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2005
Thiadiazine derivatives
R 0660
1,2,4-Benzothiadiazine Derivatives as α1 and 5-HT1A Receptor Ligands. — The
and the pharmacological profile of six new benzothiadiazine-arylpiperazines
26- 103 synthesis
and the effect of some structural modifications on the affinity and selectivity for
α1-adrenergic and 5-HT 1A serotoninergic receptor subtypes are presented. The best profile of activity at adrenergic system resides in (VIa), which shows high α1D affinity and
relevant α1D selectivity. Compound (IXb) is identified as a novel 5-HT1A receptor ligand
and highly selective over α1D-adrenoceptor subtype. This compound can be considered
as a partial agonist at 5-HT1A receptor. — (TAIT*, A.; LUPPI, A.; FRANCHINI, S.;
PREZIOSI, E.; PARENTI, C.; BUCCIONI, M.; MARUCCI, G.; LEONARDI, A.;
POGGESI, E.; BRASILI, L.; Bioorg. Med. Chem. Lett. 15 (2005) 4, 1185-1188; Dip.
Sci. Farm., Univ. Modena, I-41100 Modena, Italy; Eng.) — H. Hoennerscheid
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