phenylethylamine/offita

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Pharmacotoxicological screening on new derivatives of beta-phenylethylamine, potential agonists of beta3-adrenergic receptors.

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OBJECTIVE Beta3-adrenergic receptors (beta3-ARs) have been initially characterized in 1989. Afterwards, their tissue distribution was established: white and brown adipose tissue, central nervous system, myocardium (atrial and ventricular), blood vessels, smooth gastrointestinal muscles (stomach,

Structure-activity relationships of constrained phenylethylamine ligands for the serotonin 5-HT2 receptors.

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Serotonergic ligands have proven effective drugs in the treatment of migraine, pain, obesity, and a wide range of psychiatric and neurological disorders. There is a clinical need for more highly 5-HT2 receptor subtype-selective ligands and the most attention has been given to the phenethylamine

Glucose modulation of islet monoamine oxidase activity in lean and obese hyperglycemic mice.

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Islet beta-cell monoamines are known to influence the insulin-releasing mechanisms. These amines are localized in the insulin-secretory granules and are inactivated by the enzyme monoamine oxidase (MAO), a hydrogen peroxide (H2O2)-generating enzyme. The activity of islet MAO may consequently be of

Anti-hypertriglyceridaemic activity of some phenylethylamine anorectic compounds.

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In rats allowed access to food, and in food-deprived rats, fenfluramine (20 and 100 mg kg-1) and amphetamine (10 and 20 mg kg-1) provoked a hypotriglyceridaemic effect. No changes in plasma cholesterol concentration were observed. The time course of the absorption of a lipid load differed according

[Current status of the treatment of type 2 diabetes mellitus. The revival of insulin-resistance drugs].

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The relief of insulin resistance is one of the two therapeutic targets of the treatment of type 2 diabetes. Insulin-sensitizers are therefore complemental with other oral diabetic drugs. The treatment of insulin resistance was for a long time limited to dietary and exercise programmes, a biguanide,

Glucose regulates [3H](+)-amphetamine binding and Na+K+ ATPase activity in the hypothalamus: a proposed mechanism for the glucostatic control of feeding and satiety.

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Binding sites for [3H](+)-amphetamine in the hypothalamus may mediate the anorectic actions of amphetamine and related phenylethylamines. To investigate further the role of these sites in the central control of appetite, the binding of [3H](+)-amphetamine to the hypothalamus and brainstem was

Major depressive episodes and diet pills.

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A variety of medications used to assist with weight loss have been implicated in the precipitation or induction of depressive symptoms and disorders. This is true of a large number of phenylethylamine agents possessing psychostimulant properties, non-phenylethylamine psychostimulants (e.g.,

The acute effects of dexfenfluramine on human and porcine pulmonary vascular tone and resistance.

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OBJECTIVE Treatment with anorectics has become an important aspect of care for the severely obese. One such anorectic, the phenylethylamine dexfenfluramine (dFen), has been associated with the development of pulmonary hypertension. It works by reducing the neuronal uptake of 5-hydroxytryptamine

Discovery of Gut Bacteria Specific to Alzheimer's Associated Diseases is a Clue to Understanding Disease Etiology: Meta-Analysis of Population-Based Data on Human Gut Metagenomics and Metabolomics.

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Alzheimer's disease (AD)-associated sequence (ADAS) of cultured fecal bacteria was discovered in human gut targeted screening. This study provides important information to expand our current understanding of the structure/activity relationship of ADAS and putative inhibitors/activators that are

Identification of a subset of trace amine-associated receptors and ligands as potential modulators of insulin secretion.

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The worldwide prevalence of diabetes has reached 8.5% among adults, and this is characterised by elevated glucose concentrations and failing insulin secretion. Furthermore, most people with type 2 diabetes are either obese or overweight, with the associated dyslipidaemia contributing to the

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