Pharmacokinetics and Bioavailability of New Synthetic 5-HT2C Agonists, KKHQ80109 and KKHQ80114, in Sprague-Dawley Rats
- Pharmacokinetics and Bioavailability of New Synthetic 5-HT2C Agonists, KKHQ80109 and KKHQ80114, in Sprague-Dawley Rats
- 임혜연; 추현아; 배애님; 권오승
- 5-HT2c agonist; KKHQ80109; KKHQ80114; Pharmacokinetics; Bioavailability; Rats
- Issue Date
- VOL 39, NO 5, 327-331
- 5-HT2C receptors have been considered as therapeutic targets for the treatment of various central nervous
system disorders such as depression, anxiety, epilepsy, schizophrenia, and sleep disorders. We chemically synthesized
KKHQ80109 (K09) and KKHQ80114 (K14), selective 5-HT2C agonists, with the purpose of developing therapeutic agents
for the treatment of obesity. The objective of this work is to investigate pharmacokinetic parameters and bioavailability of
K09 and K14 in rats given orally or intravenously. Oral administration of 20 mg/kg K09 results in 4.11 hr of the terminal
half-life and 89.16 ng/ml of Cmax at 5.00 hr (Tmax). The terminal half-life of K14 was 3.83 hr with 215.81 ng/ml of Cmax
at 3.33 hr (Tmax) after oral dosing of 20 mg/kg K14, indicating that K14 is more rapidly absorbed than K09. Bioavailability
showed 0.17-0.21 for K09 and 0.19-0.23 for K14. Urinary excretion of parent K09 and K14 was less than 1%, indicating
that K09 and K14 undergo very extensive hepatic metabolism.
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