PTAC oxalate

PTAC oxalate is a selective muscarinic receptor ligand. PTAC oxalate is an partial agonist of M2 and M4 but antagonist of M1, M3, and M5 (Ki values of 0.2-2.8 nM for hM1-5 in CHO cells). PTAC oxalate alleviates the mechanical allodynia on the neuropathic pain and has antidepression effects[1][2].

Signaling Pathways >> Neuronal Signaling >> mAChR

Signaling Pathways >> GPCR/G Protein >> mAChR

Research Areas >> Neurological Disease

mAChR1:0.6 nM (Ki)

mAChR2:2.8 nM (Ki)

mAChR3:0.2 nM (Ki)

mAChR4:0.2 nM (Ki)

mAChR5:0.8 nM (Ki)

PTAC oxalate (0.01, 0.05 mg/kg; 腹腔给药) 在 0.05 mg/kg 时可以减轻机械异常性疼痛。PTAC oxalate 在 0.05 mg/kg 剂量下可缩短假手术组和神经损伤组小鼠的不动时间，但在 0.01 mg/kg 剂量下则不会[2]。 Animal Model: Mouse model of neuropathic pain[2] Dosage: 0.01, 0.05 mg/kg Administration: IP Result: The mechanical allodynia was alleviated with 0.05 mg/kg. At 0.05 mg/kg increased the paw withdrawal thresholds (PWTs) of the nerve-injury groups injected at day 4 after nerve injury. At 0.01 mg/kg had no effect on the PWTs in the sham and nerve-injury groups injected at day 14 after nerve injury.

[1]. F P Bymaster, et al. Unexpected antipsychotic-like activity with the muscarinic receptor ligand (5R,6R)6-(3-propylthio-1,2,5-thiadiazol-4-yl)-1-azabicyclo[3.2.1]octane. Eur J Pharmacol. 1998 Sep 4;356(2-3):109-19.  

[2]. (5R,6R)6-(3-Propylthio-1,2,5-thiadiazol-4-yl)-1-azabicyclo[3.2.1] Octane on a Mouse Model of Neuropathic Pain. Anesth Analg. 2017 Apr;124(4):1330-1338.