8-M-PDOT - CAS 134865-70-6
Category: Inhibitor
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Melatonin Receptor
8-M-PDOT is a melatonin receptor agonist, with 20-fold selective for the MT2 (vs MT1) subtype (pKi = 8.23 and 8.95 at human recombinant MT1 and MT2 receptors respectively).
≥99% by HPLC
White solid
Ethanol to 50 mM; DMSO to 100 mM
Store in a cool and dry place (or refer to the Certificate of Analysis).
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1.Melatonin Suppresses Neuropathic Pain via MT2-Dependent and -Independent Pathways in Dorsal Root Ganglia Neurons of Mice.
Lin JJ;Lin Y;Zhao TZ;Zhang CK;Zhang T;Chen XL;Ding JQ;Chang T;Zhang Z;Sun C;Zhao DD;Zhu JL;Li ZY;Li JL Theranostics. 2017 May 12;7(7):2015-2032. doi: 10.7150/thno.19500. eCollection 2017.
Melatonin (Mel) and its receptors (MT1 and MT2) have a well-documented efficacy in treating different pain conditions. However, the anti-nociceptive effects of Mel and Mel receptors in neuropathic pain (NP) are poorly understood. To elucidate this process, pain behaviors were measured in a dorsal root ganglia (DRG)-friendly sciatic nerve cuffing model. We detected up-regulation of MT2 expression in the DRGs of cuff-implanted mice and its activation by the agonist 8-M-PDOT (8MP). Also, Mel attenuated the mechanical and thermal allodynia induced by cuff implantation. Immunohistochemical analysis demonstrated the expression of MT2 in the DRG neurons, while MT1 was expressed in the satellite cells. In cultured primary neurons, microarray analysis and gene knockdown experiments demonstrated that MT2 activation by 8MP or Mel suppressed calcium signaling pathways via MAPK1, which were blocked by RAR-related orphan receptor alpha (RORα) activation with a high dose of Mel. Furthermore, expression of nitric oxide synthase 1 (NOS1) was down-regulated upon Mel treatment regardless of MT2 or RORα. Application of Mel or 8MP in cuff-implanted models inhibited the activation of peptidergic neurons and neuro-inflammation in the DRGs by down-regulating ;c-fos;, calcitonin gene-related peptide [CGRP], and tumor necrosis factor-1α [TNF-1α] and interleukin-1β [IL-1β].
2.REM sleep deprivation promotes a dopaminergic influence in the striatal MT2 anxiolytic-like effects.
Noseda AC;Targa AD;Rodrigues LS;Aurich MF;Lima MM Sleep Sci. 2016 Jan-Mar;9(1):47-54. doi: 10.1016/j.slsci.2015.10.002. Epub 2015 Nov 10.
The aim of this study was to investigate the possible anxiolytic-like effects of striatal MT2 activation, and its counteraction induced by the selective blockade of this receptor. Furthermore, we analyzed this condition under the paradigm of rapid eye movement (REM) sleep deprivation (REMSD) and the animal model of Parkinson's disease (PD) induced by rotenone. Male Wistar rats were infused with intranigral rotenone (12 μg/μL), and 7 days later were subjected to 24 h of REMSD. Afterwards the rats underwent striatal micro-infusions of selective melatonin MT2 receptor agonist, 8-M-PDOT (10 μg/μL) or selective melatonin MT2 receptor antagonist, 4-P-PDOT (5 μg/μL) or vehicle. Subsequently, the animals were tested in the open-field (OP) and elevated plus maze (EPM) tests. Results indicated that the activation of MT2 receptors produced anxiolytic-like effects. In opposite, the MT2 blockade did not show an anxiogenic-like effect. Besides, REMSD induced anxiolytic-like effects similar to 8-M-PDOT. MT2 activation generated a prevalent locomotor increase compared to MT2 blockade in the context of REMSD. Together, these results suggest a striatal MT2 modulation associated to the REMSD-induced dopaminergic supersensitivity causing a possible dopaminergic influence in the MT2 anxiolytic-like effects in the intranigral rotenone model of PD.
3.MT2-like melatonin receptor modulates amplitude receptor potential in visual cells of crayfish during a 24-hour cycle.
Mendoza-Vargas L;Solís-Chagoyán H;Benítez-King G;Fuentes-Pardo B Comp Biochem Physiol A Mol Integr Physiol. 2009 Dec;154(4):486-92. doi: 10.1016/j.cbpa.2009.07.025. Epub 2009 Aug 8.
Retinular photoreceptors are structures involved in the expression and synchronization of the circadian rhythm of sensitivity to light in crayfish. To determine whether melatonin possesses a differential effect upon the receptor potential (RP) amplitude of retinular photoreceptors circadian time (CT)-dependent, we conducted experiments by means of applying melatonin every 2h during a 24-hour cycle. Melatonin with 100 nM increased RP amplitude during subjective day to a greater degree than during subjective night. To determine whether MT(2) melatonin receptors regulate the melatonin-produced effect, we carried out two experiments, circadian times (CTs) 6 and 18, which included the following: (1) application of the MT(2) receptor selective agonist 8-M-PDOT and antagonist DH97, and (2) the specific binding of [(125)I]-melatonin in eyestalk membranes. The amount of 10 nM of 8-M-PDOT increased RP amplitude in a similar manner to melatonin, and 1 nM DH97 abolished the increase produced by melatonin and 8-M-PDOT. Binding of [(125)I]-melatonin was saturable and specific. Scatchard analysis revealed an affinity constant (K(d)) of 1.1 nM and a total number of binding sites (B(max)) of 6 fmol/mg protein at CT 6, and a K(d) of 1.
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CAS 134865-70-6 8-M-PDOT

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