Systemic ethanol administration alters protein kinase C (PKC) activity in brain, but the effects of ethanol on the expression and translocation of specific isoforms are unknown. Rats were administered ethanol (2 g/kg i.p.) or saline and PKC levels were measured in the cytosolic and membrane fractions by Western blot analysis. PKC expression was increased in the cytosol and decreased in the memb...

The reinforcing effects of D1-like and D2-like agonists, and their capacity to modify cocaine self-administration, were compared in rats with extensive cocaine self-administration experience. Cocaine (0.01–1.0 mg i.v.) dose-dependently maintained responding under a fixed ratio (FR) 5 schedule of reinforcement, and an inverted U-shaped function characterized the relationship between unit dose an...

In our study, evidence is provided that strychnine, a competitive antagonist at glycine-gated Cl channels, is also a potent competitive antagonist at native a-7-containing, a-bungarotoxin-sensitive nicotinic acetylcholine receptor (nAChRs). To address the effects of strychnine on two types of nicotinic responses, the whole-cell mode of the patch-clamp technique was applied to rat hippocampal ne...

The effects of the phytoestrogens phloretin and phloridzin on Ca handling, cell shortening, the action potential, and Ca and K currents in freshly isolated cardiac myocytes from rat ventricle were examined. Phloretin increased the amplitude and area and decreased the rate of decline of electrically evoked Ca transients in the myocytes. These effects were accompanied by an increase in the Ca loa...

The subjective, psychomotor, and physiological effects of three opioid m-receptor agonists were studied in healthy volunteers using a cumulative-dosing procedure. Sixteen volunteers with no history of drug abuse received i.v. injections of saline (SAL), morphine (MOR), hydromorphone (HM), or meperidine (MEP) in a randomized double-blind crossover design. Subjects received 1 injection/h for the ...

Interferon(IFN) is indicated for the treatment of certain viral infections including hepatitis B and C, and cancers such as melanoma. The short circulating half-life of unmodified IFNmakes frequent dosing (daily or three times weekly) over an extended period (6–12 months or more) necessary. To improve the pharmacokinetics of IFNand decrease dosing frequency, IFNwas fused to human serum albumin ...

In this study, we analyzed the anti-inflammatory effects of -melanocyte stimulating hormone (MSH)11–13 (KPV) in comparison with other MSH peptides in a model of crystal-induced peritonitis. Systemic treatment of mice with KPV, -MSH, the core melanocortin peptide His-Phe-Arg-Trp, and the melanocontin receptor 3/4 agonist Ac-Nle-c[Asp,D-Phe,Lys]NH2 ACTH4-10 (MTII) but not the selective MC1-R agon...

Conflicting results, both decreased and increased, have been reported concerning the function of T-lymphocytes in heroin addicts. We investigated the alterations of T-lymphocyte proliferative responses and immunophenotypic markers on lymphoid cells in heroin addicts and during different periods of heroin withdrawal in addicted subjects. This study has demonstrated a decrease in the response of ...

The present study was undertaken to examine whether the mechanism of action of typical and atypical antipsychotics is related in their ability to regulate key phosphorylating enzyme of adenylyl cyclase-cAMP pathway, i.e., protein kinase A (PKA). For this purpose, regulatory (R) and catalytic (Cat) activities of PKA and expression of various isoforms of regulatory and catalytic subunits were exa...

N,N -Dicyclopentyl-2-methylsulfanyl-5-nitro-pyrimidine-4,6diamine (GS39783) and structurally related compounds are described as novel allosteric enhancers of GABAB receptor function. They potentiate GABA-stimulated guanosine 5 -O-(3-[S]thio)triphosphate ([S]GTP S) binding to membranes from a GABAB(1b/2)-expressing Chinese hamster ovary cell line at low micromolar concentrations, but do not stim...