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Seroquel and the atypical antipsychotic clozapine were compared using a number of biochemical measures in rats which are indicative of potential antipsychotic activity and possible extrapyramidal side effect liability. Both in vitro and in vivo, these compounds are low potency D-2 dopamine (DA) receptor antagonists and are relatively more potent 5-HT2(More)
The effects of D-2 dopamine (DA) receptor blockade were modulated by ICI 169,369, a selective 5-hydroxytryptamine (5-HT)2 receptor antagonist, and by other 5-HT2 antagonists. Specifically, it appears that blockade of 5-HT2 receptors can attenuate the effects of D-2 receptor blockade on rat striatal dopaminergic transmission. Thus, the blockade of D-2(More)
The effects of inhibitors of voltage-sensitive calcium channels (VSCC) on K(+)-evoked [3H]D-aspartate release from rat hippocampal slices and the K(+)-evoked increase in intracellular calcium in neocortical neurons in primary culture were examined. K+ caused a concentration-dependent release of [3H]D-aspartate that was approximately 85% dependent on the(More)
1. The present study examined the interaction of omega-conotoxin GVIA (omega-CT) and aminoglycoside antibiotics on electrically evoked, nerve-mediated contractile responses in the rat vas deferens, guinea-pig ileum and guinea-pig left atria. 2. omega-CT caused a time- and concentration-dependent inhibition of the electrically evoked twitch responses of the(More)
Several protein kinases that copurify with neurofilaments (NF) were identified and each kinase was assessed for its ability to phosphorylate NF proteins. NFs were isolated using an axonal flotation procedure and the kinases were extracted from NFs with 0.8 M KCl. NF kinases were incubated with peptide substrates for selected protein kinases, [32P]ATP and(More)
Pyrazolopyridines (PZP's) in general represent a chemically unique class of non-sedative anxiolytic agents. Tracazolate (ICI 136,753) is a member of pyrazolopyridine series that has shown anxiolytic properties in animal models. Tracazolate demonstrates a wider separation between sedative and therapeutic doses than do benzodiazepines. In addition,(More)
SKF 38393, a selective D-1 dopamine (DA) agonist, enhanced the ability of spiperone, a D-2 antagonist, to increase rat striatal DA metabolite concentrations. Conversely, SKF 38393 reduced the abilities of pergolide and LY 171555, D-2 agonists, to decrease striatal DA metabolite concentrations. These findings are discussed in terms of a possible functional(More)
Haloperidol, at low concentrations that block D-2 dopamine (DA) receptors but not D-1 DA receptors (less than 10 microM), potentiated the enhancement of adenylate cyclase activity produced by the D-1 agonist SKF 38393. Low concentrations of haloperidol (less than or equal to 5 microM) also potentiated the K+-evoked release of [3H]acetylcholine from(More)
Several new non-benzodiazepine anxiolytics are reported. These include tracazolate, zopiclone, CL218,872, CGS9896, buspirone, MK-801 and fenobam. A comparison of anticonflict effects and propensity to cause sedation and potentiate the actions of ethanol is given as well as their effects upon the binding of [3H]flunitrazepam in vitro. Their anxiolytic(More)