The β-ARs are members of a large family of neurotransmitter receptors, which interact with GTP binding proteins (G-proteins) to modulate second messenger systems (1,2). The β-ARs mediate the physiological effects of the catecholamines epinephrine and norepinephrine; when ligand- ...
Catecholamines exert their physiological effects via binding to cell-surface receptors known as adrenergic receptors (ARs). Based on the pharmacological and physiological effects of various agonists, the adrenergic receptors have been grouped into a single classificatio ...
Single nucleotide polymorphisms exist at a high frequency in the human genome. Estimates of variability suggest that up to 1 in 1000 bp within coding regions of the genome are polymorphic, and the frequency of polymorphism within noncoding regions is even higher at about 1 in 500. Because of redund ...
Dopamine β-hydroxylase is a copper-containing monooxygenase that catalyzes hydroxylation of a phenylethylamine (mainly dopamine in vivo) at the β-C of the side chain to a phenylethanolamine , using molecular oxygen and ascorbic acid as an electron donor. DBH localizes in noradrener ...
Sulfate conjugation is one of the major catabolic processes involved in the inactivation and elimination of a variety of phenolic drugs and other structurally related exogenous agents. Sulfation of pharmacologically active xenobiotics is assumed to promote their biological in ...
The enzymatic activity that catalyzes the reversible hydrolysis of S-adenosyl-L-homocysteine (AdoHcy) to L-homocysteine (Hey) and adenosine (Ado), or, in reverse, the formation of AdoHcy from Hcy and Ado, is known as AdoHcy hydrolase (AHH) (EC 3.3.1.1). Another name for it, obviously, altho ...
Acetylcholinesterase (acetylcholine acetylhydrolase, AChE: EC 3.1.1.7) has been the focus of much attention since it was first suggested that it plays an important role in the rapid destruction of acetylcholine (ACh) in a living organ (Dale, 1914). In the past decade there has been considerab ...
Monoamine oxidase (MAO; EC 1.4:3.4; amine: oxygen oxidoreductase; deaminating; flavine-containing) is an enzyme that oxidizes a variety of monoamine neurotransmitters and neuromodulators, as well as exogenous bioactive monoamines. It was first characterized by (1928) as monoa ...
Histamine N-methyltransferase (HNMT; EC 2.1.1.8) was discovered a little over 25 yr ago. Since that time, HNMT has been the subject of numerous investigations, and although these studies have provided a fundamental understanding of this enzyme, HNMT has not been the subject of a comprehensive r ...
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 ...
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 ...
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 ...
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 ...
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.
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 ...
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 ...
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 ...
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).
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 ...
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 ...