Pharmacological characterization of LB50016, N-(4-amino)butyl 3-phenylpyrrolidine derivative, as a new 5-HT1A receptor agonist
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SCOPUS
- Title
- Pharmacological characterization of LB50016, N-(4-amino)butyl 3-phenylpyrrolidine derivative, as a new 5-HT1A receptor agonist
- Authors
- Lee, CH; Oh, JI; Park, HD; Kim, HJ; Park, TK; Kim, JS; Hong, CY; Lee, SJ; Ahn, KH; Kim, YZ
- Date Issued
- 1999-04
- Publisher
- PHARMACEUTICAL SOCIETY KOREA
- Abstract
- LB50016 was characterized as a selective and potent 5-MT1A 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.
- Keywords
- 5-HT1A receptors; anxiolytic; antidepressant; LB50016; pyrrolidine; 5-HYDROXYTRYPTAMINE(1A) AGONIST; ANIMAL-MODELS; BINDING-SITES; RAT; ANTAGONIST; HYPOTHERMIA; DEPRESSION; RESPONSES; 8-OH-DPAT; BUSPIRONE
- URI
- https://oasis.postech.ac.kr/handle/2014.oak/20438
- DOI
- 10.1007/BF02976540
- ISSN
- 0253-6269
- Article Type
- Article
- Citation
- ARCHIVES OF PHARMACAL RESEARCH, vol. 22, no. 2, page. 157 - 164, 1999-04
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