Switch to
| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
1
|
| pubmed:dateCreated |
1992-9-14
|
| pubmed:abstractText |
Muscarinic receptors of resistance vessels (submucosal arterioles, outside diameter 50-75 microns) from the guinea-pig small intestine were investigated in vitro using a computer-assisted videomicroscopy system (Diamtrak). The muscarinic receptor which mediates vasodilation of precontracted [U-46619 (300 nM) or (-)-noradrenaline (10 microM)] arterioles was characterized with several muscarinic agonists and subtype-selective antagonists. The following agonists all produced equivalent maximum vasodilation (given in rank order of potency): acetylcholine = arecaidine propargyl ester (APE) greater than oxotremorine = (+/-)-muscarine = (+/-)-methacholine greater than carbachol greater than 4-[[N-(4-chlorophenyl)carbamoyl]oxy]-2-butynyltrimethylammonium iodide (4-Cl-McN-A-343). 4-[[N-(3-Chlorophenyl)-carbamoyl]oxy]-2-butynyltrimethylammonium chloride (McN-A-343) and N-ethyl-guvacine propargyl ester (NEN-APE) produced minimal or no arteriolar vasodilation. The muscarinic antagonists pirenzepine, (+-)-5,11-dihydro-11-[[[2-[2-((dipropylamino)methyl)-1-piperidinyl] ethyl]amino]-carbonyl]-6H-pyrido(2,3-b)(1,4)-benzodiazepin-6-one (AF-DX 384), 11-[[4-[4-(diethylamino)butyl]-1-piperidinyl]acetyl]-5,11-dihydro- 6H-pyrido(2,3-b)(1,4)-benzodiazepin-6-one (AQ-RA 741), p-fluorohexahydro-sila-difenidol (p-F-HHSiD), 4-diphenylacetoxy-N-methylpiperidine methiodide (4-DAMP) and (R)- and (S)-hexahydro-difenidol [(R)-HHD, (S)-HHD] shifted the muscarine, methacholine or carbachol dose-response curve to the right in a competitive manner. Schild analysis of the data yielded pA2 values for pirenzepine (6.74/6.9), AF-DX 384 (6.72), AQ-RA 741 (6.58), p-F-HHSiD (7.53/7.57), 4-DAMP (9.06), (R)-HHD (7.88/8.32) and (S)-HHD (5.52/5.88). Thus, it can be concluded that submucosal arterioles possess only the M3 functional muscarinic receptor, the activation of which causes blood vessel dilation.(ABSTRACT TRUNCATED AT 250 WORDS)
|
| pubmed:grant | |
| pubmed:language |
eng
|
| pubmed:journal | |
| pubmed:citationSubset |
IM
|
| pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/15-Hydroxy-11 alpha,9...,
http://linkedlifedata.com/resource/pubmed/chemical/4-diphenylacetoxy-1,1-dimethylpiperi...,
http://linkedlifedata.com/resource/pubmed/chemical/AFDX 384,
http://linkedlifedata.com/resource/pubmed/chemical/AQ-RA 741,
http://linkedlifedata.com/resource/pubmed/chemical/Acetylcholine,
http://linkedlifedata.com/resource/pubmed/chemical/Benzodiazepinones,
http://linkedlifedata.com/resource/pubmed/chemical/Carbachol,
http://linkedlifedata.com/resource/pubmed/chemical/Methacholine Chloride,
http://linkedlifedata.com/resource/pubmed/chemical/Muscarine,
http://linkedlifedata.com/resource/pubmed/chemical/Muscarinic Antagonists,
http://linkedlifedata.com/resource/pubmed/chemical/Oxotremorine,
http://linkedlifedata.com/resource/pubmed/chemical/Parasympatholytics,
http://linkedlifedata.com/resource/pubmed/chemical/Parasympathomimetics,
http://linkedlifedata.com/resource/pubmed/chemical/Piperidines,
http://linkedlifedata.com/resource/pubmed/chemical/Pirenzepine,
http://linkedlifedata.com/resource/pubmed/chemical/Prostaglandin Endoperoxides...,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Muscarinic
|
| pubmed:status |
MEDLINE
|
| pubmed:month |
Mar
|
| pubmed:issn |
0014-2999
|
| pubmed:author | |
| pubmed:issnType |
Print
|
| pubmed:day |
17
|
| pubmed:volume |
213
|
| pubmed:owner |
NLM
|
| pubmed:authorsComplete |
Y
|
| pubmed:pagination |
53-61
|
| pubmed:dateRevised |
2007-11-14
|
| pubmed:meshHeading |
pubmed-meshheading:1499657-15-Hydroxy-11 alpha,9...,
pubmed-meshheading:1499657-Acetylcholine,
pubmed-meshheading:1499657-Animals,
pubmed-meshheading:1499657-Arterioles,
pubmed-meshheading:1499657-Benzodiazepinones,
pubmed-meshheading:1499657-Carbachol,
pubmed-meshheading:1499657-Guinea Pigs,
pubmed-meshheading:1499657-Ileum,
pubmed-meshheading:1499657-Methacholine Chloride,
pubmed-meshheading:1499657-Muscarine,
pubmed-meshheading:1499657-Muscarinic Antagonists,
pubmed-meshheading:1499657-Oxotremorine,
pubmed-meshheading:1499657-Parasympatholytics,
pubmed-meshheading:1499657-Parasympathomimetics,
pubmed-meshheading:1499657-Piperidines,
pubmed-meshheading:1499657-Pirenzepine,
pubmed-meshheading:1499657-Prostaglandin Endoperoxides, Synthetic,
pubmed-meshheading:1499657-Receptors, Muscarinic,
pubmed-meshheading:1499657-Vasodilation
|
| pubmed:year |
1992
|
| pubmed:articleTitle |
Characterization of muscarinic receptors mediating vasodilation in guinea-pig ileum submucosal arterioles by the use of computer-assisted videomicroscopy.
|
| pubmed:affiliation |
Department of Pharmacology, University of Frankfurt, Germany.
|
| pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, P.H.S.,
Research Support, Non-U.S. Gov't
|