Abstract
In this study, a series of 1-phenoxyalkyl-4-[(N,N-disubstitutedamino)alkyl]piperazine derivatives has been prepared and in vitro tested as H3-receptor antagonists (electrically evoked contraction of the guinea pig jejunum). All compounds investigated show moderate in vitro affinities. The most potent antagonists in this series are the compounds 9b, 1b, 1f, and 1l, which exhibit, independently of the substituent at the end of -N- moiety, almost the same level of affinity (pA2 = 7.18, pA2 = 7.27, pA2 = 7.13, pA2 = 7.12, respectively). The histaminergic H1 antagonism of the aforementioned four products was established on the isolated guinea pig ileum by conventional methods; the pA2 values were compared with the potency of pyrilamine. None of them shows any H1-antagonistic activity (pA2 < 4; for pyrilamine pA2 = 9.35).
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
