Milameline hydroiodide  (Synonyms: CI 979 hydroiodide; RU 35926 hydroiodide)

Milameline (CI 979; RU35926) hydroiodide is a nonselective, partical and orally active muscarinic receptor agonist that improves cognition. Milameline hydroiodide has equal affinity for different subtypes of human muscarinic receptors with IC₅₀ of 1.3 µM for M1-, 1.1 µM for M2-, 1.5 µM for M3-, and 1.9 µM for M4-muscarinic receptors. Milameline hydroiodide has a higher affinity for sites [³H]CMD (IC₅₀ = 20 nM), than [³H]QNB, (IC₅₀ = 3059 nM). Milameline hydroiodide produces both central and peripheral cholinergic effects and reverses the cognitive deficits induced by Scopolamine (HY-N0296). Milameline hydroiodide can be used for the study of Alzheimer’s Disease^[1].

Milameline hydroiodide 可增加转染了人类 M1 或 M3 受体的 CHO 细胞中可溶性 APP (sAPP) 的分泌^[1]。

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

Milameline (0.2 mg/kg (大鼠), 口服, 或 0.01 mg/kg (猴), 肌注, 单次给药) hydroiodide 在大鼠中产生中枢效应 (体温过低) 并在猴中产生中枢胆碱能效应 (脑电图 (EEG) 中新皮层觉醒度增加)^[1]。
Milameline (0.02- > 0.1 mg/kg, 口服) 在低剂量 (0.02-0.1 mg/kg) hydroiodide 下有效逆转东莨菪碱诱导的大鼠工作记忆损伤，但在高剂量下 (> 0.1 mg/kg) 该效应减弱^[1]。
Milameline hydroiodide 增加大鼠脑血流量，并且其在大脑中的分布与胆碱能系统富集的区域一致^[1]。

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

282.12

C₈H₁₅IN₂O

固体

Yellow to orange

Room temperature in continental US; may vary elsewhere.

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

• [1]. Heidrich, A., and M. Rösler. "Milameline hydrochloride: nonselective, partial muscarinic receptor agonist for the treatment of Alzheimer's disease?." CNS Drug Reviews (1999).