DH 97 - CAS 343263-95-6
Category: Inhibitor
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Melatonin Receptor
DH 97 is a selective MEL-1B-R (melatonin receptor) antagonist.
Brife Description:
MEL-1B-R antagonist
White Solid
DH-97; DH 97; DH97; N-[2-(2-benzyl-1H-indol-3-yl)ethyl]pentanamide
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1.Melatonin-induced calcium signaling in clusters of human and rat duodenal enterocytes.
Sjöblom M;Säfsten B;Flemström G Am J Physiol Gastrointest Liver Physiol. 2003 Jun;284(6):G1034-44. Epub 2003 Feb 12.
The amount of melatonin present in enterochromaffin cells in the alimentary tract is much higher than that in the central nervous system, and melatonin acting at MT(2) receptors mediates neural stimulation of mucosal HCO(3)(-) secretion in duodenum in vivo. We have examined effects of melatonin and receptor ligands on intracellular free calcium concentration ([Ca(2+)](i)) signaling in human and rat duodenal enterocytes. Clusters of interconnecting enterocytes (10-50 cells) were isolated by mild digestion (collagenase/dispase) of human duodenal biopsies or rat duodenal mucosa loaded with fura-2 AM and attached to the bottom of a temperature-controlled perfusion chamber. Clusters provided viable preparations and respond to stimuli as a syncytium. Melatonin and melatonin receptor agonists 2-iodo-N-butanoyl-5-methoxytryptamine and 2-iodomelatonin (1.0-100 nM) increased enterocyte [Ca(2+)](i), EC(50) of melatonin being 17.0 +/- 2.6 nM. The MT(2) receptor antagonists luzindole and N-pentanoyl-2-benzyltryptamine abolished the [Ca(2+)](i) responses. The muscarinic antagonist atropine (1.0 microM) was without effect on basal [Ca(2+)](i) and did not affect the response to melatonin. In the main type of response, [Ca(2+)](i) spiked rapidly and returned to basal values within 4-6 min.
2.Melatonin enhances the hypoxic response of rat carotid body chemoreceptor.
Chen Y;Tjong YW;Ip SF;Tipoe GL;Fung ML J Pineal Res. 2005 Apr;38(3):157-63.
Melatonin attenuates carotid chemoreceptor response to hypercapnic acidosis and may contribute to the effect of circadian rhythms on the chemoreflex. The purpose of this study was to test the hypothesis that melatonin modulates rat carotid chemoreceptor response to hypoxia. To examine the effect of melatonin on the hypoxic response of the chemosensitive cells, cytosolic calcium ([Ca2+]i) was measured by spectrofluorometry in fura-2-loaded type-I (glomus) cells dissociated from rat carotid bodies. Melatonin (0.01-10 nm) did not change the resting Ca2+]i level of the glomus cells but it concentration-dependently increased peak Ca2+]i response to cyanide or deoxygenated buffer. An agonist of melatonin receptors, iodomelatonin also enhanced the Ca2+]i response to hypoxia. The melatonin-induced enhancement of the Ca2+]i response was abolished by pretreatment with nonselective mt1/MT2 antagonist, luzindole, and by MT2 antagonists, 4-phenyl-2-propionamidotetraline or DH97. These findings suggest that melatonin receptors in the glomus cells mediate the effect of melatonin on the chemoreceptor response to hypoxia. In addition, melatonin increased the carotid afferent response to hypoxia in unitary activities recorded from the sinus nerve in isolated carotid bodies superfused with bicarbonate-buffer saline.
3.Comparison of the structure-activity relationships of melatonin receptor agonists and antagonists: lengthening the N-acyl side-chain has differing effects on potency on Xenopus melanophores.
Teh MT;Sugden D Naunyn Schmiedebergs Arch Pharmacol. 1998 Nov;358(5):522-8.
The potency and affinity of two series of melatonin receptor ligands were examined using the pigment aggregation response in a clonal line of Xenopus laevis melanophores and radioligand binding assays on native receptors in chicken brain, recombinant human mt1 and MT2 and Xenopus laevis mel1c receptor subtypes. One series was based on melatonin and had a methoxy group at the 5-position of the indole ring, while the other was based on luzindole and lacked this substituent but did have a 2-benzyl moiety; the N-acyl group of each series of analogues was varied from one to five carbon atoms. All analogues in the melatonin series were full agonists in melanophores (pEC50 7.76-10.24), while all compounds in the luzindole series were competitive melatonin antagonists (pA2 5.47-6.60). With the agonist series, increasing the N-acyl side-chain from one to three carbon atoms was well tolerated in both the functional and binding assays, but further lengthening of the side-chain progressively and dramatically reduced potency and affinity. In contrast, for the antagonist series neither potency nor binding affinity changed substantially with the length of the N-acyl chain, except at the recombinant MT2 subtype where two of the analogues had a lower affinity.
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CAS 343263-95-6 DH 97

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