- Binding properties of dipropyltryptamine at the human 5-HT1a receptor
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Dipropyltryptamine (DPT) is a synthetic indolealkylamine first characterized in the 1960s. Largely forgotten since the discovery of multiple serotonin receptor subtypes, some of the properties of DPT at the cloned human 5-HT1a receptor are described here. When [3H]8-OH-DPAT is bound to the receptor, DPT inhibits the interaction with an IC50 of 0.1 μmol/l. This interaction is shown to be competitive when double-reciprocal plots of the DPT/agonist interaction are analyzed. DPT's effects in the signal transduction system are complex. While DPT alone (0.1-1,000 μmol/l) activates Gi when both cAMP and γ-S-GTP incorporation are measured, in the presence of 5-HT (0.1-10 μmol/l), DPT blocks the agonist effect. In combination, the findings suggest that DPT is a moderate affinity partial agonist at the human 5-HT1a receptor. These results provide evidence that DPT has potential as a versatile experimental tool at 5-HT1a receptors. Copyright
- Thiagaraj, Harish V.,Russo, Ethan B.,Burnett, Andrea,Goldstein, Eric,Thompson, Charles M.,Parker, Keith K.
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- Benzocarbazoles heterocyclic compound and its preparation and use (by machine translation)
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The present invention provides a class of non-nucleoside anti-viral inhibitors, in particular to such as shown in formula I benzo heterocyclic compound or its pharmaceutically acceptable salt or hydrate, the invention also provides the compound or its pharmaceutically acceptable salt or hydrate of the preparation method. Pharmacological test indicates that the compound or its pharmaceutically acceptable salt or hydrate can effectively inhibit hepatitis b virus DNA replication and hepatitis c virus RNA replication, therefore, the invention also provides the compounds in the preparation of preventing and/or the treatment of viral infections, particularly hepatitis b virus (HBV) infection, hepatitis c virus (HCV) infection of use of the medicament. (by machine translation)
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Paragraph 0106; 0108
(2016/10/07)
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- Tryptamine derivatives as novel non-nucleosidic inhibitors against hepatitis B virus
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A series of tryptamine derivatives were synthesized and evaluated for their anti-hepatitis B virus (HBV) activity and cytotoxicity in the HepG2.2.15 cell line. The preliminary SAR was discussed. Compounds 2e and 4a showed potent antiviral activity (IC50 = 0.4 and 50 = 40.6 and >25 μM, respectively).
- Qu, Shi-Jin,Wang, Gui-Feng,Duan, Wen-Hu,Yao, Shan-Yan,Zuo, Jian-Ping,Tan, Chang-Heng,Zhu, Da-Yuan
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experimental part
p. 3120 - 3127
(2011/06/24)
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