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CDD0102 (CDD0102A) Sale

(Synonyms: CDD0102A) 目录号 : GC31255

CDD0102 (CDD0102A) 是一种有效的 M1 毒蕈碱受体激动剂。

CDD0102 (CDD0102A) Chemical Structure

Cas No.:146422-58-4

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1mg
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Sample solution is provided at 25 µL, 10mM.

Description

CDD0102 is a potent M1 Muscarinic receptor agonist.

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].

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].

[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.

实验参考方法

Cell experiment:

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 experiment:

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.

Chemical Properties

Cas No. 146422-58-4 SDF
别名 CDD0102A
Canonical SMILES CCC1=NOC(C2CN=CNC2)=N1
分子式 C8H12N4O 分子量 180.21
溶解度 Soluble in DMSO 储存条件 Store at -20°C
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 5.5491 mL 27.7454 mL 55.4908 mL
5 mM 1.1098 mL 5.5491 mL 11.0982 mL
10 mM 0.5549 mL 2.7745 mL 5.5491 mL
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