G-protein-coupled receptors.
نویسندگان
چکیده
G-Protein-coupled receptors mediate many of the hypnotic and analgesic actions of the drugs employed in anesthesia. Notably, opioid agonists represent the most successful and efficacious class of analgesic agents employed over the last century. Also, major clinical advances have been made by the study of alpha(2) adrenoceptor agonists, which possess both hypnotic and analgesic qualities that are being increasingly exploited in both anesthetic and critical care settings. Furthermore orexin, gamma-aminobutyric acid (GABA) (B), and muscarinic cholinergic receptors have been identified as potential anesthetic targets; clinical exploitation of ligands at these receptors may lead to important advances in anesthetic pharmacology. In this review we discuss the relevant molecular and neural network pharmacology of anesthetic agents acting at G-protein-coupled receptors.
منابع مشابه
G-protein Coupled Receptor Dimerization
A growing body of evidence suggests that GPCRs exist and function as dimers or higher oligomers. The evidence for GPCR dimerization comes from biochemical, biophysical and functional studies. In addition, researchers have shown the occurrence of heterodimerization between different members of the GPCR family. Two receptors can interact with each other to make a dimer through their extracellular...
متن کاملHigh glucose condition down-regulates the inhibitory G-protein subunit, Gαi, in pheochromocytoma PC12 cells
Introduction: G-proteins have an important role in the cell signaling of numerous receptors. The situation of G-proteins in health and disease and their critical role in the development of diabetic side effects is an interested scientific field. Here, the changes in the expression of G-protein subunits (Gαi, Gαs and Gβ) were evaluated in hyperglycemic situation of PC12 cells as...
متن کاملA study on the correlation of G-protein-coupled receptor types with amino acid composition.
G-protein-coupled receptors have become a target in utilizing bioinformatics and genomics technology to facilitate drug discovery for psychiatric diseases. In this study the covariant-discriminant algorithm [Chou and Elrod (1999) Protein Eng., 12, 107-118] has been used to analyze the correlation between the types of G-protein-coupled receptors and the amino acid composition. It has been found ...
متن کاملMetabotropic glutamate receptors and their ligands applications in neurological and psychiatric disorders
Metabotropic glutamate receptors (mGluRs) consist of a large family of G-protein coupled receptors that are critical for regulating normal neuronal function in the central nervous system. The wide distribution and diverse physiological roles of various mGluR subtypes make them highly attractive targets for the treatment of a number of neurological and psychiatric disorders. The discovery of ...
متن کاملA new family of regulators of G-protein-coupled receptors?
Organisms as diverse as fungi and humans use G-protein-coupled receptors to control signal transduction pathways responsive to various hormones, neuroregulatory molecules and other sensory stimuli. Continual stimulation of these receptors often leads to their desensitization, which is mediated in part by the consecutive actions of two families of proteins--the G-protein-coupled receptor kinases...
متن کاملStrategies to identify ligands for orphan G-protein-coupled receptors.
G-protein-coupled receptors are the most tractable class of protein targets for small molecule drug design. Sequencing of the human genome allied to bio-informatic analysis has identified a large number of putative receptors for which the natural ligands remain undefined. A range of currently employed and developing strategies to identify ligands that interact with these orphan receptors and to...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید
ثبت ناماگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید
ورودعنوان ژورنال:
- Handbook of experimental pharmacology
دوره 182 شماره
صفحات -
تاریخ انتشار 2008