• 제목/요약/키워드: LB50016

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Pharmacolgocial Characterization of LB50016, N-(4-Amino)Butyl 3-Phenylpyrrolidine Derivative, as a New 5-HT_{1A}Receptor Agonist

  • Lee, Chang-Ho;Oh, Jeong-In;Park, Hee-Dong;Kim, Hee-Jin;Park, Tae-Kyo;Kim, Jae-Soon;Hong, Chang-Yong;Lee, Seok-Jong;Ahn, Kyo-Han;Kim, Yong-Zu
    • Archives of Pharmacal Research
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    • 제22권2호
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    • pp.157-164
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    • 1999
  • LB50016 was characterized as a selective and potent$ 5-HT_{1A}$ receptor agonist and evaluate it anxiolytic and antidepressant activities. It shows high affinity for $ 5-HT_{1A}$receptor, moderate affinity for $\alpha$2 adrenergic and $ 5-HT_{2A}$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-HT_{1A}$ receptor activation. In the mouse forced swim model for depression, LB50016-elicited dose-dependent reductions in immobility time, showing $ED_{50}$ of approximately 3 mg/kg i.p., which was blocked by pretreatment of NAN-190, $ 5-HT_{1A}$antagonist. In face-to-face test for anxiolytic activity in mice, estimated $ED_{50}$ 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-HT_{1A}$receptors, offering an effective therapeutic candidate in the management of anxiety and depression in humans.

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