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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
6
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pubmed:dateCreated |
1999-1-26
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pubmed:abstractText |
A new bivalent ligand of formula 3 which results from the covalent coupling of two sumatriptan molecules with a p-xylyl spacer at the level of the sulfonamide nitrogen has been prepared and evaluated as a 5-HT1B/1D receptors agonist. In vitro experiments at 5-HT1B human cloned receptors (Ki = 0.64 nM; EC50 = 0.58 nM) and at the level of the contraction of the New Zealand white rabbit saphenous vein (pD2 = 6.6) demonstrate the superior potency of dimer 3 as a 5-HT1B receptor agonist when compared to sumatriptan or zolmitriptan. Interestingly enough, the new bivalent agonist 3 was found to induce hypothermia in the guineapig upon oral administration suggesting good oral activity and access to the brain.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Mar
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pubmed:issn |
0960-894X
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:day |
17
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pubmed:volume |
8
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
675-80
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pubmed:dateRevised |
2010-11-18
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pubmed:meshHeading |
pubmed-meshheading:9871581-Animals,
pubmed-meshheading:9871581-Cell Line,
pubmed-meshheading:9871581-Dimerization,
pubmed-meshheading:9871581-Drug Design,
pubmed-meshheading:9871581-Guinea Pigs,
pubmed-meshheading:9871581-Humans,
pubmed-meshheading:9871581-Models, Chemical,
pubmed-meshheading:9871581-Rabbits,
pubmed-meshheading:9871581-Receptor, Serotonin, 5-HT1B,
pubmed-meshheading:9871581-Receptors, Serotonin,
pubmed-meshheading:9871581-Serotonin Receptor Agonists,
pubmed-meshheading:9871581-Sumatriptan
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pubmed:year |
1998
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pubmed:articleTitle |
Dimerization of sumatriptan as an efficient way to design a potent, centrally and orally active 5-HT1B agonist.
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pubmed:affiliation |
Medicinal Chemistry Division, Centre de Recherche Pierre FABRE, Castres, France.
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pubmed:publicationType |
Journal Article
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