PF-03463275是一种中枢神经系统渗透性、具有口服活性、选择性、竞争性甘氨酸转运蛋白-1(GlyT1)可逆抑制剂，Ki为11.6nM。PF-03463275有可能用于精神分裂症的研究。
PF-03463275 is a centrally penetrant, orally available, selective, and competitive GlyT1 (glycine transporter-1) reversible inhibitor, with a Ki of 11.6 nM. PF-03463275 has the potential for Schizophrenia research[1][2].
PF-03463275 (1-10 mg/kg; s.c.) attenuates oscillatory potentials (OPs)[2]. Animal Model: Male Sprague-Dawley rats[2]
[1]. Lowe JA 3rd, et al. The discovery of a structurally novel class of inhibitors of the type 1 glycine transporter [published correction appears in Bioorg Med Chem Lett. 2009 Aug 15;19(16):4885. Bronk, Brian S [added]; Schaeffer, Eric [added]]. Bioorg Med Chem Lett. 2009;19(11):2974-2976. [2]. Liu CN, Pettersen B, Seitis G, Osgood S, Somps C. GlyT1 inhibitor reduces oscillatory potentials of the electroretinogram in rats. Cutan Ocul Toxicol. 2014;33(3):206-211.
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