GYKI-46903 is a non-competitive antagonist for 5-HT3 receptors. In displacement studies, the pIC50 values of GYKI-46903 against [3H]granisetron binding to rat cerebral cortex membranes were 6.91. GYKI-46903, when administered by intravenous infusion, antagonized the decrease in heart rate evoked by serotonin (Bezold-Jarisch reflex) in anaesthetized rats, and the maximal reversal was less than 50%.
MedKoo Cat#: 526606
Name: GYKI-46903 HCl
CAS#: 142999-59-5
Chemical Formula: C17H21ClFNO2
Exact Mass:
Molecular Weight: 325.81
Elemental Analysis: C, 62.67; H, 6.50; Cl, 10.88; F, 5.83; N, 4.30; O, 9.82
The following data is based on the product molecular weight 325.81 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
