Author: Gefteas, Estelle ; Smicker, Oanh ; Randall, Kristen ; Tietz, Drew ; Gregory, Jill ; Danthi, Sanjay J ; Klodnitsky, Helen ; Coupland, Benjamin ; Kuntzweiler, Theresa A ; Belanger, Adam ; Liang, Beirong

SLC6A19 (B⁰AT1) is a neutral amino acid transporter, the loss of function of which results in Hartnup disease. SLC6A19 is also believed to have an important role in amino acid homeostasis, diabetes, and weight control. A small-molecule inhibitor of human SLC6A19 (hSLC6A19) was identified using two functional cell-based assays: a fluorescence imaging plate reader (FLIPR) membrane potential (FMP) assay and a stable isotope-labeled neutral amino acid uptake assay. A diverse collection of 3440 pharmacologically active compounds from the Microsource Spectrum and Tocriscreen collections were tested at 10 µM in both assays using MDCK cells stably expressing hSLC6A19 and its obligatory subunit, TMEM27. Compounds that inhibited SLC6A19 activity in both assays were further confirmed for activity and selectivity and characterized for potency in functional assays against hSLC6A19 and related transporters. A single compound, cinromide, was found to robustly, selectively, and reproducibly inhibit SLC6A19 in all functional assays. Structurally related analogs of cinromide were tested to demonstrate structure-activity relationship (SAR). The assays described here are suitable for carrying out high-throughput screening campaigns to identify modulators of SLC6A19.

01 Aug 1989·EpilepsiaQ1 · MEDICINE

Double‐Blind, Placebo‐Controlled Evaluation of Cinromide in Patients with the Lennox‐Gastaut Syndrome

Q1 · MEDICINE

Article

01 Jan 1988·Physiologia Bohemoslovaca

Influence of cinromide on metrazol--induced seizures during ontogenesis in rats.

Article

Author: Mares, P ; Rokyta, R ; Bernásková, K

The effects of cinromide on two types of metrazol-induced seizures were studied in 236 male rats aged 7, 12, 18, 25 and 90 days. Cinromide was administered intraperitoneally in a dose of 25 or 50 mg.kg-1 30 min before a subcutaneous injection of metrazol. Major, i.e. generalized tonic-clonic seizures could be elicited by metrazol in all age groups. Cinromide was efficient against this type of seizures at all developmental stages, but its action in 7- and especially in 12-day-old rat pups was less marked than in older animals. Minimal metrazol seizures (predominantly clonic) could be reliably elicited since the age of 18 days. Cinromide was also able to suppress this type of seizures, but in adult rats the dose of 75 mg.kg-1 had to be administered because even the 50 mg.kg-1 dose was not sufficient. Quantitative changes of the antimetrazol action of cinromide were demonstrated during maturation in rats.

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Indication	Highest Phase	Country/Location	Organization	Date
Diabetes Mellitus	Preclinical	US	Sanofi Ventures	-

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