| pubmed-article:1677298 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:1677298 | lifeskim:mentions | umls-concept:C0031330 | lld:lifeskim |
| pubmed-article:1677298 | lifeskim:mentions | umls-concept:C2003941 | lld:lifeskim |
| pubmed-article:1677298 | lifeskim:mentions | umls-concept:C0231491 | lld:lifeskim |
| pubmed-article:1677298 | lifeskim:mentions | umls-concept:C0082604 | lld:lifeskim |
| pubmed-article:1677298 | pubmed:issue | 4 | lld:pubmed |
| pubmed-article:1677298 | pubmed:dateCreated | 1991-8-28 | lld:pubmed |
| pubmed-article:1677298 | pubmed:abstractText | 1. This paper describes the pharmacology of the novel alpha 2-adrenoceptor antagonist fluparoxan (GR 50360) which is currently being studied clinically as a potential anti-depressant. Idazoxan and yohimbine were included in many studies for comparison. 2. In the rat isolated, field-stimulated vas deferens and the guinea-pig isolated, field-stimulated ileum preparations, fluparoxan was a reversible competitive antagonist of the inhibitory responses to the alpha 2-adrenoceptor agonist UK-14304 with pKB values of 7.87 and 7.89 respectively. In the rat isolated anococcygeus muscle, fluparoxan was a much weaker competitive antagonist of the contractile response to the alpha 1-adrenoceptor agonist phenylephrine with a pKB of 4.45 giving an alpha 2: alpha 1-adrenoceptor selectivity ratio of greater than 2500. 3. In the conscious mouse, fluparoxan (0.2-3.0 mg kg-1) was effective by the oral route and of similar potency to idazoxan in preventing clonidine-induced hypothermia and antinociception. In the rat, UK-14304-induced hypothermia (ED50 = 1.4 mg kg-1, p.o. or 0.5 mg kg-1, i.v.) and rotarod impairment (ED50 = 1.1 mg kg-1 p.o. or 1.3 mg kg-1, i.v.) were antagonized by fluparoxan. Fluparoxan, 0.67-6 mg kg-1, p.o., also prevented UK-14304-induced sedation and bradycardia in the dog. 4. In specificity studies fluparoxan had low or no affinity for a wide range of neurotransmitter receptor sites at concentrations up to at least 1 x 10(-5) M. It displayed weak affinity for 5-HT1A (pIC50 = 5.9) and 5-HT1B (pKi = 5.5) binding sites in rat brain. 5. We conclude that fluparoxan is a highly selective and potent alpha 2-adrenoceptor antagonist. The density of rat brain [3H]-dihydroalprenolol binding sites was reduced by 26% when fluparoxan was administered chronically for 6 days at a dose of 12 mg kg- 1 orally twice daily. The down-regulation of beta-adrenoceptors by fluparoxan is consistent with its antidepressant potential. | lld:pubmed |
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| pubmed-article:1677298 | pubmed:language | eng | lld:pubmed |
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| pubmed-article:1677298 | pubmed:citationSubset | IM | lld:pubmed |
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| pubmed-article:1677298 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:1677298 | pubmed:month | Apr | lld:pubmed |
| pubmed-article:1677298 | pubmed:issn | 0007-1188 | lld:pubmed |
| pubmed-article:1677298 | pubmed:author | pubmed-author:TyersM BMB | lld:pubmed |
| pubmed-article:1677298 | pubmed:author | pubmed-author:SkingleMM | lld:pubmed |
| pubmed-article:1677298 | pubmed:author | pubmed-author:HallidayC ACA | lld:pubmed |
| pubmed-article:1677298 | pubmed:author | pubmed-author:KRAFTR ARA | lld:pubmed |
| pubmed-article:1677298 | pubmed:author | pubmed-author:WalshD MDM | lld:pubmed |
| pubmed-article:1677298 | pubmed:author | pubmed-author:WiseHH | lld:pubmed |
| pubmed-article:1677298 | pubmed:issnType | Print | lld:pubmed |
| pubmed-article:1677298 | pubmed:volume | 102 | lld:pubmed |
| pubmed-article:1677298 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:1677298 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:1677298 | pubmed:pagination | 887-95 | lld:pubmed |
| pubmed-article:1677298 | pubmed:dateRevised | 2010-1-13 | lld:pubmed |
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