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Sedative and Hypnotic Drugs
Published in Sahab Uddin, Rashid Mamunur, Advances in Neuropharmacology, 2020
Arup Kumar Misra, Pramod Kumar Sharma
Volinanserin, eplivanserin, and pruvanserin are the new 5-HT2A serotonin receptor subtype agents. As compared with existing antidepressants with sedative action, they have least affinity for dopamine, histamine, and adrenergic receptors. These drugs have shown efficacy in maintenance of sleep and also increases in slow wave pattern of sleep. Eplivanserin was discontinued during development stages for unknown reasons. The drug development of volinanserin and pruvanserin were stopped despite having positive efficacy data of phase III clinical trial (Teegarden et al., 2008).
A definite measure of occupancy exposures, seeking with non-radiolabeled in vivo 5-HT2A receptor occupancy and in vitro free fractions
Published in Journal of Receptors and Signal Transduction, 2018
Gopinadh Bhyrapuneni, Jagadeesh Babu Thentu, Veera Raghava Choudary Palacharla, Nageswararao Muddana, Raghupathi Reddy Aleti, Devender Reddy Ajjala, Ramakrishna Nirogi
Quetiapine hemifumarate, eplivanserin hemifumarate, ketanserin tartrate, clozapine, olanzapine, and other chemical reagents were procured from Sigma-Aldrich, Chemicals (St. Louis, MO). MDL-100,907 hydrochloride was synthesized at Suven Life Sciences Ltd, Hyderabad, India. Quetiapine was dissolved in 0.25% (v/v) tween 80 plus 99.75% Carboxymethylcellulose (1% w/v) in milli-Q water, eplivanserin was dissolved in 20% (v/v) captisol with milli-Q water, ketanserin was dissolved in 20% captisol plus glucose (4% w/v) in 25 mM phosphate buffer, clozapine was dissolved in 0.5% acetic acid plus glucose (4% w/v) in 25 mM phosphate buffer, and olanzapine was dissolved in 10 µL acetic acid in 5.5% glucose solution. MDL-100,907 was dissolved in dimethyl sulfoxide (DMSO) and further diluted with normal saline (0.9% w/v) for intravenous administration. High-throughput dialysis assembly and dialysis membranes were obtained from HT Dialysis (Gales Ferry, CT).