We investigated the pharmacological profile of a novel series of quinoxaline-based 5-HT(3) receptor ligands bearing an extra basic moiety oil 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 it brain penetrating agent.
Novel, Potent, and Selective Quinoxaline-Based 5-HT3 Receptor Ligands. 1: Further Structure-Activity Relationships and Pharmacological Characterization / 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.. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0022-2623. - STAMPA. - 52:21(2009), pp. 6946-6950. [10.1021/jm901126m]
Novel, Potent, and Selective Quinoxaline-Based 5-HT3 Receptor Ligands. 1: Further Structure-Activity Relationships and Pharmacological Characterization
MORELLI, ELENA;Brindisi M.;NOVELLINO, ETTORE;
2009
Abstract
We investigated the pharmacological profile of a novel series of quinoxaline-based 5-HT(3) receptor ligands bearing an extra basic moiety oil 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 it brain penetrating agent.| File | Dimensione | Formato | |
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