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.

Article Details

Citation

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
DrugTargetPropertyMeasurementpHTemperature (°C)
Mianserin5-hydroxytryptamine receptor 1AIC 50 (nM)398.11N/AN/ADetails
Mianserin5-hydroxytryptamine receptor 2AIC 50 (nM)20.89N/AN/ADetails
MianserinAlpha-2C adrenergic receptorIC 50 (nM)42.66N/AN/ADetails
MianserinDopamine D2 receptorIC 50 (nM)7079.46N/AN/ADetails
MianserinDopamine D3 receptorIC 50 (nM)3890.45N/AN/ADetails