1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. GABA Receptor
  3. PF-06372865

PF-06372865 

Cat. No.: HY-120874
Handling Instructions

PF-06372865 is an orally active, α2/α3/α5 subtype-selective GABAA positive allosteric modulator (PAM). PF-06372865 is a high affinity ligand at GABAA receptors containing α1/α2/α3/α5 subunits (Kis of 2.9 nM, 21 nM, 134 nM for α2, α1 PAM, α2 PAM, respectively), with low affinity for α4/α6 subunits. PF-06372865 has the potential for epilepsy.

For research use only. We do not sell to patients.

PF-06372865 Chemical Structure

PF-06372865 Chemical Structure

CAS No. : 1614245-70-3

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Description

PF-06372865 is an orally active, α2/α3/α5 subtype-selective GABAA positive allosteric modulator (PAM). PF-06372865 is a high affinity ligand at GABAA receptors containing α1/α2/α3/α5 subunits (Kis of 2.9 nM, 21 nM, 134 nM for α2, α1 PAM, α2 PAM, respectively), with low affinity for α4/α6 subunits. PF-06372865 has the potential for epilepsy[1].

IC50 & Target

Ki: 2.9 nM (α2), 21 nM (α1 PAM) and 134 nM (α2 PAM)[1]

In Vitro

PF-06372865 has Ki values of 0.18 nM, 2.9 nM, 1.1 nM, 18 nM for human GABAA α1β3γ2, α2β2γ2, α3β3γ2, α5β2γ2 and 0.34 nM, 4.58 nM for rat GABAA α1β3γ2, α2β2γ2[1].

In Vivo

PF-06372865 (3, 10 mg/kg; orally) significantly increases the paw withdrawal threshold (PWT) in chronic constriction injury (CCI) animals[1].
PF-06372865 (0.3, 3, 10 mg/kg for mouse and 1, 3, 10 mg/kg for rat; orally) exhibits efficacy in two models of epilepsy, PTZ induced seizures (mouse), and amygdala kindling (rat) [1].
PF-06372865 (0.1, 0.32, 1, 3.2 and 10 mg/kg; orally) has anxiolytic activity at 3.2 and 10 mg/kg in elevated plus maze (male C57Bl/6 mice) [1].
PF-06372865 has a T1/2 of 1.1 hours, a CLp of 22 mL/min/kg, and a Vss of 2.1 L/kg for rats[1].
PF-06372865 has a T1/2 of 0.9 hours, a CLp of 29 mL/min/kg, and a Vss of 3.4 L/kg for dogs[1].

Animal Model: Chronic constriction injury (CCI) model (male Wistar rats)[1]
Dosage: 3, 10 mg/kg
Administration: Orally
Result: Significantly increased paw withdrawal latency.
Molecular Weight

440.49

Formula

C₂₂H₂₁FN₄O₃S

CAS No.

1614245-70-3

SMILES

CCN1C2=NN=CC(C(C=C3)=CC(C(C=CC([S](CC)(=O)=O)=C4)=C4OC)=C3F)=C2N=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

References
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Keywords:

PF-06372865PF06372865PF 06372865GABA ReceptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid Receptororallyα2α3α5GABAAPAMα1α4α6subunitsepilepsyα1β3γ2α2β2γ2α3β3γ2α5β2γ2Inhibitorinhibitorinhibit

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