Synonyms: (1R, 2R)-N-[2- (2,3-Dihydrobenzofuran-4-yl)cyclopropylmethyl]propanamide; BMS-214778; Hetlioz; MA 1; N-[[(1R,2R)-2-(2,3-Dihydro-4-benzofuranyl)cyclopropyl]methyl]propanamide; VEC-162
Molecular Formula: C15H19NO2
Molecular Weight: 245.32
Linear Structural Formula: C15H19NO2
MDL Number: MFCD09033789
Purity: >=98% (HPLC)
Storage: 2-8C
Biochem Physiol Actions: Tasimelteon is a Dual Melatonin Receptor Agonist (DMRA) recently approved (Hetlioz) for the treatment of Non-24-hour sleep-wake disorder, a disorder primarily found in the totally blind, where a lack of normal synchronization between the 24-hour light-dark cycle and the endogenous circadian rhythm causes it to drift out of alignment with conventional sleep-wake schedules. The endogenous rhythm of the circadian pacemaker in the suprachiasmatic nuclei (SCN) is typically slightly longer than 24 h and therefore must be synchronized to the 24-hour day, normally by light, but exogenous melatonin can also phase-shift circadian rhythms. Tasimelteon is a selective agonist for the SCN melatonin receptors MT1 and MT2 with greater affinity for the MT2 receptor thought to be more important in mediating circadian rhythm phase-shifting. EC50 values are 0.75 nM for MT1 and 0.1 nM for MT2 measured by inhibition of forskolin-stimulated cAMP accumulation in NIH-3T3 cells expressing human MT1 and MT2.