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Serotonin receptors and valvular heart disease
Published in Demetrius Pertsemlidis, William B. Inabnet III, Michel Gagner, Endocrine Surgery, 2017
Javier G. Castillo, David H. Adams
Among the seven families of 5-HT receptors, the 5-HT2 family has been traditionally linked to secondary cardiovascular disease, especially 5-HT2A and 5-HT2B [19]. This family consists of three different GPCRs (5-HT2A, 5-HT2B, and 5-HT2C) that induce a sudden increase in the intracellular concentration of IP3, thus generating the production of DAG and calcium. Parallel to these reactions, 5-HT2 receptors also generate secondary organ-specific responses, among which the brain is the most prevalent target [20]. In the brain, 5-HT2C receptors are uniformly distributed in all brain areas and represent an important target for psychoactive agents (i.e., atypical antipsychotics and anorectics), whereas the presence of 5-HT2A receptors is only important in cortical regions and the concentration of 5-HT2B receptors is very low (minor involvement) [21]. However, a very characteristic trait of 5-HT2 receptors is the lack of selectivity. This is due to an approximate 50% homology among receptors, and as a consequence, drugs intended to target 5-HT2A or 5-HT2C receptors located in the brain may interact with peripheral 5-HT2B receptors and vice versa [22].
Neuroendocrine disease
Published in Philip E. Harris, Pierre-Marc G. Bouloux, Endocrinology in Clinical Practice, 2014
Treatment of patients with Parkinson’s disease with high doses of cabergoline (≥3 mg daily) has been shown to be associated with an increased risk of valvular fibrosis and moderate-to-severe valvular regurgitation. This response is due to agonist activity at the 5-HT2b receptor. These doses are much higher than those routinely used in the management of prolactinomas or acromegaly. Current published data are largely from cross-sectional studies.13,17 Presently, the consensus is that there is no increased risk of valvulopathy with the typical doses of 1–2 mg/week, but definitive risk assessment requires the results of long-term prospective follow-up with large cohorts of patients.
Movement Disorders
Published in John W. Scadding, Nicholas A. Losseff, Clinical Neurology, 2011
Ergoline derivatives have long been recognized to rarely cause vasospasm, erythromelalgia, pleuropulmonary or retroperitoneal fibrosis. However, since 2004, there has been increasing concern about their capacity to cause cardiac valve fibrosis (often right-sided), so they are now second-line agonists, and rarely if ever given. This adverse effect is thought to be mediated through 5HT2B receptor agonism. All dopaminergic medications, including levodopa, can also cause drowsiness, so that patients should be instructed not to drive if they are experiencing sleepiness. Apomorphine causes fewer neuropsychiatric side effects than oral agonists, but may cause painful inflamed swellings at injection sites, which sometimes preclude further injections.
Healthcare resource utilization, costs and treatment patterns in patients with bipolar disorder treated with lurasidone or cariprazine
Published in Journal of Medical Economics, 2021
Huan Huang, Luke Schmerold, Carole Dembek, Qi Fan, Christopher Dieyi, G. Rhys Williams, Antony Loebel
Four atypical antipsychotics have been approved by the US Food and Drug Administration (FDA) for the treatment of adult patients with bipolar depression: lurasidone, cariprazine, quetiapine, and olanzapine/fluoxetine combination2. Among these four, lurasidone is the only atypical antipsychotic approved as both monotherapy and adjunctive therapy with lithium or valproate for the treatment of major depressive episodes associated with bipolar I disorder in adults (both approved in June 2013)11. Cariprazine was initially approved for the treatment of manic or mixed episodes (approved in September 2015) and recently approved for the treatment of depressive episodes (approved in May 2019) associated with bipolar I disorder in adults12. Lurasidone demonstrates high binding affinity for dopamine D2 and serotonin 5-HT2A and 5-HT7 receptors as an antagonist and moderate binding affinity for serotonin 5-HT1A receptors as a partial agonist13. Cariprazine shows high binding affinity for dopamine D3, dopamine D2, and serotonin 5-HT2B receptors as a partial agonist and moderate affinity for serotonin 5-HT1A (partial agonist) and 5-HT2A (antagonist) receptors14. Lurasidone’s antidepressant effects are believed to be mediated, in part, by 5-HT7 activity13 whereas potent binding to D3 is thought to be associated with cariprazine’s effect on mood14.
A positive association between a polymorphism in the HTR2B gene and cocaine-crack in a French Afro-Caribbean population
Published in The World Journal of Biological Psychiatry, 2020
Jerome Lacoste, Sandrine Lamy, Nicolas Ramoz, Nicolas Ballon, Louis Jehel, Luc Maroteaux, Florence Thibaut
Furthermore, a recent genome-wide association study of physical aggression occurring under the influence of cannabis in African Americans implicated the HTR2B-rs17440378 TT genotype, which was not previously considered a key cannabis target (Montalvo-Ortiz et al. 2018). Treating the 5-HT2B receptor knockout mice with THC resulted in increased aggressive behaviour in the resident-intruder paradigm, while the opposite effect was observed in wild-type mice. Thus, HTR2B variation in expression moderates the effects of cannabis on aggression and social interactions in mice (Montalvo-Ortiz et al. 2018). Interestingly, null expression or blockade of 5-HT2B receptors diminishes the reinforcing effects of psychoactive drugs by modulating serotonin and dopamine signalling. The direct effects of HTR2B-rs17440378 (an intronic polymorphism) on protein function, including regulation, are unknown. In general, crack users have a higher level of impulsivity compared to cannabis users, which means that it may be more difficult to disentangle the respective roles of impulsivity and crack use disorders effects in the association with SNPs, especially in a small sample.
An up-to-date evaluation of lorcaserin hydrochloride for the treatment of obesity
Published in Expert Opinion on Pharmacotherapy, 2020
Beverly G. Tchang, Brittany Abel, Christina Zecca, Katherine H. Saunders, Alpana P. Shukla
Although not known to specifically regulate appetite, the 5HT2B receptor has been an important player in the history of serotonin receptor agonists. The 5HT2B receptor is expressed on cardiac valves; prior AOMs fenfluramine and dexfenfluramine, which were nonselective serotonin receptor agonists, were found to cause valvulopathies due to agonistic effects at the 5HT2B receptor [25,26].