We previously reported that the novel dual 5-HT₂B and 5-HT7 receptor antagonist N-(9-hydroxy-9H-fluorene-2-carbonyl)guanidine (4) exerted a suppressing effect on 5-HT-induced dural protein extravasation in guinea pigs. To develop a synthetic strategy, we performed docking studies of lead compound 4 bound
The Journal of pharmacology and experimental therapeutics, 294(2), 672-679 (2000-07-20)
The 5-hydroxytryptamine(7) (5-HT(7)) receptor was originally defined by molecular biology techniques. The 5-HT(7) receptor protein and mRNA are found in brain areas, such as the CA3 subfield of the hippocampus, that are involved in various neuropsychiatric disease states. No functional
FASEB journal : official publication of the Federation of American Societies for Experimental Biology, 33(3), 3870-3886 (2018-12-07)
According to early models of GPCR signaling, G proteins only interact with activated receptors. However, some GPCRs were shown to assemble with G proteins before receptor activation, in accordance with more recent models. Previously, we found that the 5-HT7 receptor
Mutations in mitochondrial DNA (mtDNA) have been linked to a variety of metabolic, neurological and muscular diseases which can present at any time throughout life. MtDNA is replicated by DNA polymerase gamma (Pol γ), twinkle helicase and mitochondrial single-stranded binding
International immunopharmacology, 52, 93-100 (2017-09-11)
Chronic inflammation is a major contributing factor in the pathogenesis of many diseases. Natural product berberine (BBR) exhibits potent anti-inflammatory effect in vitro and in vivo, while the underlying mechanisms remain elusive. Sirt1, a NAD
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