372198-80-6
Chemical Structure
Org 24461
- CAS No.: 372198-80-6
- Formula:C19H20F3NO3
- Molecular Weight:367.36
InChIKey: KZWQAWBTWNPFPW-UHFFFAOYSA-N
SMILES: O=C(CN(CCC(C1=CC=CC=C1)OC2=CC=C(C(F)(F)F)C=C2)C)O
Biological Activity: Org 24461 is a selective and brain-penetrant GlyT-1 inhibitor. Org 24461 blocks glycine uptake, reuptake, reverse operation, [3H]glycine efflux and release. Org 24461 enhances NMDA receptor function, modulates striatal monoamine/glutamate levels, and reverses PCP-induced behavioral and electrographic abnormalities. Org 24461 can be used for the research of retinal hypoxia/ischemia, and schizophrenia[1][2][3][4][5].
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Org 24461 | Org 24461 is a selective and brain-penetrant GlyT-1 inhibitor. Org 24461 blocks glycine uptake, reuptake, reverse operation, [3H]glycine efflux and release. Org 24461 enhances NMDA receptor function, modulates striatal monoamine/glutamate levels, and reverses PCP-induced behavioral and electrographic abnormalities. Org 24461 can be used for the research of retinal hypoxia/ischemia, and schizophrenia. | |||||||||||||||||||||
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- [1]. Kertesz S, et al. Temporal alteration of spreading depression by the glycine transporter type-1 inhibitors NFPS and Org-24461 in chicken retina. Brain Res. 2013;1492:1-6. [Content Brief]
- [2]. Harsing LG Jr, et al. Inhibition of hypoxia-induced [(3)H]glycine release from chicken retina by the glycine transporter type-1 (GlyT-1) inhibitors NFPS and Org-24461. Exp Eye Res. 2012;94(1):6-12. [Content Brief]
- [3]. Nagy K, et al. Alterations in brain extracellular dopamine and glycine levels following combined administration of the glycine transporter type-1 inhibitor Org-24461 and risperidone. Neurochem Res. 2010;35(12):2096-2106. [Content Brief]
- [4]. Harsing LG Jr, et al. The glycine transporter-1 inhibitors NFPS and Org 24461: a pharmacological study. Pharmacol Biochem Behav. 2003;74(4):811-825. [Content Brief]
- [5]. Papp A, et al. The synaptic and nonsynaptic glycine transporter type-1 inhibitors Org-24461 and NFPS alter single neuron firing rate in the rat dorsal raphe nucleus. Further evidence for a glutamatergic-serotonergic interaction and its role in antipsychotic action. Neurochem Int. 2008;52(1-2):130-134. [Content Brief]
Keywords
