5-HT2A receptor ligand

F]Fluorobenzophenones are also precursors, after reduction into the corresponding alcohol, of different complex structures such as a 5-HT2A receptor ligand [180] and several dopamine transporter ligands GBR 13119 [181], GBR 12909 [182] and analogues [183], NNC 12-0817 and 12-0818 [184] (Scheme 40). 

Johnson MP, Siegel BW, Carr AA. [3H]MDL 100,907 a novel selective 5-HT2A receptor ligand. Naunyn-Schmicdcbcrgs Arch Pharmacol 1996 354 205-209. 

Travis, M. J., Busatto, G. F., Pilowsky, L. S. et al. 5-HT2A receptor blockade in patients with schizophrenia treated with risperidone or clozapine. A SPET study using the novel 5-HT2A ligand 123I-5-I-R-91150. Br. J.Psychiatr. 173 236-241, 1998. 

Pietzsch, H. J., Scheunemann, M., Kretzschmar, M. et al. Synthesis and autoradiographic evaluation of a novel high-affinity Tc-99m ligand for the 5-HT2A receptor. Nucl. Med. Biol. 26 865-875,1999. 

Fig. 2. Results from the MD simulations showing the values of the angle between the indole plane of W6.48 and the plane of the membrane in the presence (A) and absence (B) of the ligand, 5-HT, interacting with the F6.52 sensor in the binding pocket of the 5-HT2A receptor model.

Ebersole, B. J., Visiers, I., Weinstein, H., and Sealfon, S. (2003) Molecular basis of partial agonism orientation of indolamine ligands in the binding pocket of the human serotonin 5-HT2A receptor determines relative efficacy. Mol. Pharmacol. 63, 36—43. 

P.Z. Tan, R.M. Baldwin, T. Fu, D.S. Charney, R.B. Innis, Rapid synthesis of F-18 and H-2 dual-labeled altanserin, a metabolically resistant PET ligand for 5-HT2A receptors, J. Label. Compds Radiopharm. 42 (1999) 457-467. 

Fig. 3. Two-dimensional analysis of PDZ proteins interacting with the 5-HT2A and the 5-HT2C receptors C-termini. (A) Proteins from mice brain that bind to the C-terminus of the last 14 residues of the receptors were separated on 2D gels and stained with silver. Proteins that interact specifically (directly or indirectly) with the PDZ ligand of the receptor (arrows) were detected comparing protein patterns obtained with the native peptides (see Fig. 1) and mutant peptides in which the last residue was replaced by alanine. The position of one protein retained in a PDZ-independent manner by the 5-HT2A receptor C-terminus is also indicated (arrowhead). (B) Molecular determinants in the C-terminus of 5-HT2A receptor involved in its preferential interaction with CIPP.

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