English Journal

Ackermann TM, Bhokare K, Höfner G, Wanner KT.
Neuropharmacology. 2019 12;161()107561.
In this study an alternative to radioligand binding assays addressing the glycine transporter 1 (GlyT1) based on quantification of a nonlabelled reporter ligand by means of mass spectrometry (MS) is presented. The established MS Binding Assays employ the GlyT1 inhibitor Org24598 as reporter ligand f
PMID 30851306

Al-Khrasani M, Mohammadzadeh A, Balogh M, Király K, Barsi S, Hajnal B, Köles L, Zádori ZS, Harsing LG.
Brain research bulletin. 2019 10;152()143-158.
Interneurons operating with glycine neurotransmitter are involved in the regulation of pain transmission in the dorsal horn of the spinal cord. In addition to interneurons, glycine release also occurs from glial cells neighboring glutamatergic synapses in the spinal cord. Neuronal and glial release
PMID 31302238

Phylogeny of the genus Hypophthalmus Cuvier, 1829 (Pimelodidae - Siluriformes), based on a multilocus analysis, indicates diversification and introgression in the Amazon basin.

Santos JCMD, Ferreira ES, Oliveira C, Oliveira TB, Costa ASLD, Queiroz AKO, Schneider H, Sampaio I, Santos S.
Molecular phylogenetics and evolution. 2019 08;137()285-292.
The genus Hypophthalmus encompasses four valid South American freshwater catfish species: H. marginatus, H. edentatus, H. fimbriatus, and H. oremaculatus. More recently two new species were proposed Hypophthalmus n. sp. 1 and Hypophthalmus n. sp. 2. While Hypophthalmus species are a fundamentally im
PMID 31121309

Japanese Journal

内山博登,渡辺俊,森田元樹,尾山実砂,岩井孝志,田辺光男
日本薬理学会年会要旨集 93(0), 3-P-363, 2020
… Glycine transporter subtype 1 (GlyT1) is abundant in astrocytes and GlyT1 inhibitors have analgesic effect. … We found that GlyT1 mRNA expression in C6 glioma cells was increased during amino acid starvation. … To investigate the mechanisms underlying GlyT1 mRNA upregulation, we focused on ATF4 (activating transcription factor 4) that is activated during amino acid starvation and mTOR (mammalian target of rapamycin) that is inactivated during amino acid starvation. …
NAID 130007811923

Identification of 1-Methyl-N-(propan-2-yl)-N-({2-[4-(trifluoromethoxy)phenyl]pyridin-4-yl}methyl)-1H-imidazole-4-carboxamide as a Potent and Orally Available Glycine Transporter 1 Inhibitor

Yamamoto Shuji,Ohta Hiroshi,Abe Kumi,Kambe Daiji,Tsukiyama Naohiro,Kawakita Yasunori,Moriya Minoru,Yasuhara Akito
ＣＨＥＭＩＣＡＬ　＆　ＰＨＡＲＭＡＣＥＵＴＩＣＡＬ　ＢＵＬＬＥＴＩＮ 64(11), 1630-1640, 2016
… We previously identified 3-chloro-N-{(S)-[3-(1-ethyl-1H-pyrazol-4-yl)phenyl][(2S)-piperidine-2-yl]methyl}-4-(trifluoromethyl)pyridine-2-carboxamide (5, TP0439150) as a potent and orally available glycine transporter 1 (GlyT1) inhibitor. … exhibited potent GlyT1 inhibitory activity, a favorable pharmacokinetics profile, and elicited an increase in the cerebrospinal fluid (CSF) concentration of glycine in rats. …
NAID 130005268088

Discovery of 3-Chloro-N-{(S)-[3-(1-ethyl-1H-pyrazol-4-yl)phenyl][(2S)-piperidine-2-yl]methyl}-4-(trifluoromethyl)pyridine-2-carboxamide as a Potent Glycine Transporter 1 Inhibitor

Yamamoto Shuji,Shibata Tsuyoshi,Abe Kumi,Oda Koji,Aoki Takeshi,Kawakita Yasunori,Kawamoto Hiroshi
ＣＨＥＭＩＣＡＬ　＆　ＰＨＡＲＭＡＣＥＵＴＩＣＡＬ　ＢＵＬＬＥＴＩＮ 64(9), 1321-1337, 2016
… A novel glycine transporter 1 (GlyT1) inhibitor was designed by the superposition of different chemotypes to enhance its inhibitory activity. … Starting from 2-chloro-N-{(S)-phenyl[(2S)-piperidin-2-yl]methyl}-3-(trifluoromethyl)benzamide (2, SSR504734), the introduction of heteroaromatic rings enabled an increase in the GlyT1 inhibitory activity. …
NAID 130005261563