MEN15596, a novel nonpeptide tachykinin NK2 receptor antagonist
C Cialdai, M Tramontana, R Patacchini, A Lecci… - European journal of …, 2006 - Elsevier
The pharmacological profile of MEN15596 or (6-methyl-benzo [b] thiophene-2-carboxylic
acid [1-(2-phenyl-1R-{[1-(tetrahydropyran-4-ylmethyl)-piperidin-4-ylmethyl]-carbamoyl}-
ethylcarbamoyl)-cyclopentyl]-amide), a novel potent and selective tachykinin NK2 receptor
antagonist endowed with oral activity, is described. At the human recombinant tachykinin
NK2 receptor, MEN15596 showed subnanomolar affinity (pKi 10.1) and potently
antagonized (pKB 9.1) the neurokinin A-induced intracellular calcium release. MEN15596 …
acid [1-(2-phenyl-1R-{[1-(tetrahydropyran-4-ylmethyl)-piperidin-4-ylmethyl]-carbamoyl}-
ethylcarbamoyl)-cyclopentyl]-amide), a novel potent and selective tachykinin NK2 receptor
antagonist endowed with oral activity, is described. At the human recombinant tachykinin
NK2 receptor, MEN15596 showed subnanomolar affinity (pKi 10.1) and potently
antagonized (pKB 9.1) the neurokinin A-induced intracellular calcium release. MEN15596 …
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