IOP response induced by selective 5-HT1A receptor agonists and 5-HT2 receptor antagonists after topical ocular administration to the hypertensive eye of conscious cynomolgus monkeys
Compounda | Reported Receptor Selectivity | Baseline IOPb | Percentage IOP Reduction 3 h Postdoseb |
|---|---|---|---|
| mm Hg | |||
| (R)-8-OH-DPATc | 5-HT1A agonistd | 30.4 (1.95) | 4.0 (4.84) |
| DP-5-CTc | 5-HT1A agonistd | 38.0 (2.99) | 11.9 (1.67) |
| Flesinoxanf,g | 5-HT1A agonist α1-antagonistd | 37.4 (3.88) | 11.6 (1.91) |
| 5-Me-urapidilh | 5-HT1A agonist α1-antagonistd | 45.0 (3.75) | 16.8 (9.38) |
| WB-4101c | 5-HT1A agonist α1-antagonistd | 45.2 (3.45) | 9.5 (5.38) |
| Ketanserinf | 5-HT2A antagonist | ||
| α1 antagonist | 40.6 (3.53) | 3.4 (6.39) | |
| M-100907c | 5-HT2A antagonist | ||
| α1 antagonist | 35.8 (2.04) | 15.8 (3.81) | |
| Cinanserinc | 5-HT2 antagonist | 40.9 (3.45) | 6.8 (2.18) |
| Ritanserinc | 5-HT2 antagonist | ||
| α1 antagonist | 34.6 (1.96) | 10.2 (3.58) | |
| SB-206553c | 5-HT2B/2C antagonist | 39.1 (2.32) | 13.4 (4.41) |
| RS-102221c | 5-HT2C antagonist | 35.8 (3.17) | 7.9 (2.62) |
| SB-242084c | 5-HT2C antagonist | 35.6 (2.20) | 12.2 (1.69) |
e Highest dose tested, 500 μg.
↵ a Highest dose tested; vehicle, phosphate-buffered saline, pH 7.4.
↵ b Values are the mean of at least eight animals ± S.E.M.
↵ c Highest dose tested, 300 μg.
↵ d See Table 1 for 5-HT1A receptor binding and functional data.
↵ f Highest dose tested, 250 μg.
↵ g pH 6.2.
↵ h Highest dose tested, 1000 μg.