Electrophysiological effects of WAY 100635, a new 5-HT1A receptor antagonist, on dorsal raphe nucleus serotoninergic neurones and CA1 pyramidal cells in vitro.
The novel 5-HT1A receptor antagonist WAY 100635 [(N-(2-(-4(2-metoxyphenyl)-1-piperazinyl)ethyl)-N-(2-pyridinyl)cyc lohexane carboxamide)] has been tested on 5-HT1A receptor-mediated inhibition of firing and intracellularly recorded hyperpolarisation of serotoninergic cells of the dorsal raphe nucleus (DRN) and on hyperpolarisation of hippocampal CA1 pyramidal cells. WAY 100635 selectively blocked 5-HT1A receptor-mediated responses of 5-HT, 8-OH-DPAT, lesopitron and 5-CT. The antagonism of the hyperpolarisation elicited by 5-CT was competitive in the DRN and non competitive in CA1, probably because of the existence of a 5-HT1A receptor reserve in serotoninergic cells of DRN.
Corradetti
R
R
Department of Preclinical and Clinical Pharmacology, University of Florence, Firenze, Italy.
Pugliese
A M
AM
Le Poul
E
E
Laaris
N
N
Hamon
M
M
Lanfumey
L
L
D000818:Animals; D004594:Electrophysiology; D006624:Hippocampus / Q000166:cytology / Q000187:drug effects / Q000502:physiology; D066298:In Vitro Techniques; D008564:Membrane Potentials / Q000187:drug effects; D009474:Neurons / Q000187:drug effects / Q000378:metabolism*; D010879:Piperazines / Q000494:pharmacology*; D017966:Pyramidal Cells / Q000187:drug effects / Q000378:metabolism*; D011725:Pyridines / Q000494:pharmacology*; D011903:Raphe Nuclei / Q000166:cytology* / Q000187:drug effects; D051381:Rats; D012702:Serotonin Antagonists / Q000494:pharmacology*
D010879:Piperazines; D011725:Pyridines; D012702:Serotonin Antagonists; C090413:N-(2-(4-(2-methoxyphenyl)-1-piperazinyl)ethyl)-N-(2-pyridinyl)cyclohexanecarboxamide