5-Hydroxytryptamine1A receptor binding activity of bisbenzyltetrahydroisoquinoline alkaloids from Popowia odoardi
A 96-well filtration-based 5-HT1A receptor-radioligand binding assay was optimized and adapted to carry out a bioassay-guided fractionation of the methanol extract of the bark of Popowia odoardi Diels(Annonaceae). This purification led to the isolation of two compounds identified as O-methyldaurici...
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| Main Authors: | , , , , |
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| Format: | Article |
| Language: | en |
| Published: |
Taylor & Francis
2009
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| Subjects: | |
| Online Access: | http://eprints.um.edu.my/2454/1/5-Hydroxytryptamine1A_receptor_binding_activity_of_bisbenzyltetrahydroisoquinoline_alkaloids_from_Popowia_odoardi.pdf http://eprints.um.edu.my/2454/ |
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| Summary: | A 96-well filtration-based 5-HT1A receptor-radioligand binding assay was optimized and adapted to carry out a bioassay-guided fractionation of the methanol extract of the bark of Popowia odoardi Diels(Annonaceae). This purification led to the isolation of two compounds identified as O-methyldauricine (1)and popisidine (2), which bind competitively to 5-HT 1A receptors at high concentrations with K ivalues of 4.5 and 5.8 μM, with [
3 H]8-OH-DPAT as the radioligand. These results suggest that both of these bisbenzyltetrahydroisoquinoline alkaloids influence the activity of 5-HT 1A receptors through competitive binding as agonists or antagonists and may possess anxiolytic and anti-depressive effects. |
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