201939-40-4

201939-40-4 structure
201939-40-4 structure
  • Name: PTAC oxalate
  • Chemical Name: (5R,6R)-6-[4-(Propylsulfanyl)-1,2,5-thiadiazol-3-yl]-1-azabicyclo[3.2.1]octane ethanedioate (1:1)
  • CAS Number: 201939-40-4
  • Molecular Formula: C14H21N3O4S2
  • Molecular Weight: 359.464
  • Catalog: Signaling Pathways GPCR/G Protein mAChR
  • Create Date: 2018-06-27 12:23:03
  • Modify Date: 2024-02-09 17:52:20
  • 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].

Name (5R,6R)-6-[4-(Propylsulfanyl)-1,2,5-thiadiazol-3-yl]-1-azabicyclo[3.2.1]octane ethanedioate (1:1)
Synonyms 1-Azabicyclo[3.2.1]octane, 6-[4-(propylthio)-1,2,5-thiadiazol-3-yl]-, (5R,6R)-, ethanedioate (1:1)
(5R,6R)-6-[4-(Propylsulfanyl)-1,2,5-thiadiazol-3-yl]-1-azabicyclo[3.2.1]octane ethanedioate (1:1)
Description 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].
Related Catalog
Target

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)

In Vivo 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.
References

[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.  

Molecular Formula C14H21N3O4S2
Molecular Weight 359.464
Exact Mass 359.097351