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A series of compounds derived from phencyclidine (PCP) was examined in the sigma receptor and PCP receptor binding assays. The derivatives included compounds containing methylene, ethylene or carboxyl ethylene insertion between the cycloalkyl ring and the amine group of PCP. Various phenyl substitutions, cycloalkyl rings and amines of these derivatives were(More)
Rat submandibular cells treated with methylcholanthrene are able to be propagated in continuous culture while retaining beta-adrenergic responsiveness. A specific clone, RSMT-A5, has been isolated and studied in detail. RSMT-A5 cells possess beta-adrenergic receptors (BARS) as judged by [3H]-dihydroalprenolol ([3H]-DHA) binding studies. [3H]-DHA binds to(More)
Rats were trained on a fixed-ratio schedule under which every 30th response produced food reinforcement. Five 3-min periods of fixed-ratio reinforcement were each preceded by a 10-min time-out in which responding had no scheduled consequence. Cumulative dose-effect functions for naltrexone were determined once per week by administering increasing doses(More)
We investigated the effects of phorbol myristate acetate on muscarinic receptor-induced Ca2+ release from intracellular stores and extracellular entry in a human salivary duct cell line, HSG-PA. Phorbol myristate acetate (approximately 10(-7) M) blocked both Ca2+ release and Ca2+ entry induced by the muscarinic agonist carbachol. This blockade was the(More)
Whole cell voltage clamp studies were performed on NCB-20 cells to examine physiological responses to drugs possessing affinities for sigma receptors. Those drugs [haloperidol, alpha-(4-fluoro-phenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazinebutano l (BMY-14802), pentazocine, N-allylnormetazocine (SKF-10047), 3-(3-hydroxyphenyl)-N-(1-propyl)piperidine(More)
1. Membrane preparations obtained from RSMT-A5, an established rat submandibular cell line, possess alpha 1-adrenergic receptors as judged by [3H]prazosin binding studies. Scatchard analysis reveals a single class of binding sites with an equilibrium dissociation constant (Kd) of 0.052 nM and a receptor density (Bmax) of 104 fmol/mg protein. 2. These(More)
Plagiochin E (PLE), a macrocyclic bis(bibenzyl) isolated from the liverwort Marchantia polymorpha, has been reported to have antifungal activity and resistance reversal effects on Candida albicans. In order to understand the underlying mechanisms, we studied the effects of PLE alone and in combination with fluconazole (FLC) on the ergosterol biosynthetic(More)
Homogenates from guinea pig vas deferens were examined for possible existence of sigma receptor and phencyclidine (PCP) receptor using a radioligand binding assay. [3H](+)-SKF-10047 bound saturably in the homogenates to a single population of binding sites with a Kd of 311 and a Bmax of 1090 fmol/mg protein. IC50S of several representative sigma in(More)
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