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The tetracyclic antidepressants mianserin and mirtazapine are α 2 blockers, although their efficacy as antidepressants may come from their activity at other receptor sites. [citation needed] Mechanistically, α 2 blockers increase adrenergic, dopaminergic and serotonergic neurotransmitters and induce insulin secretion, decreasing blood sugar ...
Adopted orphan receptors in the nuclear receptor group include FXR, liver X receptor (LXR), and peroxisome proliferator-activated receptor (PPAR). Another example of an orphan receptor site is the PCP binding site in the NMDA receptor, [10] a type of ligand-gated ion channel. This site is where the recreational drug PCP works, but no endogenous ...
Alpha blockers, also known as α-blockers or α-adrenoreceptor antagonists, are a class of pharmacological agents that act as antagonists on α-adrenergic receptors (α-adrenoceptors). [ 2 ] Historically, alpha-blockers were used as a tool for pharmacologic research to develop a greater understanding of the autonomic nervous system.
[1] [9] Alpha 2 blockers are rarely utilised in clinical practice because of their substantial off-target binding and associated risks. [1] Non-selective beta blockers. Non-selective beta blockers can cause a range of adverse effects, including bradycardia, hypotension, fatigue, dizziness, nausea, and constipation. [10]
Other side effects may include low blood pressure and urinary problems. [11] It appears to work by activating α 2A-adrenergic receptors in the brain, thereby decreasing sympathetic nervous system activity. [10] Guanfacine was first described by 1974 [12] and was approved for medical use in the United States in 1986. [10]
Yohimbine is an α 2-adrenergic receptor antagonist, and has been used in a variety of research projects. It is a veterinary drug used to reverse sedation in dogs and deer. While yohimbine behaves as an aphrodisiac in some mammals, it does not do so in humans.
Cyproheptadine is a very potent antihistamine or inverse agonist of the H 1 receptor. At higher concentrations, it also has anticholinergic , antiserotonergic , and antidopaminergic activities. Of the serotonin receptors , it is an especially potent antagonist of the 5-HT 2 receptors .
GnRH antagonists competitively and reversibly bind to GnRH receptors in the pituitary gland, blocking the release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) from the anterior pituitary.