PF-06256142 is a potent, selective, CNS-penetrant and orally active agonist of the D1 receptor, with an EC50 and Ki of 33 nM and 12 nM, respectively. PF-06256142 has the potential for the research of schizophrenia and Parkinson's disease[1].
PF-06256142 is a potent, selective, CNS-penetrant and orally active agonist of the D1 receptor, with an EC50 and Ki of 33 nM and 12 nM, respectively. PF-06256142 has the potential for the research of schizophrenia and Parkinson's disease[1].
PF-06256142 exhibits IC50 values of 10 μM)[1].
PF-06256142 exhibits high oral bioavailability (rat 85%) following oral administration (rat 5 mg/kg)[1].PF-06256142 exhibits terminal elimination half-life (rat 2.3 h) following intravenous administration (rat 5.0 mg/kg)[1].
PF-06256142 exhibits high oral bioavailability (rat 85%) following oral administration (rat 5 mg/kg)[1].
PF-06256142 exhibits terminal elimination half-life (rat 2.3 h) following intravenous administration (rat 5.0 mg/kg)[1].
| Animal Model: | Rat[1] |
| Dosage: | 5.0 mg/kg for i.v.; 5 mg/kg for oral (Pharmacokinetic Analysis) |
| Administration: | Intravenous injection and oral administration |
| Result: | Oral bioavailability (85%), T1/2 (2.3 h). |
Human D1 Receptor: 33 nM (EC50)
[1]. Davoren JE, et al. Discovery and Lead Optimization of Atropisomer D1 Agonists with Reduced Desensitization. J Med Chem. 2018 Nov 15.
