Skip to main content
. Author manuscript; available in PMC: 2019 Sep 25.
Published in final edited form as: Curr Top Med Chem. 2019;19(16):1381–1398. doi: 10.2174/1568026619666190709101449

Fig. (4). Proposed outcomes mediated by activation of specific members of the 5-HT2R family are depicted.

Fig. (4).

(A) The 5-HT receptor family is comprised of 13 GPCRs and one ligand-gated ion channel (divided into seven subtype categories). Each receptor is activated by endogenous 5-HT. Therefore, the orthosteric site is highly conserved across receptor subtypes. (B) Agonist-mediated activation of 5-HT2AR accounts for the hallucinogenic actions of such abused drugs as d-lysergic acid diethylamide. Agonist-mediated activation of 5-HT2BR can lead to pulmonary hypertension and valvular heart disease. Agonist-mediated activation of 5-HT2CR represents an attractive therapeutic approach to treat obesity, substance use disorders and impulse control disorders. However, the high sequence homology at the orthosteric sites of these receptors present challenges to selectively target the 5-HT2CR.