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Modulators affect the existing responses within tissues and can allow tissue specific drug targeting. This is unlike orthosteric drugs, which tend to produce a less targeted effect within body on all of the receptors they can bind to. [4] Some modulators have also been shown to lack the desensitizing effect that some agonists have.
Evidence of the allosteric action of escitalopram on the serotonin transported is based on the observation that the R isomer of citalopram can decrease the potency and inhibit the effects of the S isomer, probably through an allosteric interaction between two distinct, non-overlapping binding sites for the two different isomers on the serotonin transporter.
Allosteric regulation of an enzyme. In the fields of biochemistry and pharmacology an allosteric regulator (or allosteric modulator) is a substance that binds to a site on an enzyme or receptor distinct from the active site, resulting in a conformational change that alters the protein's activity, either enhancing or inhibiting its function.
These neurosteroids exert inhibitory actions on neurotransmission.They act as positive allosteric modulators of the GABA A receptor (especially δ subunit-containing isoforms), and possess, in no particular order, antidepressant, anxiolytic, stress-reducing, rewarding, [10] prosocial, [11] antiaggressive, [12] prosexual, [11] sedative, pro-sleep, [13] cognitive and memory-impairing, [citation ...
Ethinylestradiol (EE) is an estrogen medication which is used widely in birth control pills in combination with progestins. [7] [8] In the past, EE was widely used for various indications such as the treatment of menopausal symptoms, gynecological disorders, and certain hormone-sensitive cancers.
Estrogens are typically bound to albumin and/or sex hormone-binding globulin in the circulation. They are metabolized in the liver by hydroxylation (via cytochrome P450 enzymes ), dehydrogenation (via 17β-hydroxysteroid dehydrogenase ), and conjugation (via sulfation and glucuronidation ).
Muscimol (also known as agarin or pantherine) is one of the principal psychoactive constituents of Amanita muscaria and related species of mushroom. Muscimol is a potent and selective orthosteric agonist for the GABA A receptor [3] and displays sedative-hypnotic, depressant and hallucinogenic [citation needed] psychoactivity.
Anastrozole works by reversibly binding to the aromatase enzyme, and through competitive inhibition blocks the conversion of androgens to estrogens in peripheral (extragonadal) tissues. [25] The medication has been found to achieve 96.7% to 97.3% inhibition of aromatase at a dosage of 1 mg/day and 98.1% inhibition of aromatase at a dosage of 10 ...