HTS065M - ChemiSCREEN™ MT1 Melatonin Receptor Membrane Preparation

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    Melatonin (5-methoxy-acetyltryptamine) is a vertebrate hormone synthesized and secreted in a circadian manner with high levels occurring at night. Melatonin has been implicated in photoperiod regulation of various neural and endocrine processes, including seasonal reproduction, body weight, metabolism, and coat color (Masana and Dubocovich, 2001). In mammals, the melatonin rhythm is generated by an endogenous circadian clock in the suprachiasmatic nucleus (SCN) of the hypothalamus, which is entrained by the light/dark cycle to the 24h day. Melatonin may be effective in synchronizing disturbed circadian rhythms in humans, and there is considerable interest in melatonin’s potential for treatment of disordered circadian rhythms in jet-lag, shift work, blindness and in delayed/advanced sleep phase syndromes (Hagan and Oakley, 1995). The two mammalian melatonin receptor subtypes, MT1 and MT2, are G-protein coupled receptors which signal through inhibition of cyclic AMP synthesis (Dubocovich et al., 2000). In addition, MT1 is involved in regulation of proliferation of human breast cancer cells (Ram et al., 2002; Collins et al., 2003). MT1 membrane preparations are crude membrane preparations made from our proprietary stable recombinant cell lines to ensure high-level of GPCR surface expression; thus, they are ideal HTS tools for screening of MT1 interactions with its ligands. The membrane preparations exhibit a Kd of 1.7 nM for [125I]-Iodomelatonin. With 0.5 nM [125I]-Iodomelatonin, 5 mg/well MT1 Membrane Prep typically yields greater than 15-fold signal-to-background ratio.

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    Item Unit of Measure: EA
    Quantity: 200 units
    Storage: On receipt of material store at -70°C. Unopened reagent is stable for a minimum of 1 year from date of shipment when stored at recommended storage temperature. Avoid repeat freeze/thaw cycles. For maximum recovery of product, centrifuge original vial
    Applications: Radioligand Binding Assay, GTPγS Binding
    Species: Full-length human MTNR1A cDNA encoding MT1 (Accession Number: NM_005958)
    Host Cell: Chem-1, an adherent mammalian cell line without any endogenous MT1 expression.
    Reference 1: 1. A. Collins, L. Yuan, T.L. Kiefer, Q. Cheng, L. Lai, S.M. Hill (2003). Overexpression of the MT1 melatonin receptor in MCF-7 human breast cancer cells inhibits mammary tumor formation in nude mice. Cancer Letters. 189: 49-57.
    Reference 2: 2. Dubocovich ML, Cardinali DP, Delagrange P, Krause DN, Strosberg AD, Sudgen D, Yocca FD (2000). Melatonin receptors. The IUPHAR Compendium of Receptor Characterization and Classification. 2nd Edition, D. Girdlestone, Ed. (IUPHAR Media, London).
    Reference 3: 3. Hagan RM and Oakley NR (1995). Melatonin comes of age Trends Pharmacol Sci. 16: 81-3.
    Reference 4: 4. Masana MI and Dubocovich ML (2001). Melatonin receptor signaling: finding the path through the dark. Sci STKE. 107: PE39.
    Reference 5: 5. P.T. Ram, J. Dai, L. Yuan, C. Dong, T.L. Kiefer, L. Lai, S.M. Hill (2002) Involvement of the MT1 melationin receptor in human breast cancer. Cancer Letters 179: 141-150.