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 2.
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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 2.
Bioorg Med Chem Lett. 2002 Jan 21;12(2):249-53.
- PubMed ID
- 11755365 [ View in PubMed]
- Abstract
Following the programme started at Janssen Research Foundation searching for 5-HT(2A/2C) antagonists, we now report on the synthesis of a series of substituted 2-(Dimethylaminomethyl)-2,3,3a,8-tetrahydrodibenzo[c,f]isoxazolo[2,3-a]azepine derivatives. The 5-HT(2A), 5-HT(2C) and H(1) receptor affinities as well as the mCPP antagonistic activity of the compounds synthesised is described.
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) 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