PF-4211 

PF-4211 is a selective non-catechol D1R agonist. PF-4211 activates adenylate cyclase by binding to D1R, thereby increasing intracellular cAMP levels. PF-4211 can be used in research related to Parkinson's disease and schizophrenia^[1][2].

PF-4211 (Compound 6) acts as a partial agonist at the hD1 receptor in HEK293 cells overexpressing hD1, with a geometric mean functional EC₅₀ of 2.293 μM and 37% maximal effect relative to dopamine^[1].
PF-4211 binds directly to the hD1 receptor with a geometric mean binding K_i of 2.2 μM^[1].
PF-4211 (11-point concentration response curve with half-log increments; 30 min) acts as a partial agonist at human D1 receptors expressed in HEK293 cells, with an EC₅₀ of 2519 nM and a maximum efficacy of 42% relative to dopamine^[2].
PF-4211 (10^-10-10^-4 M; 30 min) induces a dose-dependent increase in cAMP in hD1R-expressing HEK293 cells, with a lower maximum efficacy than dopamine and optimized non-catechol analogs^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

291.30

C₁₇H₁₃N₃O₂

2292115-41-2

CN1N=CC=C1C2=CC=C(C=C2)OC3=NC=CC4=C3C=CO4

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Davoren JE, et al. Discovery and Lead Optimization of Atropisomer D1 Agonists with Reduced Desensitization. Journal of medicinal chemistry. 2018 Dec 27;61(24):11384-11397.  [Content Brief]

  [2]. Gray DL, et al. Impaired β-arrestin recruitment and reduced desensitization by non-catechol agonists of the D1 dopamine receptor. Nature communications. 2018 Feb 14;9(1):674.  [Content Brief]