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  • Affinity
  • Estimates of muscarinic receptor affinity are usually obtained from direct radioligand binding studies performed on subcellular fractions and from the measurement of biological responses of intact tissues. (springer.com)
  • Contrary to expectations, morphine increased muscarinic receptor density in the right atrium and left ventricle by 17 and 34%, respectively, with no change in the apparent affinity of the receptor ( K D ). Morphine also increased the expression of the G protein G i α by 115 and 233%, respectively, in right atrial and left ventricular sarcolemmal membranes. (aspetjournals.org)
  • extracellular
  • induced a concentration-dependent increase in intracellular calcium, via the M3 receptor, which consisted of an initial spike from IP3-sensitive stores, followed by a sustained elevation and oscillations, which were dependent upon extracellular calcium. (washington.edu)
  • Some G q -coupled receptors can be activated through the specific binding of ligands or drugs to the extracellular domains of the protein. (moleculardevices.com)
  • C, the effects of the CamKII inhibitor KN-62 (10 μm) added 10 min before NMDA or the effects of removal of extracellular calcium on the NMDA-mediated desensitization of the M3-muscarinic receptor phosphoinositide response. (nih.gov)
  • transmembrane
  • Liu J, Schoneberg T, van Rhee M and Wess J (1995) Mutational analysis of the relative orientation of transmembrane helices I and VII in G protein‐coupled receptors. (els.net)
  • opioid
  • Thus, the complex interplay that can occur among opposing muscarinic, opioid, and adrenergic systems and their common second messengers provides multiple opportunities for altered autonomic function during long-term opiate administration. (aspetjournals.org)
  • putative
  • In one model, M 1 -muscarinic receptors (M 1 Rs) may inhibit both Ca 2+ (L- and N-) and K + (M-) currents by losing a putative interaction between channels and phosphatidylinositol-4,5-bisphosphate (PIP 2 ). (jneurosci.org)
  • 001), whereas the putative receptor-operated Ca 2+ channel blocker SK&F 96365 converted this vasoconstriction into vasodilation that was not mediated by nitric oxide. (aspetjournals.org)
  • Constitutive
  • This potential model for narcotic tolerance was developed further by Sadee and Wang (1995) , who provided evidence that μ receptors assume constitutive activity during continuous exposure to morphine and no longer require agonist for signal transduction. (aspetjournals.org)
  • compounds
  • The main goal of the phase 1 clinical studies is to show that the drug does not have any cholinergic adverse effects," says Conn. Given the previous history of serious side effects caused by muscarinic compounds, demonstrating that this new compound does not lead to those same adverse effects in humans is key to get industry partners to invest and fund phases 2 and 3 of the clinical study. (aspet.org)
  • cognitive
  • BOSTON--( BUSINESS WIRE )-- Karuna Pharmaceuticals , focused on targeting muscarinic receptors for the treatment of disorders marked by psychosis and cognitive impairment, today announced the completion of a $42 million Series A financing round, including the issuance of $22 million in shares upon conversion of debt into equity. (biospace.com)