A melatonin receptor agonist (Kis = 14

Ramelteon – 10 mg

Brand:
Cayman
CAS:
196597-26-9
Storage:
-20
UN-No:
Non-Hazardous - /

Ramelteon is a melatonin (MT) receptor agonist (Kis = 14, 112, and 23.1 pM for human MT1, human MT2, and chick forebrain receptors, respectively).{42292} It is selective for MT1 and MT2 over MT3 receptors (Ki = 2.65 μM for hamster brain MT3 receptors) as well as a panel of benzodiazepine, dopamine, and opiate receptors, ion channels, transporters, and enzymes when used at a concentration of 10 μM. Ramelteon stimulates cAMP production in CHO cells expressing human MT1 and MT2 receptors (IC50s = 21.2 and 53.4 pM, respectively). In vivo, ramelteon (0.03 and 0.3 mg/kg, p.o.) shortens latency to sleep onset and increases duration of sleep in free-moving crab-eating macaques.{42293} It also accelerates reentrainment of circadian rhythm in rats, shifting running wheel activity back to the dark period 2.4 and 3 days more quickly than vehicle-treated animals following an eight-hour phase shift in the light-dark cycle when administered at 0.1 and 1 mg/kg, respectively, with no effect on learinng and memory in the Morris water maze and delayed match-to-position tasks.{42294}  

 

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Description

A melatonin receptor agonist (Kis = 14, 112, and 23.1 pM for human MT1, human MT2, and chick forebrain receptors, respectively); selective for MT1 and MT2 over MT3 receptors (Ki = 2.65 μM for hamster brain MT3 receptors) as well as a panel of benzodiazepine, dopamine, and opiate receptors, ion channels, transporters, and enzymes when used at a concentration of 10 μM; stimulates cAMP production in CHO cells expressing human MT1 and MT2 receptors (IC50s = 21.2 and 53.4 pM, respectively); shortens latency to sleep onset and increases duration of sleep in free moving crab-eating macaques at 0.03 and 0.3 mg/kg; accelerates reentrainment of circadian rhythm in rats at 0.1 and 1 mg/kg,

Formal name: N-[2-[(8S)-1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-yl]ethyl]-propanamide

Synonyms:  TAK-375

Molecular weight: 259.3

CAS: 196597-26-9

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Neuroscience|Behavioral Neuroscience|Learning & Memory||Research Area|Neuroscience|Behavioral Neuroscience|Sleep & Biological Rhythms

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