1. GPCR/G Protein
    Neuronal Signaling
  2. mAChR
  3. PD 102807

PD 102807 

Cat. No.: HY-107646
Handling Instructions

PD 102807 is a M4 muscarinic receptor antagonist with an IC50 of 90.7 nM. PD 102807 inhibits M1, M2, M3, M5 muscarinic receptor with IC50s of 6558.7, 3440.7, 950.0, and 7411.7 nM, respectively. Antidyskinetic effect.

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

PD 102807 Chemical Structure

PD 102807 Chemical Structure

CAS No. : 23062-91-1

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Description

PD 102807 is a M4 muscarinic receptor antagonist with an IC50 of 90.7 nM. PD 102807 inhibits M1, M2, M3, M5 muscarinic receptor with IC50s of 6558.7, 3440.7, 950.0, and 7411.7 nM, respectively[1]. Antidyskinetic effect.

In Vitro

PD 102807 (example 1) shows selectivity for M4 muscarinic receptor with 72-fold (M1), 38-fold (M2), 10-fold (M3), and 82-fold (M5) more selective compared to the other receptors[1].
PD 102807, a novel M4 selective antagonist, counteracts the M4 receptor-induced stimulation of [35S]-GTPγS binding to membrane G proteins with a pKB of 7.40, a value which is 63-, 33- and 10-fold higher than those display at M1 (pKB=5.60), M2 (pKB=5.88) and M3 (pKB=6.39) receptor subtypes, respectively[2].
PD-102807 is an M4 mAChR preferring antagonist, with 7-28 nM affinity for M4 mAChRs, a 14-36-fold selectivity for M4 over M3 mAChRs, and 76-2600-fold selectivity for M4 over M1, M2 and M5 mAChRs[3].

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

In Vivo

Striatal perfusion of PD-102807 (3 μM) alleviates levodopa-induced dyskinesia (LID) and inhibits nigral GABA and Glu along with striatal Glu release[3].

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

Animal Model: Male Sprague-Dawley rats[3]
Dosage: 3 μM
Administration: Administration:Perfusion started 40 min prior to L-DOPA (6 mg/Kg plus 12 mg/Kg benserazide, s.c.) administration and continued until the end of experiment.
Result: Basal dialysate levels in PD-102807 experiment were 19.19±2.62 nM and 47.77±3.42 nM for GABA and Glu in SNr, respectively, and 41.38±4.25 nM for Glu in striatum.
Reduced global Axial Limb Orolingual (ALO) Abnormal Involuntary Movements (AIM) expression from 70.75±5.64 to 25.38±6.64, significantly attenuating limb, axial and orolingual AIMs at 3 μM.
Inhibited the L-DOPA-induced rise of substantia nigra pars reticulata (SNr) GABA, SNr Glu, and striatal Glu at 3 μM.
Molecular Weight

392.45

Formula

C₂₃H₂₄N₂O₄

CAS No.
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PD 102807
Cat. No.:
HY-107646
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