Synthesis and structure-activity relationship of 2-(aminoalkyl)-2,3,3a,8-tetrahydrodibenzo[c,f]isoxazolo[2,3-a]azepine derivatives: a novel series of 5-HT(2A/2C) receptor antagonists. Part 1.
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Andres JI, Alcazar J, Alonso JM, Diaz A, Fernandez J, Gil P, Iturrino L, Matesanz E, Meert TF, Megens A, Sipido VK
Synthesis and structure-activity relationship of 2-(aminoalkyl)-2,3,3a,8-tetrahydrodibenzo[c,f]isoxazolo[2,3-a]azepine derivatives: a novel series of 5-HT(2A/2C) receptor antagonists. Part 1.
Bioorg Med Chem Lett. 2002 Jan 21;12(2):243-8.
- PubMed ID
- 11755364 [ View in PubMed]
- Abstract
The synthesis of a series of novel 2-(aminoalkyl)-2,3,3a,8-tetrahydrodibenzo[c,f]isoxazolo[2,3-a]azepine derivatives as well as their 5-HT(2A/2C) and H(1) receptor binding affinities are described. The in vivo activity as potential anxiolytics of the synthesised compounds was measured in a mCPP challenge test. One of the compounds, 2a, proved to be a potent 5-HT(2A/2C) receptor antagonist showing as well oral activity and therefore could be considered as a potential anxiolytic/antidepressant agent.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Mianserin 5-hydroxytryptamine receptor 1A IC 50 (nM) 398.11 N/A N/A Details Mianserin 5-hydroxytryptamine receptor 2A IC 50 (nM) 10.47 N/A N/A Details Mianserin 5-hydroxytryptamine receptor 2C IC 50 (nM) 7.41 N/A N/A Details Mianserin 5-hydroxytryptamine receptor 7 IC 50 (nM) 114.82 N/A N/A Details Mianserin Alpha-2A adrenergic receptor IC 50 (nM) 20.89 N/A N/A Details Mianserin Alpha-2C adrenergic receptor IC 50 (nM) 42.66 N/A N/A Details Mianserin Dopamine D2 receptor IC 50 (nM) 7079.46 N/A N/A Details Mianserin Dopamine D3 receptor IC 50 (nM) 3890.45 N/A N/A Details Mianserin Histamine H1 receptor IC 50 (nM) 3.39 N/A N/A Details