Differences in agonist-independent activity of 5-HT2A and 5-HT2C receptors revealed by heterologous expression
β Scribed by M. S. Grotewiel; E. Sanders-Bush
- Publisher
- Springer-Verlag
- Year
- 1999
- Tongue
- English
- Weight
- 68 KB
- Volume
- 359
- Category
- Article
- ISSN
- 0028-1298
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π SIMILAR VOLUMES
The ternary complex model as applied to G-protein coupled receptors (GPCR) predicts that an agonist binds with low affinity (K L ) to the free receptor (R), leading to an agonist/receptor/G-protein complex. This ternary complex displays high agonist affinity (K H ), resulting in signal transduction.
Several substituted 2-pyridazinyl benzoxazole derivatives (VII), (VIII) and (IX) are prepared and evaluated for their utility as 5-HT 3 receptor agonists. A detailed structure-activity relationship study is presented. The most promising results are obtained for the derivatives (VIIa), (VIId) and (VI