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Discovery of a new series of centrally active tricyclic isoxazoles combining serotonin (5-HT) reuptake inhibition with alpha2-adrenoceptor blocking activity.
Andrés JI, Alcázar J, Alonso JM, Alvarez RM, Bakker MH, Biesmans I, Cid JM, De Lucas AI, Fernández J, Font LM, Hens KA, Iturrino L, Lenaerts I, Martínez S, Megens AA, Pastor J, Vermote PC, Steckler T. Andrés JI, et al. Among authors: megens aa. J Med Chem. 2005 Mar 24;48(6):2054-71. doi: 10.1021/jm049619s. J Med Chem. 2005. PMID: 15771448
Pharmacological profile of (2R-trans)-4-[1-[3,5-bis(trifluoromethyl)benzoyl]-2-(phenylmethyl)-4-piperidinyl]-N-(2,6-dimethylphenyl)-1-acetamide (S)-Hydroxybutanedioate (R116301), an orally and centrally active neurokinin-1 receptor antagonist.
Megens AA, Ashton D, Vermeire JC, Vermote PC, Hens KA, Hillen LC, Fransen JF, Mahieu M, Heylen L, Leysen JE, Jurzak MR, Janssens F. Megens AA, et al. J Pharmacol Exp Ther. 2002 Aug;302(2):696-709. doi: 10.1124/jpet.102.034348. J Pharmacol Exp Ther. 2002. PMID: 12130734
71 results