2-Pyridinamine, 5-[(2R,5S)-5-methyl-4-propyl-2-morpholinyl]-
2-Pyridinamine, 5-[(2R,5S)-5-methyl-4-propyl-2-morpholinyl]- Basic information
- Product Name:
- 2-Pyridinamine, 5-[(2R,5S)-5-methyl-4-propyl-2-morpholinyl]-
- Synonyms:
-
- 2-Pyridinamine, 5-[(2R,5S)-5-methyl-4-propyl-2-morpholinyl]-
- PF592379,PF 592379
- CAS:
- 710655-15-5
- MF:
- C13H21N3O
- MW:
- 235.32534
- Mol File:
- 710655-15-5.mol
2-Pyridinamine, 5-[(2R,5S)-5-methyl-4-propyl-2-morpholinyl]- Chemical Properties
- Boiling point:
- 377.0±42.0 °C(Predicted)
- Density
- 1.058±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- Soluble in DMSO
- pka
- 7.47±0.40(Predicted)
2-Pyridinamine, 5-[(2R,5S)-5-methyl-4-propyl-2-morpholinyl]- Usage And Synthesis
Uses
PF-592379 is a potent dopamine D3 receptor agonist with an EC50 of 21 nM.
in vivo
PF-592379 is an oral dopamine 3 agonist in rat, and dog. PF-592379 has low-moderate clearance relative to liver blood flow of 6.3 and 8.5 mL/min/kg in dog and 44.8 and 58.2 mL/min/kg in rat. It has high permeability in Caco-2 cells and is completely absorbed in rat and dog pharmacokinetic studies with an oral bioavailability of 28% in both rats and 61 and 87% in the dogs[1].
References
[1] Attkins N, et al. Pharmacokinetics and elucidation of the rates and routes of N-glucuronidation of PF-592379, an oral dopamine 3 agonist in rat, dog, and human. Xenobiotica. 2010 Nov;40(11):730-42. DOI:10.3109/00498254.2010.514961
[2] Wager TT, et al. Dopamine D3/D2 Receptor Antagonist PF-4363467 Attenuates Opioid Drug-Seeking Behavior without Concomitant D2 Side Effects. ACS Chem Neurosci. 2017 Jan 18;8(1):165-177. DOI:10.1021/acschemneuro.6b00297
[3] Collins GT, et al. Lack of abuse potential in a highly selective dopamine D3 agonist, PF-592,379, in drug self-administration and drug discrimination in rats. Behav Pharmacol. 2012 Jun;23(3):280-91. DOI:10.1097/FBP.0b013e3283536d21
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