Structure activity relationship of selective GABA uptake inhibitors was written by Vogensen, Stine B.;Joergensen, Lars;Madsen, Karsten K.;Jurik, Andreas;Borkar, Nrupa;Rosatelli, Emiliano;Nielsen, Birgitte;Ecker, Gerhard F.;Schousboe, Arne;Clausen, Rasmus P.. And the article was included in Bioorganic & Medicinal Chemistry in 2015.Recommanded Product: Methyl piperazine-2-carboxylate dihydrochloride This article mentions the following:
A series of β-amino acids with lipophilic diarom. side chain was synthesized and characterized pharmacol. on mouse γ-amino butyric acid (GABA) transporter subtypes mGAT1-4 to investigate structure activity relationships (SAR) for mGAT2 (corresponding to hBGT-1). Variation in the lipophilic diarom. side chain was probed to understand the role of the side chain for activity. This yielded several selective compounds of which the best (1R,2S)-5a was more than 10 fold selective towards other subtypes, although potency was moderate. A docking study was performed to investigate possible binding modes of the compounds in mGAT2 suggesting a binding mode similar to that proposed for Tiagabine in hGAT1. Specific interactions between the transporter and the amino acid part of the ligands may account for a reverted preference towards mGAT2 over mGAT1. In the experiment, the researchers used many compounds, for example, Methyl piperazine-2-carboxylate dihydrochloride (cas: 122323-88-0Recommanded Product: Methyl piperazine-2-carboxylate dihydrochloride).
Methyl piperazine-2-carboxylate dihydrochloride (cas: 122323-88-0) belongs to piperazine derivatives. A form in which piperazine is commonly available industrially is as the hexahydrate, C4H10N2. 6H2O, which melts at 44 °C and boils at 125–130 °C. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines. The connecting property of all these chemicals is the presence of a piperazine functional group.Recommanded Product: Methyl piperazine-2-carboxylate dihydrochloride
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics