190953-69-6Relevant academic research and scientific papers
BICYCLIC HETEROARYL-ALKYLENE-(HOMO)PIPERAZINONES AND THIONE ANALOGUES THEREOF, THEIR PREPARATION, AND THEIR USE OF AS SELECTIVE AGONISTS OF 5HT1-LIKE RECEPTORS
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, (2008/06/13)
A class of piperazinones, homopiperazinones and thione analogues thereof, substituted at the 1-position by an optionally substituted alkenyl, alkynyl, aryl-alkyl or heteroaryl-alkyl moiety, and linked at the 4-position via an alkylene spacer to a fused bicyclic heteroaromatic moiety, typically indolyl, are selective agonists of 5-HT. sub.1-like receptors, being potent agonists of the human 5-HT 1Dα receptor subtype while possessing at least a 10-fold selective affinity for the 5-HT 1Dα receptor subtype relative to the 5-HT 1D. beta. subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT 1D receptors is indicated, while eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT 1D receptor agonists.
3-(piperazinylpropyl)indoles: Selective, orally bioavailable h5-HT(1D) receptor agonists as potential antimigraine agents
Chambers, Mark S.,Street, Leslie J.,Goodacre, Simon,Hobbs, Sarah C.,Hunt, Peter,Jelley, Richard A.,Matassa, Victor G.,Reeve, Austin J.,Sternfeld, Francine,Beer, Margaret S.,Stanton, Josephine A.,Rathbone, Denise,Watt, Alan P.,MacLeod, Angus M.
, p. 691 - 705 (2007/10/03)
Clinically effective antimigraine drugs such as Sumatriptan have similar affinity at h5-HT(1D) and h5-HT(1B) receptors. In the search for a h5- HT(1D)-selective agonist as an antimigraine agent, a novel series of 3- (propylpiperazinyl)indoles have been sy
