A receptor is a protein molecule that receives chemical signals from outside a cell, which enables the cell to respond to the signal molecule. Receptors mediate numerous important physiologic effects upon binding extracellular agonists. However, sustained activation of the receptor may lead to pathologic effects. Cells can regulate the number and function of receptors to alter their sensitivity...

243 Introduction 474 Discussion 1165 Non standard abbreviations: AMY, amylin receptor phenotype; CGRP, calcitonin gene-related peptide; CLR, calcitonin receptor-like receptor; CT, calcitonin; CTR, calcitonin receptor; GPCR, G protein-coupled receptor; HA, haemagglutinin epitope tag; hCT, human calcitonin; RAMP, receptor activity modifying protein; rAmy, rat amylin; sCT, salmon calcitonin; TMD, ...

  As I was deeply interested in the effects of drugs on the human body, I chose pharmacology as the subject of special study when I became a 4th year student at Shizuoka College of Pharmacy. I studied abroad as a postdoctoral fellow for two years, from 1978, under the tutelage of Professor Henry I. Yamamura (pharmacology) in the College of Medicine at the University of Arizona, USA. He taught m...

Corticotropin-releasing factor (CRF) receptor antagonists are under preclinical and clinical investigation for stress-related disorders. In this study the impact of receptor-ligand binding kinetics on CRF₁ receptor antagonist pharmacology was investigated by measuring the association rate constant (k₁), dissociation rate constant (k₋₁), and kinetically derived affinity at 37°C. Three aspects of...

Background: This study aimed to investigate the molecular mechanism of Radix Paeoniae Alba (white peony, WP) in treating immune inflammatory diseases rheumatoid arthritis (RA) and tumor necrosis factor-alpha (TNF-?) inhibitors (TNFis) by using network pharmacology docking. Methods: In this study, ingredient WP potential targets RA were obtained from Traditional Chinese Medicine Systematic Pharm...

Despite proven clinical utility, buprenorphine has not been used widely for the treatment of chronic pain. Questions about "ceiling effect" or bell-shaped curve observed for analgesia in preclinical studies and potential withdrawal issues on combining with marketed μ-agonists continue to hinder progress in expanding full potential of buprenorphine in the treatment of cancer and noncancer pain. ...

Melanocortinergic and dopaminergic systems are widely distributed in the CNS and have been established as a crucial regulatory component in diverse physiological functions. The pharmacology of both melanocortinergic and dopaminergic systems including their individual receptors, signaling mechanisms, agonists and antagonists has been extensively studied. Several lines of evidence showed that the...