The following remarks are intended to serve as an introduction to this particular volume as well as to the whole series of volumes of which this is the first. The intent of the series is to provide an authentic and relatively complete statement about the status of our understanding of the receptors. The models we had in mind while developing this series are The Enzymes, The Proteins, and comparable groups of books. The receptors have received a degree of importance and richness of understanding that makes them deserving of comprehensive and complete coverage. The study of these molecules,...
The following remarks are intended to serve as an introduction to this particular volume as well as to the whole series of volumes of which this is th...
Research on muscarinic receptors is advancing at an extraordinary rate. Ten years ago, the existence of muscarinic receptor sub types was a logical assumption with only scattered experimen tal support. The discovery that pirenzepine recognized apparent heterogeneity in muscarinic binding sites infused new life into the problem of subclassifying muscarinic receptors. Simultaneous advances in molecular biology created a frenzy to clone cell sur face receptors. The muscarinic receptor succumbed surprisingly quickly, revealing its structure and that of at least four closely related gene products...
Research on muscarinic receptors is advancing at an extraordinary rate. Ten years ago, the existence of muscarinic receptor sub types was a logical as...
Serotonin (5-HT) was isolated and chemically characterized nearly four decades ago, and is now generally accepted to function as a neurotransmitter and neuromodulatory agent. Early research focused on the measurement of concentrations, synthesis, and metabolism of 5-HT, and only recently has the focus shifted to characterization of 5-HT receptors. Gaddum and Picarelli first sug gested in 1957 that the effect of 5-HT in the guinea pig ileum is mediated by two pharmacologically distinguishable receptors; however, the possibility of dual5-HT receptors was not explored systematically or...
Serotonin (5-HT) was isolated and chemically characterized nearly four decades ago, and is now generally accepted to function as a neurotransmitter an...
GABA is the principal inhibitory neurotransmitter in the CNS and acts via GABAA and GABAB receptors. Recently, a novel form of GABAA receptor-mediated inhibition, termed "tonic" inhibition, has been described. Whereas synaptic GABAA receptors underlie classical "phasic" GABAA receptor-mediated inhibition (inhibitory postsynaptic currents), tonic GABAA receptor-mediated inhibition results from the activation of extrasynaptic receptors by low concentrations of ambient GABA. Extrasynaptic GABAA receptors are composed of receptor subunits that convey biophysical properties ideally suited to the...
GABA is the principal inhibitory neurotransmitter in the CNS and acts via GABAA and GABAB receptors. Recently, a novel form of GABAA receptor-mediated...
In Functional Selectivity of G Protein-Coupled Receptors, experts review the work that demonstrated the existence of functional selectivity, placed it within a theoretical framework, and provided a mechanistic basis for the phenomenon.
In Functional Selectivity of G Protein-Coupled Receptors, experts review the work that demonstrated the existence of functional selectivity, placed it...
As research has progressed, the cannabinoid CB 1 and CB 2 receptors have expanded significantly in importance within the neuroscience mainstream. In The Cannabinoid Receptors, leading experts introduce newcomers to the cannabinoid field with chapters covering cannabinoid ligand synthesis and structure activity relationships, the molecular pharmacology of the cannabinoid receptors and the endocannabinoid system, and ultimately, the whole animal pharmacology and therapeutic applications for cannabinoid drugs. Adding to those key topics, the book also examines...
As research has progressed, the cannabinoid CB 1 and CB 2 receptors have expanded significantly in importance within the neur...
Functional selectivity refers to the ability of different ligands acting at one receptor subtype to activate multiple signaling pathways in unique combinations; that is, one drug can be an agonist at pathway A and an antagonist or partial agonist at pathway B, and another drug can have the reverse profile. Functional selectivity has profound implications for drug development, for chemical biology, and for the design of experiments to characterize receptor function. In Functional Selectivity of G Protein-Coupled Receptors expert neuroscientists and pharmacologists review the work that...
Functional selectivity refers to the ability of different ligands acting at one receptor subtype to activate multiple signaling pathways in unique com...
Much of our knowledge of the cerebral circulation has been derived from studies of species other than human. There is increas ing recognition of species differences and concern that studies in animals may be misleading if unquestioningly applied to the human. A dramatic example of this occurred in the early his tory of the study of the circulation of the brain. Galen of Pergamo (131-201 AD) described a rete mirabile or "marvelous network" of blood vessels at the base of the human skull that he must have derived from observations of certain animals. This vascular structure was supplied by the...
Much of our knowledge of the cerebral circulation has been derived from studies of species other than human. There is increas ing recognition of speci...
