(R)-1,2,3,4-tetrahydro[1]benzothieno[2,3-c]pyridines: novel optically active compounds with strong 5-HT1A receptor binding ability exhibiting anticonflict activity and lessening of memory impairment.
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Kawakubo H, Takagi S, Yamaura Y, Katoh S, Ishimoto Y, Nagatani T, Mochizuki D, Kamata T, Sasaki Y
(R)-1,2,3,4-tetrahydro[1]benzothieno[2,3-c]pyridines: novel optically active compounds with strong 5-HT1A receptor binding ability exhibiting anticonflict activity and lessening of memory impairment.
J Med Chem. 1993 Nov 12;36(23):3526-32.
- PubMed ID
- 7902439 [ View in PubMed]
- Abstract
(R)-1,2,3,4-Tetrahydro[1]benzothieno[2,3-c]pyridine derivatives (60-114) were synthesized. The (R)-isomers have affinity for the 5-HT1A receptor while the (S)-isomers have no such ability. The affinity of the (R)-isomers was discussed on the basis of structure-activity relationships between the affinity and hydrophobicity of the (R)-isomers. Compounds 71 and 107, which are representative derivative compounds, have anticonflict activity and lessening of memory impairment. In particular, compound 107 cannot bind to receptors other than the 5-HT1A receptor, demonstrating that it is a unique compound with a different mechanism of action from that of conventional anxiolytics.
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- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Buspirone Dopamine D2 receptor Ki (nM) 90 N/A N/A Details