title: Levo-Tetrahydroberberrubine Produces Anxiolytic-Like Effects in Mice through the 5-HT1A Receptor.
abstract: Tetrahydroprotoberberines (THPBs) are isoquinoline alkaloids isolated from the Chinese herb Corydalis yanhusuo. In the present study, we performed competitive binding assays to examine the binding of l-THBr to neurotransmitter receptors known to be involved in sedation, hypnosis and anxiety. Our results show that l-THBr does not interact with GABAergic receptors but has binding affinities for dopamine and serotonin receptors. In addition, cAMP and [35S]GTPγS assays were used to determine the agonist or antagonist properties of l-THBr at dopamine (D1, D2) or serotonin (5-HT) receptors. Our results show that l-THBr displays D1 and D2 antagonist and 5-HT1A agonist properties. Moreover, l-THBr-treated rodents exhibit anxiolytic-like effects in the light/dark box and elevated plus-maze tests, and the anxiolytic effect of l-THBr can be reduced by WAY-100635, a selective 5-HT1A receptor antagonist. Our results suggest that l-THBr may produce potent anxiolytic-like effects mainly through serotonin receptors.
authors.affiliation: Beijing Institute of Basic Medical Sciences, Haidian District, Beijing, China.
authors.forename: Guiyun
authors.initials: G
authors.lastname: Mi
authors.affiliation: Beijing Institute of Basic Medical Sciences, Haidian District, Beijing, China.
authors.forename: Shuai
authors.initials: S
authors.lastname: Liu
authors.affiliation: Department of Complex Prescription of Traditional Chinese Medicine, China Pharmaceutical University, Nanjing, China.
authors.forename: Jian
authors.initials: J
authors.lastname: Zhang
authors.affiliation: Beijing Institute of Basic Medical Sciences, Haidian District, Beijing, China.
authors.forename: Huichun
authors.initials: H
authors.lastname: Liang
authors.affiliation: The 89 Hospital of PLA, WeiFang, China.
authors.forename: Yunyun
authors.initials: Y
authors.lastname: Gao
authors.affiliation: Beijing Institute of Basic Medical Sciences, Haidian District, Beijing, China.
authors.forename: Nuomin
authors.initials: N
authors.lastname: Li
authors.affiliation: Department of Complex Prescription of Traditional Chinese Medicine, China Pharmaceutical University, Nanjing, China.
authors.forename: Boyang
authors.initials: B
authors.lastname: Yu
authors.affiliation: Beijing Institute of Basic Medical Sciences, Haidian District, Beijing, China.
authors.forename: Hongju
authors.initials: H
authors.lastname: Yang
authors.affiliation: Beijing Institute of Basic Medical Sciences, Haidian District, Beijing, China.
authors.forename: Zheng
authors.initials: Z
authors.lastname: Yang
mesh_terms: D000818:Animals; D014151:Anti-Anxiety Agents / Q000494:pharmacology*; D001007:Anxiety / Q000188:drug therapy* / Q000378:metabolism; D001522:Behavior, Animal / Q000187:drug effects*; D001599:Berberine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D008297:Male; D051379:Mice; D008813:Mice, Inbred ICR; D051381:Rats; D017207:Rats, Sprague-Dawley; D044282:Receptor, Serotonin, 5-HT1A / Q000378:metabolism*; D017447:Receptors, Dopamine D1 / Q000378:metabolism; D017448:Receptors, Dopamine D2 / Q000378:metabolism; D058825:Serotonin 5-HT1 Receptor Agonists / Q000494:pharmacology*
chemical_list: D014151:Anti-Anxiety Agents; D017447:Receptors, Dopamine D1; D017448:Receptors, Dopamine D2; D058825:Serotonin 5-HT1 Receptor Agonists; D001599:Berberine; D044282:Receptor, Serotonin, 5-HT1A; C000613728:tetrahydroberberrubine