Novel, flexible, and conformationally defined analogs of gepirone: synthesis and 5-HT1A, 5-HT2A, and D2 receptor activity.
Novel, flexible arylpiperazine gepirone analogs (1a-3a) with a mixed 5-HT1A/5-HT2A receptor profile, low D2 receptor affinity, and agonistic (2a) or partial agonistic (1a, 3a) activity toward 5-HT1A receptor sites were synthesized. Their conformationally restricted counterparts (1b-3b) were selective 5-HT1A ligands (over 5-HT2A and D2 receptors), which turned out to be agonists (2b, 3b), or partial agonist (1b) of 5-HT1A receptors.
Paluchowska
Maria H
MH
Department of Medicinal Chemistry, Institute of Pharmacology, Polish Academy of Science, 12 Smetna Street, 31-343 Kraków, Poland. paluchm@if-pan.karkow.pl
Bugno
Ryszard
R
Bojarski
Andrzej J
AJ
Charakchieva-Minol
Sijka
S
Duszyńska
Beata
B
Tatarczyńska
Ewa
E
Kłodzińska
Aleksandra
A
Stachowicz
Katarzyna
K
Chojnacka-Wójcik
Ewa
E
D000818:Animals; D018491:Dopamine Agonists / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D051379:Mice; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D017208:Rats, Wistar; D044282:Receptor, Serotonin, 5-HT1A / Q000187:drug effects*; D044402:Receptor, Serotonin, 5-HT2A / Q000187:drug effects*; D017448:Receptors, Dopamine D2 / Q000187:drug effects*; D017366:Serotonin Receptor Agonists / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology
D018491:Dopamine Agonists; D011743:Pyrimidines; D044402:Receptor, Serotonin, 5-HT2A; D017448:Receptors, Dopamine D2; D017366:Serotonin Receptor Agonists; D044282:Receptor, Serotonin, 5-HT1A; C039979:gepirone