G protein-coupled receptors (GPCRs) participate in a variety of physiological functions and are major targets of pharmaceutical drugs. More than 600 GPCRs have been identified in the human genome. Although GPCRs are expressed in multiple tissues and individual tissues express multi ...

The genes for G protein-coupled receptors (GPCRs) including those encoding the classical mu, delta, and kappa opioid receptors (MOR, DOR, and KOR); cannabinoid receptors (CB1); ACTH receptor (melanocortin receptor type 2, MC2R); and serotonin receptors (5HT1B) have been a focus of the studi ...

Alternative pre-mRNA splicing involves editing of a gene to generate a number of different mRNAs and proteins. It provides a mechanism for only 20,000 genes to generate hundreds of thousands of proteins. Like other proteins, it is estimated that 50% of G protein-coupled receptors undergo alte ...

The G protein-coupled receptors (GPCRs) form the largest and most multi-functional protein �superfamilies known. From a drug discovery and pharmaceutical industry perspective, the GPCRs are among the most commercially and economically important groups of proteins yet identi ...

A new approach for characterizing the plasma membrane delivery of G protein-coupled receptors is described in this chapter. This approach uses an existing technology, the regulated secretion/aggregation technology (RPD™), to cause the accumulation of G protein-coupled recepto ...

Drugs targeting the opioid neurotransmission system have been used for centuries recreationally and for medical purposes. In spite of this vast experience and competence in opioid pharmacotherapy, fine details about the cellular and molecular mechanisms underlying opioid rec ...

G protein-coupled receptors (GPCRs) are the major sites of actions for the body’s endogenous hormones and neurotransmitters which make them ideal targets for pharmaceutical development with the goal of either mimicking the normal transmitter response or tempering it. In recent year ...

Technologies developed to interfere with gene transcripts were developed back in the 1980. However, it was not before the last decade that light was shed on the underlying mechanisms of what is now known as RNA interference. From then, RNAi was propelled to the forefront as a revolutionizing appro ...

The phenomenon of antagonist-induced receptor upregulation is common to many G protein-coupled receptors (GPCRs) such as adrenergic, muscarinic, opioid, cannabinoid, histamine, GABA(B), serotonin, and dopamine receptors. This chapter reviews data that support antagonist- ...

The technique of flow cytometry was initially developed to count and size particles. However, it has progressively evolved into a sophisticated analytic tool for rapidly quantifying multiple properties of individual cells or cellular constituents in suspended nonhomogeneous ...

A knowledge of how drugs are metabolized in the body is often of clinical relevance because often an administered drug is not soley responsible for observed pharmacological and toxicological effects. Regrettably, the formation of drug metabolites is often not considered in pharmacol ...

Genetic analysis of viruses capable of producing tumors in mice led to the discovery of cancer-causing genes termed oncogenes. The v-fos oncogene is responsible for the ability of the FBJ-MSV virus to produce bone tumors (Finkel et al., 1966; Curran and Teich, 1982). Shortly after identification ...

Neuroscientists are often faced with the choice of obtaining quantitative data at the expense of morphological information or vice versa. The identification of a pathway in the brain offers a potential anatomical basis for a given physiological function, for example, but does not direct ...

Over the last 30 yr, in vitro assessment of interactions between drugs and drug-metabolizing enzymes has developed from a scientific curiosity to a topic of major clinical and commercial importance. For clinicians, knowledge of this area assists in the ability to predict the likelihood of a dr ...

It is inevitable that most graduate students and researchers in the neurosciences will, from time to time, be faced with a problem related to enzymes. Tasks such as screening novel compounds for enzyme-inhibitor potency, examining the effects of drug administration on enzyme activities, e ...

During development of the nervous system, cell migration, axonal outgrowth, axonal guidance, and selective cell adhesion and recognition are some of the crucial processes required for neural pattern formation. Numerous studies reveal that cells bind selectively to one another and t ...

The ribonuclease protection assay (RPA) is one of the widely used techniques for detection and quantification of mRNA. This assay offers at least 5–10 times the sensitivity of Northern blots and also enables the investigator to use multiple probes in a single assay. Ribonuclease protection i ...

Receptors for peptide YY (PYY) were discovered in the rat small intestine epithelium (1) and were defined as PYY-preferring because they display a slightly higher affinity for PYY than for neuropeptide Y (NPY). In contrast, they have a very low affinity for pancreatic polypeptide (PP). They are ex ...

Radioligand binding is an extremely powerful technique that can provide detailed information about receptor-ligand interactions both in vitro and in vivo. Several types of binding assay can be performed, including studies of the kinetics of association or dissociation of the radio ...

Neuropeptide receptors can be used as molecular targets to deliver chemotherapeutic drugs into cancer cells. The gastrin-releasing peptide (GRP) receptor was used to deliver a camptothecin (CPT)–bombesin (BB) conjugate into the lung cancer cell line NCI-H1299. The CPT–BB conjugate ...