Table 2.
WAY-211612 is a dual SSRI/5-HT1A receptor antagonist
| Compound | 5-HT Transporter | 5-HT1A Receptors | |||
|---|---|---|---|---|---|
| Binding | Function | Binding | cAMP | GTPγS | |
| (Ki, nmol·L−1) | (KB, nmol·L−1) | (Ki, nmol·L−1) | (KB, nmol·L−1) | (KB, nmol·L−1) | |
| WAY-211612 | 1.5 ± 0.1 | 17.7 ± 3.3 | 1.2 ± 0.2 | 6.3 ± 0.23 | 19.8 ± 2.6 |
| Fluoxetine | 3.9 ± 0.3 | 37.3 ± 2.9 | |||
| WAY-100635 | 1.0 ± 0.2 | 1.64 ± 0.3 | 3.4 ± 0.3 | ||
Values shown are means ± SEM. 5-HT transporter affinity was determined by competition with 3H-paroxetine binding in rat cortical membranes and function was determined by the ability of compounds to inhibit 3H-5-HT uptake into JAR cells expressing the human 5-HT transporter. 5-HT1A affinity and function were obtained using recombinant human 5-HT1A receptors. Receptor affinity was determined using 3H-8-OHDPAT binding and antagonism was assessed using both an adenylate cyclase assay and a GTPγS assay. See methods for full details.
SSRI, 5-HT selective reuptake inhibitor.