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PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
4
pubmed:dateCreated
1996-7-24
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.
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
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Feb
pubmed:issn
0007-1188
pubmed:author
pubmed:issnType
Print
pubmed:volume
117
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
703-11
pubmed:dateRevised
2009-11-18
pubmed:meshHeading
pubmed:year
1996
pubmed:articleTitle
Comparison of guinea-pig, bovine and rat alpha 1-adrenoceptor subtypes.
pubmed:affiliation
Department of Pediatrics, University of Essen, Germany.
pubmed:publicationType
Journal Article, Comparative Study, In Vitro, Research Support, Non-U.S. Gov't