Rigid analogues of buspirone and gepirone, 5-HT1A receptors partial agonists

Chilmonczyk, 2001, 5-HT1A receptors and their role in anxiety and depression, Saudi Pharm. J., 9, 123 Schechter, 1999, Serotonergic antidepressants: Current and future perspectives, Curr. Opin. CPNS Invest. Drugs, 1, 432 Levine, 1999, 5-HT1A agonist, partial agonists and antagonists in anxiety and depression: A lost case?, Curr. Opin. CPNS Invest. Drugs, 1, 448 Paluchowska, 1999, On the bioactive conformation of NAN-190 (1) and MP3022 (2), 5-HT1A receptor antagonists, J. Med. Chem., 42, 4952, 10.1021/jm991045h Chilmonczyk, 1995, Buspirone analogues as ligands of the 5-HT1A receptor. 1. The molecular structure of buspirone and its two analogues, J. Med. Chem., 38, 1701, 10.1021/jm00010a015 Chilmonczyk, 1997, Conformational flexibility of serotonin1A receptor ligands from crystallographic data. Updated model of receptor pharmacophore, Arch. Pharm. Pharm. Med. Chem., 330, 146, 10.1002/ardp.19973300507 Nelson, 1957, Bicyclo[3.1.0]hexane derivatives. I. Synthesis of bicyclo[3.1.0]-2-hexanone and methyl bicyclo[3.1.0]hexane-1-carboxylate, J. Org. Chem., 22, 1146, 10.1021/jo01361a003 Franzus, 1963, Structural determination of cis- and trans-1,3-dibromocyclohexane, J. Org. Chem., 2238, 10.1021/jo01044a020 Howard, 1953, Piperazines. II. 1-Heterocyclicpiperazines and 1-heterocyclic-4-carbethoxypiperazines, J. Org. Chem., 18, 1484, 10.1021/jo50017a004 Middlemis, 1983, 8-Hydroxy-2-(di-n-propylamino)-tetralin discriminates between subtypes of the 5-HT1 recognition site, Eur. J. Pharmacol., 9, 151, 10.1016/0014-2999(83)90230-3 Bojarski, 1993, Structure–activity relationship studies of CNS agents. Part 9. 5-HT1A and 5-HT2 receptor affinity of some 2- and 3-substituted 1,2,3,4-tetrahydro-carbolines, Pharmazie, 48, 289 Mokrosz, 1995, Quantitative analysis of alkyl chain effects on the 5-HT1A and 5-HT2 receptor affinities of 4-alkyl-1-arylpiperazines and their analogs, Arch. Pharm. (Weinheim), 328, 143, 10.1002/ardp.19953280210 Hoyer, 1991, 5-HT receptors: Subtypes and second messengers, J. Receptor Res., 11, 197, 10.3109/10799899109066399 Mokrosz, 1992, Part 5. Effect of the hydrocarbon chain on the affinity of 4-substituted 1-(3-chlorophenyl)piperazines for 5-HT1A receptor site, J. Med. Chem., 35, 2369, 10.1021/jm00091a004 Mokrosz, 1994, Strukture–activity relationship studies of CNS agents. Part 14: Structural requirements for the 5-HT1A and 5-HT2A receptor selectivity 1-(2-pyrimidyl)piperazine derivatives, Pharmazie, 49, 801 Pardo, 1997, The effect of the molecular mechanism of G protein-coupled receptor activation on the process of signal transduction, Eur. J. Pharmacol., 335, 73, 10.1016/S0014-2999(97)01170-9