by G Serafini 2024 Cited by 14Aripiprazole is an interesting psychoactive compound acting as a dopamine D2 partial agonist, serotonin 5-HT(1A) partial agonist and serotonin 5-HT(2A)
A number of new medications include the prokinetic selective 5-HT 4 receptor agonist (prucalopride), the intestinal chloride channel activator (lubiprostone) and the guanylate cyclase-C agonist (linaclotide). 5-HT 4 receptor has been highlighted as an attractive drug target for the treatment of GI motility disorders. 5-HT 4 receptor agonists
Vortioxetine is a recently introduced multimodal antidepressant that inhibits the serotonin transporter (SERT) and antagonizes several serotonin receptors (5-HT 3, 5-HT 7, and 5-HT 1D). 12 It also acts as a partial agonist on 5-HT 1B and as a full agonist on 5-HT 1A receptors. 13 Vortioxetine binds with high affinity to the SERT (Ki = 1.6 nM).
In vitro, aripiprazole is a neutral antagonist or very weak partial agonist at 5-HT 2A and 5-HT 7, and is an inverse agonist at 5-HT 2B receptors. 62 According to the prescribing information for Abilify, aripiprazole is an 1 antagonist.
Vortioxetine is a multimodal antidepressant with two different types of pharmacologic targets: serotonin receptors and transporters. In vitro, vortioxetine acts as a 5-HT 1A receptor agonist, 5-HT 3, 5-HT 7, and 5-HT 1D receptor antagonist, 5-HT 1B receptor partial agonist, and inhibitor of the 5-HT transporter (SERT) .
Serotonin 5-HT-receptor agonists work as abortive agents. Abortive agents constrict the blood vessels and prevent inflammation by stimulating 5-HT-receptors in the brain. 5-HT-receptor agonists bind to the 5-HT-receptors in the brain and inhibit the release of serotonin to reduce pain, nausea, and other symptoms of migraine.
Previous nonselective 5-hydroxytryptamine receptor 4 (5-HT(4)) agonists have been associated with significant interactions with other receptors (5-HT(1B), 5-HT(1D), and 5-HT(2B) for tegaserod; hERG for cisapride), leading to adverse cardiovascular events resulting in withdrawal of these drugs from the market.
This semisynthetic ergot derivative exhibits potent agonist activity on dopamine D 2 - and D 3-receptors. It also exhibits: agonist activity (in order of decreasing binding affinities) on 5-hydroxytryptamine (5-HT) 2B, 5-HT 2A, 5-HT 1D, dopamine D 4, 5-HT 1A, dopamine D 1, 5-HT 1B and 5-HT 2C receptors and antagonist activity on 2B, 2A
Triptans. As a class of drugs, the triptans, were specifically developed for the acute treatment of migraine. Triptans are 5-HT receptor agonists (selective for 5-HT 1 receptors), and are analogues of the neurotransmitter serotonin (5-HT).
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