| 19831400 |
Butini S, Budriesi R, Hamon M, Morelli E, Gemma S, Brindisi M, Borrelli G, Novellino E, Fiorini I, Ioan P, Chiarini A, Cagnotto A, Mennini T, Fracasso C, Caccia S, Campiani G: Novel, potent, and selective quinoxaline-based 5-HT (3) receptor ligands. 1. J Med Chem. 2009 Nov 12;52(21):6946-50.
Further structure-activity relationships and pharmacological characterization.. We investigated the pharmacological profile of a novel series of quinoxaline-based 5-HT (3) receptor ligands bearing an extra basic moiety on the piperazine N-4. High affinity and selectivity were dependent on the electronic properties of the substituents, and at cardiac level 3a and 3c modulated chronotropy but not inotropy. In von Bezold-Jarisch reflex test 3a-c were partial agonists while 3i was a full agonist. Preliminary pharmacokinetic studies indicated that 3a is a brain penetrating agent. |
82(1,1,1,2) |