Antarelix (EP 24332) a novel water soluble LHRH antagonist.
A novel water soluble LHRH antagonist (EP 24332-Antarelix) is described. Its activity in vitro and in vivo in several animal models is given. Antarelix (Ac-D-Nal, D-Cpa, D-Pal, Ser, Tyr, D-Hci, Leu, Lys-(iPr), Pro, D-Ala-NH2) in view of its potency, modest histamine-liberating activity and high water solubility has been selected for further development.
Deghenghi
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R
Europeptides, Argenteuil, France.
Boutignon
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F
Wüthrich
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P
Lenaerts
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V
D000818:Animals; D005260:Female; D007987:Gonadotropin-Releasing Hormone / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000494:pharmacology*; D006636:Histamine Release / Q000187:drug effects; D066298:In Vitro Techniques; D008297:Male; D009842:Oligopeptides / Q000494:pharmacology*; D051381:Rats; D017207:Rats, Sprague-Dawley; D012995:Solubility
D009842:Oligopeptides; D007987:Gonadotropin-Releasing Hormone; C084350:antarelix