Citation

Lee CH, Oh JI, Park HD, Kim HJ, Park TK, Kim JS, Hong CY, Lee SJ, Ahn KH, Kim YZ. Arch. Pharm. Res. 1999; 22(2): 157-164.

Affiliation

Department of Pharmacology, Hanyang University, College of Medicine, Seoul, Korea.

Copyright

(Copyright © 1999, Pharmaceutical Society of Korea, Publisher Holtzbrinck Springer Nature Publishing Group)

DOI

unavailable

PMID

10230506

Abstract

LB50016 was characterized as a selective and potent 5-HT1A receptor agonist and evaluate its anxiolytic and antidepressant activities. It shows high affinity for 5-HT1A receptor, moderate affinity for alpha 2 adrenergic and 5-HT2A receptors and no significant affinity for other receptors tested. Hypothermia and increased serum corticosterone level were observed in LB50016-treated rats, which are mediated mostly by post synaptic 5-HT1A receptor activation. In the mouse forced swim model for depression, LB50016-elicited dose-dependent reductions in immobility time, showing ED50 of approximately 3 mg/kg i.p., which was blocked by pretreatment of NAN-190, 5-HT1A antagonist. In face-to-face test for anxiolytic activity in mice, estimated ED50 was 2 mg/kg, i.p. In isolation-induced aggression test with mice, fifty-fold increases in latency to attack were observed at 30 min and last up to 4 h after LB50016 treatment (3 mg/kg, i.p.). Taken together, LB50016-induced pharmacological activities are mediated by activation of 5-HT1A receptors, offering an effective therapeutic candidate in the management of anxiety and depression in humans.

Language: en