title: Inhibition of locus coeruleus neurons by the phencyclidine analog, N-[1-(2-benzo(b)thiophenyl)cyclohexyl]piperidine: evidence for potent indirect adrenoceptor agonist properties.
abstract: The effects of the phencyclidine derivative, N-[1-(2-benzo(b)thiophenyl)cyclohexyl]piperidine (BTCP), on the electrical activity of noradrenaline (NA) neurons of the locus coeruleus (LC) were studied in halothane-anesthetized rats. Systemic administration of BTCP potently inhibited LC neurons (ID50 of 1.1 +/- 0.1 mg/kg i.v.). This effect was mimicked by local microejection of BTCP into the LC. Both the systemic and local effects of BTCP were blocked by alpha 2-adrenoceptor antagonists and prevented by prior depletion of catecholamines with reserpine. These and other data suggest that BTCP behaves as a potent indirect NA agonist (i.e. via NA re-uptake and/or release systems).
authors.affiliation: INSERM U 171, Hopital Sainte Eugénie, CHU Lyon-Sud, Pierre-Bénite, France.
authors.forename: K
authors.initials: K
authors.lastname: Chergui
authors.forename: H
authors.initials: H
authors.lastname: Akaoka
authors.forename: J L
authors.initials: JL
authors.lastname: Brunet
authors.forename: P J
authors.initials: PJ
authors.lastname: Charléty
authors.forename: C F
authors.initials: CF
authors.lastname: Saunier
authors.forename: M
authors.initials: M
authors.lastname: Buda
authors.forename: A
authors.initials: A
authors.lastname: Privat
authors.forename: J
authors.initials: J
authors.lastname: Vignon
authors.forename: J M
authors.initials: JM
authors.lastname: Kamenka
authors.forename: G
authors.initials: G
authors.lastname: Chouvet
mesh_terms: D000818:Animals; D004298:Dopamine / Q000378:metabolism; D008125:Locus Coeruleus / Q000187:drug effects*; D008297:Male; D009638:Norepinephrine / Q000378:metabolism; D010622:Phencyclidine / Q000031:analogs & derivatives* / Q000494:pharmacology; D051381:Rats; D011919:Rats, Inbred Strains; D011941:Receptors, Adrenergic / Q000187:drug effects*
chemical_list: D011941:Receptors, Adrenergic; C056415:1-(1-(2-benzo(b)thienyl)cyclohexyl)piperidine; D010622:Phencyclidine; D004298:Dopamine; D009638:Norepinephrine