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The novel kappa agonist U50-488H in vitro produced a concentration-dependent decrease (0.25-25 microM) in [3H]nimodipine binding in neuronal P2 fractions [corrected] from rat brain cortex. Kinetic analysis indicates the decrease in binding results from a reduced Bmax with no change in affinity (Kd). The kappa antagonist, MR2266, blocked the decrease in(More)
The present studies examined the relationship between protein kinase C (PKC) and L-type voltage-dependent calcium channels in modulating the release of neurotransmitter from K(+)-depolarized rat spinal cord synaptosomes. Activators of PKC, such as phorbol 12-myristate 13-acetate (PMA), mezerein and oleoyl acetylglycerol produced a concentration-dependent(More)
The study aims on by contact analysis of a cylindrical wheel and a rail structure of I–section with considering the material properties of an elastic–plastic adhesive frictional contact. Different materials are considered for the analysis based on Young's modulus and yield strength ratio (E/Y). The contact analysis of this model has been carried out using(More)
Fluoxetine, a selective 5-HT uptake inhibitor, inhibited 15 mM K(+)-induced [3H]5-HT release from rat spinal cord and cortical synaptosomes at concentrations greater than 0.5 uM. This effect reflected a property shared by another selective 5-HT uptake inhibitor paroxetine but not by less selective uptake inhibitors such as amitriptyline, desipramine,(More)
The release of [3H]monoamines from preloaded synaptosomes from spinal cord is K(+)-dependent and can be modulated by L-type Ca2+ channel agonists such as the 1,4-dihydropyridine (1,4-DHP), Bay K 8644. Whereas the basal release of [3H]monoamines was not altered by Bay K 8644, K(+)-stimulated release of [3H]norepinephrine was enhanced 35% and [3H]serotonin(More)
The in vivo effect of the mu agonist morphine and antagonist naloxone on [3H]nimodipine receptor binding in rat brain regions has been investigated. Morphine administration (15 mg/s.c.) for thirty minutes produced a 19% decrease in [3H]nimodipine receptor binding (Bmax 158.2 fmol to 128.9 fmol) in cortex and 29% decrease in cerebellum (65.3 fmol to 46.0(More)
The present study reports the existence of high-affinity [3H]nitrendipine ([3H]NIT) binding sites in rat spinal cord. Characterization studies revealed [3H]NIT binding to synaptosomes to be specific, rapid and saturable, occurring at a single population of sites. The Bmax was 51 fmol/mg of protein and Kd 0.22 nM with a Hill slope of 0.96. Studies with(More)
The effects of a kappa opiate agonist have been evaluated on [3H]nimodipine binding to dihydropyridine receptors for 'L'-type Ca2+ channels in rat brain regions. Administration of U50-488H (trans-(+/-)-3,4-dichloro-N-methyl-N-[2-(1,-pyrolidinyl-cyclohexyl benzeneacetamide) produced a 28% decrease in Bmax in cortex and a 23% decrease in cerebellum. No(More)