed-meshheading:10323493-Diamines,
pubmed-meshheading:10323493-Duodenum,
pubmed-meshheading:10323493-Female,
pubmed-meshheading:10323493-Guinea Pigs,
pubmed-meshheading:10323493-Ileum,
pubmed-meshheading:10323493-Male,
pubmed-meshheading:10323493-Muscarinic Antagonists,
pubmed-meshheading:10323493-Quinuclidinyl Benzilate,
pubmed-meshheading:10323493-Rabbits,
pubmed-meshheading:10323493-Rats,
pubmed-meshheading:10323493-Rats, Wistar,
pubmed-meshheading:10323493-Receptors, Muscarinic
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pubmed:year |
1999
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pubmed:articleTitle |
Subtypes of muscarinic receptors in rat duodenum: a comparison with rabbit vas deferens, rat atria, guinea-pig ileum and gallbladder by using imperialine.
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pubmed:affiliation |
Department of Pharmacology, Istanbul University School of Pharmacy, Turkey.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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