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KMID : 0043319990220020157
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Archives of Pharmacal Research
1999 Volume.22 No. 2 p.157 ~ p.164
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Pharmacolgocial Characterization of LB50016, N-(4-Amino)Butyl 3-Phenylpyrrolidine Derivative, as a New 5-HT_{1A}Receptor Agonist
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Lee Chang-Ho
Oh Jeong-In
Park hee-Dong
Kim Hee-Jin
Park Tae-Kyo
Kim Jae-Soon
Hong Chang-Yong
Lee Seok-Jong
Kim Yong-Zu
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Abstract
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LB50016 was characterized as a selective and potent receptor agonist and evaluate it anxiolytic and antidepressant activities. It shows high affinity for receptor, moderate affinity for 2 adrenergic and 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 receptor activation. In the mouse forced swim model for depression, LB50016-elicited dose-dependent reductions in immobility time, showing of approximately 3 mg/kg i.p., which was blocked by pretreatment of NAN-190, antagonist. In face-to-face test for anxiolytic activity in mice, estimated 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 receptors, offering an effective therapeutic candidate in the management of anxiety and depression in humans.
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KEYWORD
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5-HT1A receptors, Anxiolytic, Antidepressant, LB50016, Pyrrolidine
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