146422-58-4

146422-58-4 structure
146422-58-4 structure
  • Name: CDD0102
  • Chemical Name: 3-ethyl-5-(1,4,5,6-tetrahydropyrimidin-6-yl)-1,2,4-oxadiazole
  • CAS Number: 146422-58-4
  • Molecular Formula: C8H12N4O
  • Molecular Weight: 180.20700
  • Catalog: Signaling Pathways GPCR/G Protein mAChR
  • Create Date: 2017-07-17 06:47:53
  • Modify Date: 2024-01-15 07:00:48
  • CDD0102 is a potent M1 Muscarinic receptor agonist.

Name 3-ethyl-5-(1,4,5,6-tetrahydropyrimidin-6-yl)-1,2,4-oxadiazole
Synonyms cdd-102a
unii-9f064nj81d
cdd 0102
CDD0102
Description CDD0102 is a potent M1 Muscarinic receptor agonist.
Related Catalog
Target

mAChR[1]

In Vitro CDD0102 (CDD-0102) is an efficacious muscarinic agonist in cell lines expressing M1 receptors. CDD0102 displays much lower activity at M3 and M5 receptors[1].
In Vivo After i.p. injections, CDD0102 (CDD-0102) crosses the blood-brain barrier (BBB) in a dose-dependent manner. In toxicological studies, the LD50 of CDD0102 is 190 mg/kg following i.p. injections and greater than 1,000 mg/kg following oral administration. In follow-up studies, after oral administration at a dose of 10 mg/kg, CDD0102 fully reverses memory deficits associated with IgG-192 saporin administration. Again, no side effects are observed at this dose[1].
Cell Assay A9 L cells expressing muscarinic receptor subtypes are cultured. Biochemical studies examine the ability of compounds (e.g., CDD0102, 0.01 nM, 0.1 nM, 1 nM, 10 nM, 100 nM, 1 μM, 10 μM, 100 μM and 1 mM) to stimulate relevant biochemical responses through muscarinic receptors expressed in A9 Lcells. Assays of PI metabolism provides a measure of in vitro activity associated with M1, M3, and M5 receptor activation, while inhibition of adenylyl cyclase activity determined efficacy at M2 and M4 receptors[1].
Animal Admin Mice[1] Young, male CF-1 mice are administered CDD0102 or xanomeline by either p.o. or i.p. injection with doses from 1 to 1,000 mg/kg by each route, and monitored for 24 h. Animals are observed daily for 1 wk for appearance of delayed toxicity. A second set of animals is treated with a narrow range of concentrations based on the preliminary studies to determine the LD50.
References

[1]. Messer WS Jr. The utility of muscarinic agonists in the treatment of Alzheimer's disease. J Mol Neurosci. 2002 Aug-Oct;19(1-2):187-93.

Molecular Formula C8H12N4O
Molecular Weight 180.20700
Exact Mass 180.10100
PSA 63.31000
LogP 0.45910
Storage condition 2-8℃