<?xml version="1.0" encoding="UTF-8"?><xml><records><record><source-app name="Biblio" version="7.x">Drupal-Biblio</source-app><ref-type>17</ref-type><contributors><authors><author><style face="normal" font="default" size="100%">Adhikari, Amit Singh</style></author><author><style face="normal" font="default" size="100%">Yadav, Annu</style></author><author><style face="normal" font="default" size="100%">Pandit, Soumen</style></author><author><style face="normal" font="default" size="100%">Kumar, Suresh</style></author><author><style face="normal" font="default" size="100%">Pandey, Vinay Kumar</style></author><author><style face="normal" font="default" size="100%">Maurya, Arvind Kumar</style></author><author><style face="normal" font="default" size="100%">Umrao, Deepmala</style></author><author><style face="normal" font="default" size="100%">Chand, Diwan</style></author><author><style face="normal" font="default" size="100%">Maity, Debalina</style></author><author><style face="normal" font="default" size="100%">Gayen, Jiaur R.</style></author><author><style face="normal" font="default" size="100%">Srivastava, Kinshuk Raj</style></author><author><style face="normal" font="default" size="100%">Yadav, Prem N.</style></author><author><style face="normal" font="default" size="100%">Majumdar, Nilanjana</style></author></authors></contributors><titles><title><style face="normal" font="default" size="100%">Synthesis and evaluation of novel aza-aromatics as dual 5-HT2A and 5-HT2C receptor agonists</style></title><secondary-title><style face="normal" font="default" size="100%">ACS Medicinal Chemistry Letters</style></secondary-title></titles><keywords><keyword><style  face="normal" font="default" size="100%">5-HT2A</style></keyword><keyword><style  face="normal" font="default" size="100%">5-HT2C</style></keyword><keyword><style  face="normal" font="default" size="100%">Centhaquin</style></keyword><keyword><style  face="normal" font="default" size="100%">GPCR</style></keyword><keyword><style  face="normal" font="default" size="100%">Head Twitch Response</style></keyword><keyword><style  face="normal" font="default" size="100%">Serotonin Receptor</style></keyword></keywords><dates><year><style  face="normal" font="default" size="100%">2025</style></year><pub-dates><date><style  face="normal" font="default" size="100%">DEC </style></date></pub-dates></dates><volume><style face="normal" font="default" size="100%">16</style></volume><pages><style face="normal" font="default" size="100%">2435-2443</style></pages><language><style face="normal" font="default" size="100%">eng</style></language><abstract><style face="normal" font="default" size="100%">&lt;p&gt;
	The 5-HT2A and 5-HT2C receptors are key therapeutic targets for CNS disorders. We investigated whether a nonhallucinogenic dual 5-HT2A/5-HT2C agonist could offer novel treatment potential. Large screening of in-house structurally diverse compounds revealed centhaquin, an FDA-approved hypovolemic shock drug, as a selective 5-HT2C agonist (EC50: 35 nM). We then synthesized 22 aza-aryl analogs with modified piperazine groups, and identified two dual agonists, 3ci and 3dh (EC50 &amp;lt; 1 mu M), with no 5-HT2B activity up to 10 mu M. Molecular docking highlighted critical interactions with Ser159 (5-HT2A) and Ser138 (5-HT2C) on the upper side of the orthosteric binding pocket. Pharmacokinetic studies in mice demonstrated that 3ci was rapidly absorbed in the plasma and brain (T-max = 0.08 h; C-max = 936.4 ng/mL plasma, 2446.8 ng/g brain). Both compounds (3ci and 3dh, 20 mg/kg, i.p.) triggered a head-twitch response but were less potent than the hallucinogenic control 2,5-dimethoxy-4-iodoamphetamine, suggesting a reduced hallucinogenic liability. These results highlight 3ci as a promising lead for developing 5-HT2A/2C dual agonists to treat CNS disorders.&lt;/p&gt;
</style></abstract><issue><style face="normal" font="default" size="100%">12</style></issue><work-type><style face="normal" font="default" size="100%">Article</style></work-type><custom3><style face="normal" font="default" size="100%">&lt;p&gt;
	Foreign&lt;/p&gt;
</style></custom3><custom4><style face="normal" font="default" size="100%">&lt;p&gt;4.0&lt;/p&gt;
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