Despite its prevalence, nerve injury-related (neuropathic) pain in humans is not well understood and, as such, remains difficult to manage (1–3). A variety of clinical conditions can lead to neuropathic pain, which contributes to our lack of understanding of this phenomenon. Although there ...

Place conditioning is a classical conditioning paradigm in which animals (typically rats or mice) learn to associate the effects of a drug (or other discrete treatment) with a particular environment. Although it is often referred to as the “Conditioned Place Preference (CPP)” paradigm, th ...

The International Association for the Study of Pain (IASP) defines pain as “an unpleasant sensory or emotional experience associated with actual or potential tissue damage, or described in terms of such damage” (1). To successfully manage pain syndromes, the clinical situation, exact di ...

Opiates are powerful analgesics commonly used clinically to relieve pain. However, their repeated administration can lead to the development of drug dependence. During this transition from casual use to abuse, individuals initially respond to opioids as positively rewarding. To ...

Until the middle of the last century, achievement of abstinence was the only available treatment option for opioid dependence. Most often, addicts were simply expected to go “cold turkey,” although abstinence was sometimes accomplished by way of inpatient hospitalization with adjun ...

The aim of this chapter is to give a general overview of techniques employed in the process of ligand-receptor binding. The theoretical aspects of the ligand-receptor interactions and mathematical aspects of binding are not detailed here. These are considered in Chapter 9, and there are also v ...

Imidazoline receptors are divided into two main types, known as I1- and I2-receptors, and whereas I1 receptors appear to play a role in control of blood pressure, I2 receptor mediated functions are still unclear (1).

GABA (γ-aminobutyric acid) is the main inhibitory neurotransmitter in the central nervous system and acts on three pharmacologically distinct receptors: GABAA, GABAB, and GABAC. GABAA receptors are pharmacologically defined on the basis of antagonism by bicuculline and insensi ...

The vast majority of receptors are membrane proteins, so solubilization is an essential prerequisite for purification of these receptors. If the receptor can be solubilized without destroying its characteristic ability to bind specific ligands, it is possible to use the powerful tool ...

Most receptors, apart from those for steroid and thyroid hormones, are transmembrane glycoproteins and are generally expressed by tissues in relatively low quantities. Exceptions include the nicotinic acetylcholine receptor in Torpedo electric organs and the rhodopsin rece ...

An important step in understanding receptor function is determining the tissues and cells in which they are expressed. Classical physiological, biochemical, and membrane binding studies, however, usually provide inadequate spatial resolution to determine the anatomical and ...

Radioligand binding to plasma membranes or complete cell homogenates has been widely used to characterize the binding interactions between a large number of receptors and ligands (see Chapters 1–3). These experiments are generally performed under conditions that optimize the data ...

Knowledge about the neurobiology of the brain is fundamental to our understanding of neuropsychiatric disorders. There are a number of different approaches that have been successfully used to investigate brain function in neuropsychiatric disorders and to inform development of ...

The fundamental purpose of radioligand-binding experiments is to study the binding of drugs to receptors. Thus, a key question to be addressed is whether or not the binding site detected in the experiment really corresponds to the receptor of interest. However, the identification of binding ...

Autoradiographic detection of ligand binding to tissue sections has been used to localize, quantify, and characterize a diverse range of sites. Enzymes have been studied using selective inhibitors, ion channels using naturally occurring toxins, and second messenger systems using ...

A receptor is an allosteric macromolecule (usually associated with a particular cell type) that binds a specific chemical substance (usually secreted by another cell) and in the process undergoes a defined conformational change that triggers a series of biochemical and physiologic ...

Most of the autoradiography performed in human brain involves cutting sections from blocks of tissue or single hemispheres containing relevant areas. The resultant images are restricted to the particular region being studied and do not allow an overview of the plane in which the region is si ...

This chapter describes a functional assay which measures the increase in guanine nucleotide exchange at G-proteins in cell membranes, resulting from agonist binding to G-protein-coupled receptors (GPCRs), by monitoring the binding of GTPγS, a radiolabeled, hydrolysis-resist ...

In situ hybridization histochemistry (ISHH), first described in 1969 by Gall and Pardue and John et al. (1,2) and northern hybridization, first described by Alwine et al. (3), have become very powerful and now quite well established techniques in many research areas, including that of receptor re ...

G protein-coupled receptors (GPCRs) are the number one class of receptor targets for the pharmacotherapy of many pathological and disease states. This chapter presents an overview of the chapter topics presented in this new volume on the genetics of GPCRs.