Towards a New Generation of Potential Antipsychotic Agents Combining D2 and 5-HT1A Receptor Activities was written by Cuisiat, Stephane;Bourdiol, Nathalie;Lacharme, Vincent;Newman-Tancredi, Adrian;Colpaert, Francis;Vacher, Bernard. And the article was included in Journal of Medicinal Chemistry in 2007.Reference of 69393-72-2 This article mentions the following:
We report the discovery and the synthesis of novel, potential antipsychotic compounds combining potent dopamine D2 receptor antagonist and serotonin 5-HT1A receptor agonist properties in the same mol. We describe the structure-activity relationship that lead us to the promising derivative: N-[(2,2-dimethyl-2,3-dihydro-benzofuran-7-yloxy)ethyl]-3-(cyclopent-1-enyl)-benzylamine 16. The latter has high affinity for D2 and 5-HT1A receptors, whereas it possesses only a weak affinity for 5-HT2A sites. In cellular models of signal transduction, 16 behaves as a silent antagonist at rD2 receptors while activating h5-HT1A receptors with an efficacy at least equivalent to that of the prototypical 5-HT1A agonist (±)-8-OH-DPAT. These dual actions confer a unique pharmacol. profile to the product. In a behavioral model predictive of pos. symptoms, 16 has an activity comparable to that of the typical antipsychotic haloperidol, while it is devoid of cataleptogenic effects. Although it produces behaviors characteristic of 5-HT1A receptor activation in rats, these occur at doses 100 times higher than those with (±)-8-OH-DPAT. We believe that the relative balance of D2 and 5-HT1A actions in 16 is appropriate, possibly optimal, to ensure superior efficacy and tolerability over existing antipsychotic drugs. In the experiment, the researchers used many compounds, for example, Benzo[d][1,3]dioxol-4-ol (cas: 69393-72-2Reference of 69393-72-2).
Benzo[d][1,3]dioxol-4-ol (cas: 69393-72-2) belongs to alcohols. Under appropriate conditions, inorganic acids also react with alcohols to form esters. To form these esters, a wide variety of specialized reagents and conditions can be used. Converting an alcohol to an alkene requires removal of the hydroxyl group and a hydrogen atom on the neighbouring carbon atom. Dehydrations are most commonly carried out by warming the alcohol in the presence of a strong dehydrating acid, such as concentrated sulfuric acid.Reference of 69393-72-2
Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts