Milameline  (Synonyms: CI-979; RU35926)

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

Milameline increases soluble APP (sAPP) secretion in CHO cells transfected with human M1 or M3 receptors^[1].

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

Milameline (0.2 mg/kg (rat), p.o., or 0.01 mg/kg (monkey), i.m., single dose) produces central effects (hypothermia) in rats and central cholinergic effects in monkeys (increased neocortical arousal in the electroencephalogram (EEG))^[1].
Milameline (0.02- > 0.1 mg/kg, p.o.) effectively reverses Scopolamine (HY-N0296)-induced working memory impairment in rats at low doses (0.02-0.1 mg/kg), but the effect is reduced at high doses (> 0.1 mg/kg)^[1].
Milameline increases cerebral blood flow in rats, and its distribution in the brain is consistent with the areas where the cholinergic system is enriched^[1].

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

154.21

C₈H₁₄N₂O

139886-32-1

CO/N=C/C1=CCCN(C)C1

Room temperature in continental US; may vary elsewhere.

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