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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
4
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pubmed:dateCreated |
1996-7-24
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pubmed:abstractText |
1. To elucidate a possible role of species differences in the classification of alpha 1-adrenoceptor subtypes, we have characterized the alpha 1-adrenoceptors in guinea-pig spleen, kidney and cerebral cortex and in bovine cerebral cortex using concentration-dependent alkylation by chloroethylclonidine and competitive binding with 5-methlurapidil, methoxamine, (+)-niguldipine, noradrenaline, oxymetazoline, phentolamine, SDZ NVI-085, tamsulosin and (+)-tamsulosin. Rat liver alpha 1B-adrenoceptors were studied for comparison. Chloroethylclonidine-sensitivity and (+)-niguldipine affinity were also compared at cloned rat and bovine alpha 1a-adrenoceptors. 2. Chloroethylclonidine concentration-dependently inactivated alpha 1-adrenoceptors in all five tissues. While chloroethylclonidine inactivated almost all alpha 1-adrenoceptors in rat liver and guinea-pig kidney and brain, 20-30% of alpha 1-adrenoceptors in guinea-pig spleen and bovine brain were resistant to alkylation by 10 microM chloroethylclonidine. With regard to concentration-dependency guinea-pig kidney and brain were approximately 10 fold less sensitive than guinea-pig spleen or rat liver. 3. In rat liver, all drugs tested competed for [3H]-prazosin binding with steep and monophasic curves. Drug affinities were relatively low and resembled most closely those of cloned rat alpha 1b-adrenoceptors. 4. In guinea-pig spleen, all drugs tested competed for [3H]-prazosin binding with steep and monophasic curves. Drug affinities were relatively low and resembled most closely those of cloned rat alpha 1b-adrenoceptors. 5. In guinea-pig kidney most drugs tested competed for [3H]-prazosin binding with steep and monophasic curves and had relatively low drug affinities close to those of cloned rat alpha 1b- and alpha 1d-adrenoceptors. However, noradrenaline and tamsulosin had consistently biphasic competition curves recognizing 36-39% high and 61-64% low affinity sites. 6. In guinea-pig cerebral cortex, all drugs tested competed for [3H]-prazosin binding with shallow and biphasic curves. While most drugs recognized approximately 25% high affinity sites, tamsulosin and noradrenaline recognized approximately 50% high affinity sites. Drug affinities at the high and low affinity sites except those for tamsulosin and noradrenaline resembled those at cloned alpha 1a- and alpha 1b-adrenoceptors, respectively. 7. In bovine cerebral cortex all drugs tested except for noradrenaline competed for [3H]-prazosin binding with shallow and biphasic curves. All drugs recognized approximately 70% high affinity sites. Drug affinities at the high and low affinity sites resembled those at cloned alpha 1a- and alpha 1b-adrenoceptors, respectively. Noradrenaline competition curves in bovine cerebral cortex were steep and monophasic. 8. When cloned rat and bovine alpha 1a-adrenoceptors transiently expressed in COS cells were studied in a direct side-by-side comparison, both species homologues had similar chloroethylclonidine-sensitivity and (+)-niguldipine affinity. 9. We conclude that properties of bovine alpha 1A- and alpha 1B-adrenoceptors are very similar to those of other species such as rat. alpha 1-Adrenoceptor subtypes in guinea-pigs resemble alpha 1A- and alpha 1B-adrenoceptors in other species but chloroethylclonidine sensitivity and competition binding profiles of noradrenaline and tamsulosin are not compatible with previously established alpha 1-adrenoceptor subtype classification.
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pubmed:commentsCorrections |
http://linkedlifedata.com/resource/pubmed/commentcorrection/8646417-1313395,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8646417-1359975,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8646417-1379805,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8646417-1681417,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8646417-1706716,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8646417-1970822,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8646417-2548881,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8646417-2569345,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8646417-2835650,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8646417-2845398,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8646417-2853370,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8646417-2901974,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8646417-7477417,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8646417-7506392,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8646417-7815325,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8646417-7908116,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8646417-7911718,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8646417-7916507,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8646417-7935320,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8646417-7938162,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8646417-7969068,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8646417-7988645,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8646417-7990970,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8646417-7996431,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8646417-8024574,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8646417-8183249,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8646417-8264553,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8646417-942051
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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/Adrenergic alpha-Agonists,
http://linkedlifedata.com/resource/pubmed/chemical/Adrenergic alpha-Antagonists,
http://linkedlifedata.com/resource/pubmed/chemical/Clonidine,
http://linkedlifedata.com/resource/pubmed/chemical/Prazosin,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Adrenergic, alpha-1,
http://linkedlifedata.com/resource/pubmed/chemical/Tritium,
http://linkedlifedata.com/resource/pubmed/chemical/chlorethylclonidine
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pubmed:status |
MEDLINE
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pubmed:month |
Feb
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pubmed:issn |
0007-1188
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
117
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
703-11
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pubmed:dateRevised |
2009-11-18
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pubmed:meshHeading |
pubmed-meshheading:8646417-Adrenergic alpha-Agonists,
pubmed-meshheading:8646417-Adrenergic alpha-Antagonists,
pubmed-meshheading:8646417-Animals,
pubmed-meshheading:8646417-Binding, Competitive,
pubmed-meshheading:8646417-Cattle,
pubmed-meshheading:8646417-Clonidine,
pubmed-meshheading:8646417-Guinea Pigs,
pubmed-meshheading:8646417-Male,
pubmed-meshheading:8646417-Prazosin,
pubmed-meshheading:8646417-Radioligand Assay,
pubmed-meshheading:8646417-Rats,
pubmed-meshheading:8646417-Rats, Wistar,
pubmed-meshheading:8646417-Receptors, Adrenergic, alpha-1,
pubmed-meshheading:8646417-Species Specificity,
pubmed-meshheading:8646417-Tritium
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pubmed:year |
1996
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pubmed:articleTitle |
Comparison of guinea-pig, bovine and rat alpha 1-adrenoceptor subtypes.
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pubmed:affiliation |
Department of Pediatrics, University of Essen, Germany.
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pubmed:publicationType |
Journal Article,
Comparative Study,
In Vitro,
Research Support, Non-U.S. Gov't
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