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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
3
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pubmed:dateCreated |
1993-10-14
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pubmed:abstractText |
Binding of 5-[3H]methylurapidil to guinea pig liver membranes was rapid, saturable, and reversible. Scatchard analysis of saturation isotherms indicated a single class of binding sites with a Kd of 0.86 nM and a Bmax of 36 fmol/mg of protein. Preincubation of the membranes with chlorethylclonidine did not alter significantly the binding parameters for 5-[3H]methylurapidil. Binding competition experiments were performed, and the order of potency for agonists was oxymetazoline > epinephrine > norepinephrine >> methoxamine; for antagonists, the potency order was (+)-niguldipine > or = 5-methylurapidil = prazosin = WB4101 > benoxathian > or = phentolamine > or = (-)-niguldipine. The binding affinity for epinephrine was modulated by the hydrolysis-resistant GTP analogue guanosine-5'-(beta, gamma-imido)triphosphate. The pharmacological profile of the 5-[3H]methylurapidil binding sites of guinea pig liver differs markedly from those of the cloned alpha 1-adrenoceptors (i.e., alpha 1B-, alpha 1C-, and alpha 1A/D-adrenoceptors) and resembles that of the classical alpha 1A receptor subtype.
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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/5-methylurapidil,
http://linkedlifedata.com/resource/pubmed/chemical/Alkylating Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Clonidine,
http://linkedlifedata.com/resource/pubmed/chemical/Piperazines,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Adrenergic, alpha,
http://linkedlifedata.com/resource/pubmed/chemical/chlorethylclonidine
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pubmed:status |
MEDLINE
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pubmed:month |
Sep
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pubmed:issn |
0026-895X
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
44
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
589-94
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:8396719-Alkylating Agents,
pubmed-meshheading:8396719-Animals,
pubmed-meshheading:8396719-Binding, Competitive,
pubmed-meshheading:8396719-Clonidine,
pubmed-meshheading:8396719-Guinea Pigs,
pubmed-meshheading:8396719-Liver,
pubmed-meshheading:8396719-Male,
pubmed-meshheading:8396719-Piperazines,
pubmed-meshheading:8396719-Radioligand Assay,
pubmed-meshheading:8396719-Receptors, Adrenergic, alpha
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pubmed:year |
1993
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pubmed:articleTitle |
Characterization of the alpha 1A-adrenoceptors of guinea pig liver membranes: studies using 5-[3H]methylurapidil.
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pubmed:affiliation |
Instituto de Fisiología Celular, Universidad Nacional Autónoma de México, México City.
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pubmed:publicationType |
Journal Article,
In Vitro,
Research Support, Non-U.S. Gov't
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