AntagonistSelectivityBlockade of the serotonin 5-HT2AG protein-coupled receptor (5-HT2AR) is a fundamental pharmacological characteristic of numerous antipsychotic medications, which are FDA-approved to treat schizophrenia, bipolar disorder, and as adjunctive therapies in major depressive disorder. ...
to inhibit 5-HT2Amediated adhesion, and treatment with serotonin, DOI or dopamine increased adhesion via activation of the 5-HT2Athough they were unable to overcome antagonist-mediated loss of adhesion (Supplementary Fig.S5A). Atypical antipsychotics such as risperidone27have higher affinities for th...
the addition of drugs with prominent 5-HT2 receptor antagonist properties (risperidone, olanzapine, mirtazapine, and mianserin) to selective serotonin reuptake inhibitors (SSRIs) has been shown to enhance therapeutic responses in patients with major depression and treatment-refractory obsessive–compulsive...
or the 5-HT2A inverse agonist/antagonist pimavanserin, administered alone or in combination, on cocaine self-administration by rhesus monkeys in the context of a cocaine-vs-food choice procedure that has been used previously to examine effects of other candidate medications (Banks et al, 2015). ...
Narendran R, Mason NS, Laymon CM, Lopresti BJ, Velasquez ND, May MA et al (2010) A comparative evaluation of the dopamine D2/3 agonist radiotracer [11C](−)-N-propyl-norapomorphine and antagonist [11C]raclopride to measure amphetamine-induced dopamine release in the human striatum. J ...
Systemic administration of DOI, a nonsubtype-selective 5- HT2A/B/C agonist, increased cortical DA efflux which could be blocked by the 5-HT2A-preferring antagonist M100907 (Ki ¼ 1.92 for r5-HT2A: see on-line database: http://kidb. case.edu/pdsp.php; Gobert and Millan, 1999). ...
(2003) Acute administration of the selective D3 receptor antagonist SB-277011-A blocks the acquisition and expression of the conditioned place preference response to heroin in male rats. Synapse, 48, 154-156); anxiety, and depression (Reavill-C et al. (2000) Pharmacological actions of a novel...
The forced swim test is a common animal model for testing the effectiveness of antidepressant medications. This test shows that effective antidepressant treatments decrease overall immobility time. Using the forced swim test, a 5-HT2A antagonist, MDL 100907, was used to determine if blocking this ...
5-HT2C antagonistObesityPyrimidoazepineSerotonin receptor ligandsObesity is one of the most serious public health problems worldwide in the 21st century. Current therapeutic treatment for obesity is mostly focused on preventive measures involving dietary control and physical exercises in combination with ...
Lu et al. “Chronic Exposure to Anticholinergic Medications Adversely Affects the Course of Alzheimer Disease” (Jul-Aug 2003) Am J Geriatr Psychiatry 11(4):458-461 (abstract). Maher-Edwards et al “Double-blind, controlled phase II study of a 5-HT6 receptor antagonist, SB-742457, in Al...