Pharmacokinetics and Pharmacodynamics of the Glutamate Carboxypeptidase (GCP) II Inhibitor 2-MPPA Show Prolonged Alleviation of Neuropathic Pain Through an Indirect Mechanism
نویسندگان
چکیده
Brain Science Institute, NeuroTranslational Drug Discovery Program, Johns Hopkins University, Baltimore, MD., (K.M.W., Y.W., C.R., R.R., B.S.S.) Department of Neurology, Johns Hopkins School of Medicine, Baltimore, MD., (J.J.V., B.S.S., R.R.) Cerecor Inc., Baltimore, MD., (J.J.V.) Department of Psychiatry, Johns Hopkins School of Medicine, Baltimore, MD., (B.S.S.) JPET Fast Forward. Published on June 17, 2013 as DOI:10.1124/jpet.113.205039
منابع مشابه
Pharmacokinetics and pharmacodynamics of the glutamate carboxypeptidase II inhibitor 2-MPPA show prolonged alleviation of neuropathic pain through an indirect mechanism.
Glutamate carboxypeptidase II (GCP II) is a therapeutic target in neurologic disorders associated with excessive activation of glutamatergic systems. The potent, orally bioavailable GCP II inhibitor 2-(3-mercaptopropyl) pentanedioic acid (2-MPPA) is effective in preclinical models of diseases where excess glutamate release is implicated, including neuropathic pain, and was the first GCP II inhi...
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Glutamate carboxypeptidase II (GCP-II) is a brain metallopeptidase that hydrolyzes the abundant neuropeptide N-acetyl-aspartyl-glutamate (NAAG) to NAA and glutamate. Small molecule GCP-II inhibitors increase brain NAAG, which activates mGluR3, decreases glutamate, and provide therapeutic utility in a variety of preclinical models of neurodegenerative diseases wherein excess glutamate is presume...
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