PD 102807|cas:23062-91-1|西域试剂

PD 102807,98.40%

产品编号：Bellancom-107646| CAS NO：23062-91-1| 分子式：C₂₃H₂₄N₂O₄| 分子量：392.45

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-107646		￥6500.00	杭州北京（现货）

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PD 102807

产品介绍

PD 102807 是一种 M4 毒蕈碱受体拮抗剂，IC₅₀ 为 90.7 nM。PD 102807 抑制 M1、M2、M3、M5 毒蕈碱受体，IC₅₀ 分别为 6558.7、3440.7、950.0 和 7411.7 nM。具有抗运动障碍作用。

生物活性

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.

体外研究

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.
PD 102807, a novel M4 selective antagonist, counteracts the M4 receptor-induced stimulation of [³⁵S]-GTPγS binding to membrane G proteins with a pK_B of 7.40, a value which is 63-, 33- and 10-fold higher than those display at M1 (pK_B=5.60), M2 (pK_B=5.88) and M3 (pK_B=6.39) receptor subtypes, respectively.
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.

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

体内研究

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

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

Animal Model:	Male Sprague-Dawley rats
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.

体内研究

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

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

Animal Model:	Male Sprague-Dawley rats
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.