Formulation: A solid
Formal Name: N-(2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-yl)ethyl)propanamide-d5
Purity: ≥99% deuterated forms (d1-d5)
Formula Markup: C16H16D5NO2
Formula Weight: 264,4
Shelf life (days): 1460
CAS Number: 2699607-24-2
Notes: Ramelteon-d5 is intended for use as an internal standard for the quantification of ramelteon (Item No. 20389) by GC- or LC-MS. 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 learning and memory in the Morris water maze and delayed match-to-position tasks.{42294}
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