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It was discovered through high-throughput screening followed by lead optimization and was subsequently characterized as a potent and selective inhibitor of the GlyT1 transporter, with an IC 50 of 3040 nM (Pinard et al

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TABLE 8 The recovery of total radioactivity in bile, urine, feces, and cage cleaning fluid during 072 h after intramuscular administration of [3H]BPC157 in BDC rats