PF 03463275
PF 03463275 Basic information
- Product Name:
- PF 03463275
- Synonyms:
-
- PF0346275
- 1H-Imidazole-4-carboxamide, N-[(3-chloro-4-fluorophenyl)methyl]-1-methyl-N-[[(1α,5α,6α)-3-methyl-3-azabicyclo[3.1.0]hex-6-yl]methyl]-
- PF-03463275, 10 mM in DMSO
- 1H-Imidazole-4-carboxamide, N-[(3-chloro-4-fluorophenyl)methyl]-1-methyl-N-[[(1α,5α,6α)-3-methyl-3-azabicyclo[3.1.0]hex-6-yl]methyl]-
- CAS:
- 1173239-39-8
- MF:
- C19H22ClFN4O
- MW:
- 376.86
- Mol File:
- 1173239-39-8.mol
PF 03463275 Chemical Properties
- Melting point:
- 125 °C
- Boiling point:
- 575.8±45.0 °C(Predicted)
- Density
- 1.40±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO: 33.33 mg/mL (88.44 mM)
- pka
- 10.07±0.40(Predicted)
- form
- Solid
- color
- Off-white to light yellow
PF 03463275 Usage And Synthesis
Uses
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].
in vivo
PF-03463275 (1-10 mg/kg; s.c.) attenuates oscillatory potentials (OPs)[2].
| Animal Model: | Male Sprague-Dawley rats[2] |
| Dosage: | 1, 3 and 10 mg/kg |
| Administration: | S.c. |
| Result: | A dose-dependent reduction in the amplitude of oscillatory potentials (OPs) elicited from the dark-adapted rats. |
IC 50
GlyT1
References
[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. DOI:10.1016/j.bmcl.2009.04.035
[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. DOI:10.3109/15569527.2013.833937
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