4-P-PDOT - CAS 620170-78-7
Category: Inhibitor
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Melatonin Receptor
4-P-PDOT is a slelctive antagonist of MT2 melatonin receptor, and luzindole-an antagonist of both membrane receptors, on an oncostatic action of MLT. It displays >300-fold selective for the MT2 (vs MT1) subtype.
≥99% by HPLC
Store in a cool and dry place (or refer to the Certificate of Analysis).
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1.Hormonal control of luminescence from lantern shark (Etmopterus spinax) photophores.
Claes JM;Mallefet J J Exp Biol. 2009 Nov;212(Pt 22):3684-92. doi: 10.1242/jeb.034363.
The velvet belly lantern shark (Etmopterus spinax) emits a blue luminescence from thousands of tiny photophores. In this work, we performed a pharmacological study to determine the physiological control of luminescence from these luminous organs. Isolated photophore-filled skin patches produced light under melatonin (MT) and prolactin (PRL) stimulation in a dose-dependent manner but did not react to classical neurotransmitters. The alpha-melanocyte-stimulating hormone (alpha-MSH) had an inhibitory effect on hormonal-induced luminescence. Because luzindole and 4P-PDOT inhibited MT-induced luminescence, the action of this hormone is likely to be mediated through binding to the MT2 receptor subtype, which probably decreases the intracellular concentration of cyclic AMP (cAMP) because forskolin (a cAMP donor) strongly inhibits the light response to MT. However, PRL seems to achieve its effects via janus kinase 2 (JAK2) after binding to its receptor because a specific JAK2 inhibitor inhibits PRL-induced luminescence. The two stimulating hormones showed different kinetics as well as a seasonal variation of light intensity, which was higher in summer (April) than in winter (December and February).
2.Melatonin slowed the early biochemical progression of hormone-refractory prostate cancer in a patient whose prostate tumor tissue expressed MT1 receptor subtype.
Shiu SY;Law IC;Lau KW;Tam PC;Yip AW;Ng WT J Pineal Res. 2003 Oct;35(3):177-82.
Melatonin inhibited the proliferation of hormone-independent LNCaP prostate cancer cells partly via MT1 receptor activation both in vitro and in nude mice xenograft model. In this study, the melatonin receptor expression in the prostate cancer tissue of a patient with bone metastases and the effect of melatonin on the biochemical progression of hormone-refractory prostate tumor which later developed in the same patient were reported. Saturation and competition 2-[125I]iodomelatonin binding assays were conducted on prostate tumor tissue obtained by transurethral resection of the prostate from the index patient. The receptor subtype identity of melatonin receptor expressed in the cancer tissue was determined by comparison of the rank order of inhibition constants (Ki) of various melatonergic ligands and the affinity of 4-phenyl-2-propionamidotetraline relative to melatonin in inhibiting 2-[125I]iodomelatonin binding to the tumor sample and to human cell lines stably transfected with MT1 or MT2 melatonin receptor subtype. MT1 receptor expression in the cancer tissue was also examined by immunohistochemistry. The surgically castrated patient later developed biochemical relapse of his disease.
3.Signaling mechanisms of melatonin in antiproliferation of hormone-refractory 22Rv1 human prostate cancer cells: implications for prostate cancer chemoprevention.
Tam CW;Mo CW;Yao KM;Shiu SY J Pineal Res. 2007 Mar;42(2):191-202.
There is an unmet clinical demand for safe and effective pharmaceuticals/nutraceuticals for prostate cancer prevention and hormone-refractory prostate cancer treatment. Previous laboratory and human studies of our laboratory demonstrated an association between the antiproliferative action of melatonin and melatonin MT(1) receptor expression in prostate cancer. The aim of this study was to determine, using a pharmacological approach, the signaling mechanisms of melatonin in hormone-refractory 22Rv1 human prostate cancer cell antiproliferation. Both immunoreactive MT(1) and MT(2) subtypes of G protein-coupled melatonin receptor were expressed in 22Rv1 cells. Melatonin inhibited, concentration dependently, cell proliferation, upregulated p27(Kip1) gene transcription and protein expression, and downregulated activated androgen signaling in 22Rv1 cells. While the effects of melatonin were mimicked by 2-iodomelatonin, a high-affinity nonselective MT(1) and MT(2) receptor agonist, melatonin effects were blocked by luzindole, a nonselective MT(1) and MT(2) receptor antagonist, but were unaffected by 4-phenyl-2-propionamidotetraline, a selective MT(2) receptor antagonist. Importantly, we discovered that the antiproliferative effect of melatonin exerted via MT(1) receptor on p27(Kip1) gene and protein upregulation is mediated by a novel signaling mechanism involving co-activation of protein kinase C (PKC) and PKA in parallel.
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CAS 620170-78-7 4-P-PDOT

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