TY  - JOUR
PY  - 1999//
TI  - Pharmacological characterization of LB50016, N-(4-amino)butyl 3-phenylpyrrolidine derivative, as a new 5-HT1A receptor agonist
JO  - Archives of pharmacal research
A1  - Lee, C. H.
A1  - Oh, J. I.
A1  - Park, H. D.
A1  - Kim, H. J.
A1  - Park, T. K.
A1  - Kim, J. S.
A1  - Hong, C. Y.
A1  - Lee, S. J.
A1  - Ahn, K. H.
A1  - Kim, Y. Z.
SP  - 157
EP  - 164
VL  - 22
IS  - 2
N2  - 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.<p /> <p>Language: en</p>
LA  - en
SN  - 0253-6269
UR  - http://dx.doi.org/
ID  - ref1
ER  -