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Monoamine Methyltransferases: Phenylethanolamine N-Methyltransferase and Catechol O-Methyltransferase

Phenylethanolamine N-methyltransferase (PNMT) (EC 2.1.1.28, S-adenosyl-L-methionine: phenylethanolamine N-methyltransferase) is the enzyme that catalyzes the biosynthesis of norepinephrine to epinephrine in the presence of S-adenosyl-L-methionine (SAM) as the me ...

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Phenylalanine Hydroxylase, Tyrosine Hydroxylase, and Tryptophan Hydroxylase

There are four enzymes that utilize reduced pteridine as an electron donor and incorporate one atom of oxygen into their substrates. They are phenylalanine 4-monooxygenase (phenylalanine hydroxylase, PAH, EC 1.14.16.l), tyrosine 3-monooxygenase (tyrosine hydroxylase, TH, EC 1.14 ...

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Serotonin Receptors

Since the middle of the nineteenth century, physiologists have been aware of an endogenous vasoconstrictor substance. Often referred to as “vasotonin,” the factor was present in the serum of clotted blood. (1948) succeeded in isolating the compound and named it “serotonin.” The chemical st ...

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Adrenergic Receptors

Epinephrine (adrenaline, A) and norepinephrine (noradrenaline, NA) are naturally occurring catecholamines that are rmportant in many physiological processes. Adrenaline is found in high concentrations in the adrenal medulla, where it is released into the blood to function as a hor ...

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Receptor Binding in Drug Discovery and Development

The ultimate goal of any drug development program is the application of basic research, both chemical and biological, to the discovery of therapeutic modalities that can prevent, alleviate, or cure the malfunctions in the mammalian homeostatic mechanism that lead to the disease state.

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Phencyclidine (PCP) and Amphetamine Receptor Binding Sites

Both phencyclidine and amphetamine are widely abused in North America (Biel and Bopp, 1978; Petersen and Stillman, 1978). Among their various effects, it is well known that PCP induces sedation, sensory isolation, and hallucinations. Morever, drug abusers have also described strong feel ...

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Binding Sites for Antidepressants

Although antidepressant drugs have been successfully used in the treatment of depression for more than two decades, the mechanism(s) by which these drugs produce their therapeutic effect is not understood. Tricyclic antidepressants have been shown to inhibit the neuronal uptake of no ...

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The Benzodiazepine Receptor

The 1,4-benzodiazepines have become the most frequently prescribed of all psychotropic drugs since the introduction of the first member of this series, chlordiazepoxide, into clinical practice in 1960. The compounds are used as anxiolytics, sedative/hypnotics, anticonvulsan ...

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Purinergic Receptors in the CNS

The phenomenon of “nonadrenergic, noncholinergic” neurotransmission in the mammalian peripheral nervous system probably involves the mediation of the purines, adenosine and its nucleotide, ATP (Burnstock, 1972, 1983).

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Multiple Opioid Receptors in the Central Nervous System

The initial landmarks in opioid receptor research were the demonstration of stereospecificity (Becket and Casey, 1954) and the identification of receptor sites in central nervous system (CNS) membrane preparations (Pert and Snyder, 1973; Simon et al., 1973). Subsequent behavioral s ...

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Receptors for Nonopioid Neuropeptides

Until about 10 yr ago, it was generally assumed that the nervous system, the endocrine system, and the neuroendocrine system are not only anatomically distinct, but that they differ also with respect to the chemical messengers they use. There existed, however, a few exceptions, such as the presence ...

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Central Nervous System Dopamine Receptors

Dopaminergic neuronal systems constitute the principal catecholamine systems of the striatum of the brain (Carlsson, 1959) and the Inner retina (Haggendal and Malmfors, 1965). In both of these regions dopamine (DA) appears to function mainly as an inhibitory neurotransmitter (Conn ...

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GABA Receptor Binding

GABA (γ-aminobutyric acid) receptors are among the most ubiquitous in the brain, having been identified (neurophysiologitally) in all regions and at all levels (e.g., Iversen, 1978). All neuronal cells respond to the iontophoretic application of GABA, usually with a decrease in firing rate ...

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Excitatory Amino Acid Receptors

The dicarboxylic amino acids L-glutamate (Glu) and L-aspartate (Asp) are found throughout the mammalian central nervous system. Although it was initially believed that these amino acids participated solely in the metabolic activities of the brain, evidence that Glu and Asp are excitat ...

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Muscarinic Cholinergic Receptors

In the central nervous system (CNS), modulation of neuronal activity is brought about by the actions of endogenous “neurotransmitters” that specifically interact with receptor proteins located in the neuronal cell membrane. In the cholinergic system, acetylcholine is the primary ...

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General Principles of Receptor Binding

The increasing availability over the past 20 yr of biologically active radiolabeled compounds of high-specific activity has enabled investigators to label and quantitatively assay the receptor (recognition) sites that are thought to mediate the agonistic or antagonistic effe ...

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Laser Capture Microdissection of Hepatic Stages of the Human Parasite Plasmodium falciparum for Molecular Analysis

Despite the sequencing of parasite genomes and development of DNA microarray technology, gene profiling of parasites remains a difficult task. For example, transcriptome analysis cannot currently be applied to the hepatic stages of the malaria parasite Plasmodium falciparum due ...

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Laser Capture Microdissection and PCR for Analysis of Human Papilloma Virus Infection

Human papilloma virus (HPV) infection is considered one of the main factors involved in the pathogenesis of endocervical adenocarcinoma. However, the cellular location of HPV in this type of tumor is controversial. We have developed a method to determine the presence of HPV type 16 in endocerv ...

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Use of Laser Capture Microdissection Together With In Situ Hybridization and Real-Time PCR to Study Distribution of Latent Herpes Simplex Virus Genome

The herpes simplex virus (HSV) frequently establishes a latent state in neurons, which can then be reactivated from the infected neurons. Quantifying the single-cell viral load is essential for understanding latency and reactivation of this virus. In this chapter the methods of laser cap ...

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Genetic Analysis of HIV by In Situ PCR-Directed Laser Capture Microscopy of Infected Cells

Behind the exponential expansion of the acquired immunodeficiency syndrome (AIDS) epidemic, there is a continuous and progressive molecular evolution of human immunodeficiency virus (HIV)-1. In this regard, the molecular analysis of viral strains infecting several anatomic c ...

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