Quantum chemical (MNDo)caleulations have beenused toelucidate the molecular properties and structure - activity relationships of dihydropyridine (DHP) type calcium antagonists. There is a good corielation between the net atomic charges on various atoms of the 4 - phenyl ring of dihydropyridines and pharmacological activity. .Also, activity decreases with increasing free rotation of the phen...

in this study, the influence of dopamine receptor agonists and antagonists on antinociception induced by bac10fen has been examined in the formalin test. the gaba-b agonist bac10fen induced antinociception in both phases of the formalin test in mice. the dopamine receptor agonists skf 38393 and quinpirole also induced antinociception in both phases of the test. skf 38393 but not quinpirole pote...

  In this study, we investigated the effect of nicotinic receptor agonists and antagonists on the analgesic response to morphine in the formalin test. In experiments conducted in mice, nicotine produced an early dose-dependent analgesic effect. At a dose of 0.5 mg/kg, mecamylamine, a nicotinic receptor inhibitor, suppressed the analgesic effect induced by 0.1 mg/kg nicotine in both stages of th...

OBJECTIVE Pulmonary tuberculosis (PTB) is a leading cause of morbidity and mortality. Macrophages play an important role in the immunopathogenesis of tuberculosis. Extracellular ATP induces macrophage bactericidal activity through activation of the purinergic P2X7 receptor. This case- control study assesses the association of -762 T/C, 1513A/C and 1729T/A P2X7 polymorphisms in patients with PTB...

The P2X7 subtype holds a special position among P2X receptors because of its ability to act both as a classical, ligand-gated ion channel, and as a permeabilization pore that can induce cell death under prolonged activation by ATP. We have shown previously that, in rat retina, P2X7 receptors are located in the inner nuclear layer and ganglion cell layer (GCL). The present study was aimed at fin...

Objective(s): Oxytocin is involved in modulation of many brain-mediated functions. In the present study, we investigated the central effects of oxytocin and its receptor antagonist, atosiban on inflammatory pain. The contribution of opiate receptors was explored using non-selective and selective antagonists. Materials and Methods: The fourth ventricle of the brain of anesthetized rats was impla...

INTRODUCTION The P2X7 receptor plays a crucial role in bone biology and inflammation. Its main function is to promote necrotic tissue metabolism by ensuring a normal acute-phase inflammatory response. We used a mouse model to describe and compare orthodontic mechanotransduction in wild-type and P2X7 knock-out mice. METHODS By using finite element analysis, mouse orthodontic mechanics were sca...

Pannexin1 (Panx1), an ortholog to invertebrate innexin gap junctions, has recently been proposed to be the pore induced by P2X7 receptor activation. We explored the pharmacological action of compounds known to block gap junctions on Panx1 channels activated by the P2X7R and the mechanisms involved in the interaction between these two proteins. Whole cell recordings revealed distinct P2X7R and P...

BACKGROUND Genetic causes of exaggerated or reduced pain sensitivity in humans are well known. Recently, single nucleotide polymorphisms (SNPs) in the gene P2RX7, coding for the ATP-gated ion channel P2X7, have been described that cause gain-of-function (GOF) and loss-of-function (LOF), respectively of this channel. Importantly, P2RX7 SNPs have been associated with more or less severe pain scor...