Switch to
| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
2
|
| pubmed:dateCreated |
1992-10-13
|
| pubmed:abstractText |
The effects of efaroxan (RX 821037A; 2-[2-(2-ethyl-2,3-dihydrobenzofuranyl)]-2-imidazoline HCl) at alpha 1- and alpha 2-adrenoceptors were investigated in isolated tissues, pithed rats and conscious rats. In isolated tissues, efaroxan competitively antagonised the inhibitory effects of p-aminoclonidine in the electrically stimulated (0.1 Hz) rat vas deferens, (pA2 = 8.89) and the contractile effects of phenylephrine on the rat anococcygeus muscle (pA2 = 6.03). Efaroxan had a selectivity ratio (alpha 2/alpha 1) of 724 compared to a value of 182 for idazoxan. In pithed rats, the i.v. doses of efaroxan (mumol/kg) producing 2-fold shifts in dose-response curves for UK-14,304 at prejunctional cardiac alpha 2-adrenoceptors and postjunctional vascular alpha 2-adrenoceptors, and for cirazoline at postjunctional vascular alpha 1-adrenoceptors, were 0.05, 0.13 and 2.96, respectively. In conscious fasted rats, prazosin (5 mg/kg p.o.) increased resting glucose levels and exacerbated the hyperglycaemic effects of UK-14,304 and adrenaline. In contrast, efaroxan (1-5 mg/kg p.o.) had little effect on resting plasma glucose but markedly antagonised the hyperglycaemic actions of UK-14,304 and adrenaline. Efaroxan increased resting plasma insulin levels and markedly potentiated the rise in insulin levels produced by adrenaline; this latter effect was prevented by the co-administration of propranolol. These results demonstrate that efaroxan is a potent and selective alpha 2-adrenoceptor antagonist and provide further support for the involvement of alpha 2-adrenoceptors in glucose homeostasis.
|
| pubmed:language |
eng
|
| pubmed:journal | |
| pubmed:citationSubset |
IM
|
| pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Adrenergic alpha-Antagonists,
http://linkedlifedata.com/resource/pubmed/chemical/Benzofurans,
http://linkedlifedata.com/resource/pubmed/chemical/Blood Glucose,
http://linkedlifedata.com/resource/pubmed/chemical/Clonidine,
http://linkedlifedata.com/resource/pubmed/chemical/Dioxanes,
http://linkedlifedata.com/resource/pubmed/chemical/Epinephrine,
http://linkedlifedata.com/resource/pubmed/chemical/Idazoxan,
http://linkedlifedata.com/resource/pubmed/chemical/Imidazoles,
http://linkedlifedata.com/resource/pubmed/chemical/Insulin,
http://linkedlifedata.com/resource/pubmed/chemical/Prazosin,
http://linkedlifedata.com/resource/pubmed/chemical/Quinoxalines,
http://linkedlifedata.com/resource/pubmed/chemical/apraclonidine,
http://linkedlifedata.com/resource/pubmed/chemical/brimonidine,
http://linkedlifedata.com/resource/pubmed/chemical/efaroxan
|
| pubmed:status |
MEDLINE
|
| pubmed:month |
Mar
|
| pubmed:issn |
0014-2999
|
| pubmed:author | |
| pubmed:issnType |
Print
|
| pubmed:day |
24
|
| pubmed:volume |
213
|
| pubmed:owner |
NLM
|
| pubmed:authorsComplete |
Y
|
| pubmed:pagination |
205-12
|
| pubmed:dateRevised |
2011-11-17
|
| pubmed:meshHeading |
pubmed-meshheading:1355733-Adrenergic alpha-Antagonists,
pubmed-meshheading:1355733-Animals,
pubmed-meshheading:1355733-Benzofurans,
pubmed-meshheading:1355733-Blood Glucose,
pubmed-meshheading:1355733-Clonidine,
pubmed-meshheading:1355733-Decerebrate State,
pubmed-meshheading:1355733-Dioxanes,
pubmed-meshheading:1355733-Dose-Response Relationship, Drug,
pubmed-meshheading:1355733-Epinephrine,
pubmed-meshheading:1355733-Idazoxan,
pubmed-meshheading:1355733-Imidazoles,
pubmed-meshheading:1355733-Insulin,
pubmed-meshheading:1355733-Male,
pubmed-meshheading:1355733-Muscles,
pubmed-meshheading:1355733-Prazosin,
pubmed-meshheading:1355733-Quinoxalines,
pubmed-meshheading:1355733-Rats,
pubmed-meshheading:1355733-Rats, Inbred Strains,
pubmed-meshheading:1355733-Vas Deferens
|
| pubmed:year |
1992
|
| pubmed:articleTitle |
Selectivity profile of the alpha 2-adrenoceptor antagonist efaroxan in relation to plasma glucose and insulin levels in the rat.
|
| pubmed:affiliation |
Research and Development Laboratories, Reckitt and Colman Pharmaceuticals, Kingston-upon-Hull, U.K.
|
| pubmed:publicationType |
Journal Article,
Comparative Study
|