A solid-phase extraction absorbent material based on poly (N-isopropylacrylamide-comethacrylic acidco-ethylene glycol dimethacrylate) [poly (NIPAAm-MAA-co-EDMA)] monolithic column was developed for the simultaneous determination of nitrendipine and nisoldipine from human urine. The morphology of monolithic column and pressure drop across the columns were characterized. The results showed excell...

The subtypes of postjunctional alpha-adrenoceptors activated by neuronally released and exogenous norepinephrine and the source of calcium used for vasoconstrictor responses were investigated in the feline mesenteric vascular bed. Under constant flow conditions, intra-arterial injections of phenylephrine and UK14304, alpha 1- and alpha 2-adrenoceptor agonists, increased mesenteric arterial perf...

BACKGROUND The authors previously reported that the isoflurane-caused reduction of the carbachol-evoked cytoplasmic Ca transient increase ([Ca]cyt) was eliminated by K or caffeine-pretreatment. In this study the authors investigated whether the isoflurane-sensitive component of the carbachol-evoked [Ca]cyt transient involved Ca influx through the plasma membrane. METHODS Perfused attached hum...

Increased ligand binding to dihydropyridine receptors in the central nervous system after chronic ethanol consumption is thought to contribute to the withdrawal syndrome. Previous studies demonstrated such changes when the binding was measured in vitro, which, as the receptors are voltage-sensitive, may not accurately reflect the binding in vivo. In the present study, dihydropyridine binding wa...

The involvement of different types of voltage-dependent calcium channels in nerve-evoked release of neurotransmitter was studied during recovery from neuromuscular paralysis produced by botulinum toxin type A intoxication. For this purpose, a single subcutaneous injection of botulinum toxin (1 IU; dl50) on to the surface of the mouse levator auris longus muscle was performed. The muscles were r...

Background Following peripheral nerve chronic constriction injury, the accumulation of the α2δ-1 auxiliary subunit of voltage-gated Ca2+ channels in primary afferent terminals contributes to the onset of neuropathic pain. Overexpression of α2δ-1 in Xenopus oocytes increases the opening properties of Cav1.2 L-type channels and allows Ca2+ influx at physiological membrane potentials. We therefore...

A new calcium blocker, designated leualacin, has been isolated from Hapsidospora irregularis. The compound inhibits the binding of 3H-nitrendipine, a well known synthetic calcium blocker, to cardiac Ca channel in a competitive manner, although its structure is completely different from dihydropyridines.

The interaction of 1,4-dihydropyridine derivatives with their receptors on voltage-dependent calcium channels in cardiac membranes was studied to determine if there are basic differences in the binding properties of ligands that cause inhibition or activation of calcium channels. The binding characteristics of 6 pure stereoisomers, (-) and (+)202-791, (-) and (+)Bay k 8644, (-) and (+)PN 200-11...

Detailed kinetic and equilibrium studies of the binding of two radiolabeled 1,4-dihydropyridine calcium antagonists to putative calcium channels in rat brain membranes were performed. (+/-)-[3H]Nitrendipine, a racemic ligand, and (+)-[3H]isopropyl 4-(2,1,3-benzoxadiazol-4-yl)-1, 4-dihydro-2,6-dimethyl-5-methoxycarbonylpyridine-3-carboxylate (PN200-110), a pure isomer, were used and their bindin...