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Concomitant developments in molecular biology and neuroanatomy have permitted the development of techniques to visualize the expression of messenger RNA (mRNA) of interest in its neuroanatomical context and in a relatively quantitative manner. In situ hybridization can be perf ...

Opioid receptors are members of the G-protein coupled receptor (GPCR) family characterized by the presence of seven transmembrane domains. These receptors are classified as mu (μ), delta (δ), and kappa (κ). Activation of these receptors leads to uncoupling of the inhibitory G-proteins (Gi) ...

Opioid receptors are members of the superfamily of the seven transmembrane G protein-coupled receptors (GPCRs). They were initially recognized as three distinct entities in the late 1970s and early 1980s on the basis of pharmacological studies that demonstrated differential dist ...

Both sensory inputs and motor outputs of the brain occur via the spinal cord. Spinalization, via a simple surgical cut, has allowed the elucidation of some of the intrinsic spinal circuitry underlying spinal reflexes. To understand the modulation of spinal processing by local spinal innerv ...

Until recently, opioid receptors were studied only by a pharmacological approach because agonists and antagonists were the only tools available (1). Interpretation of the experimental data was complicated because of the poor selectivity of opioid compounds. The precise contribu ...

One of the main actions of natural and synthetic opioids is powerful analgesia. For many decades, opioid-based drugs, such as morphine, remain to be the most effective analgesics and are widely used in current clinical management of various pain conditions. They are particularly required to c ...

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 ...