A New Fungal Metabolite, Sch 202596, with Inhibitory Activity in the Galanin Receptor GALR1 Assay

Chen, Min; Mierzwa, Ronald; Truumees, Imbi; King, Arthur; Sapidou, Elpida; Barrabee, Ellen B.; Terracciano, Joseph; Patel, Mahesh; Gullo, Vincent P.; Burrier, Robert E.; Das, Pradip R.; Mittelman, Stanley; Puar, Mohindar S.

doi:10.1016/s0040-4039(97)01385-3

Cited by 27 publications

(6 citation statements)

References 3 publications

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“…(ref. 33 ). However, none of these compounds has shown a favorable pharmacological profile in terms of metabolic stability, high receptor affinity and selectivity, as well as ability to cross blood-brain barrier 4 .…”

Section: Discussionmentioning

confidence: 99%

Detection of galanin receptors in the spinal cord in experimental autoimmune encephalomyelitis

Michaličková¹,

Kramáriková²,

Öztürk³

et al. 2023

Biomed Pap Med Fac Univ Palacky Olomouc Czech Repub

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Aims. The neuropeptide galanin is a widely distributed neurotransmitter/neuromodulator that regulates a variety of physiological processes and also participates in the regulation of stress responses. The aims of the present study were to investigate the expression of galanin receptors (GalR1, GalR2, GalR3) in the spinal cords in a murine model of multiple sclerosis, experimental autoimmune encephalomyelitis (EAE) using qPCR analysis and to determine GalR1 cellular localization (oligodendrocytes, microglia, astrocytes, ependymal cells, and endothelial cells in the capillaries) by immunohistochemistry. Methods. Twelve samples from the EAE group and 14 samples from the control group were analyzed. Spinal cords samples were obtained at the peak of the EAE disease. Results. The GalR1 mRNA level was significantly decreased in the EAE mice compared with the controls (P=0.016), whereas the mRNA levels of GalR2 and GalR3 were not significantly different for the EAE and the control mice. No significant correlations were found between the severity of the EAE disease and the mRNA levels of GalR1, GalR2 and GalR3. Immunochemical detection of the GalR1 revealed its expression in the ependymal and endothelial cells. Additionally, a weak GalR1 immunoreactivity was occasionally detected in the oligodendrocytes. Conclusion.This study provides additional evidence of galanin involvement in EAE pathophysiology, but this has to be further investigated.

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Section: Discussionmentioning

confidence: 99%

Detection of galanin receptors in the spinal cord in experimental autoimmune encephalomyelitis

Michaličková¹,

Kramáriková²,

Öztürk³

et al. 2023

Biomed Pap Med Fac Univ Palacky Olomouc Czech Repub

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“…This ligand was described to have a modest (µM) affinity to GalR1 in vitro [129]. Thereafter, various dithiepin analogues with an affinity to bind GalR1 have been described.…”

Section: Non-peptide Ligandsmentioning

confidence: 99%

“…Spirocoumaranone 1700* -- [129] RWJ-57408 (2,3-Dihydro-2-(4-methylphenyl)-1,4-dithiepine-1,1,4,4-tetroxide) 190* 30,000* - [130] Galnon 7-((9-Fluorenylmethoxycarbonyl)cyclohexylalanyllysyl) amino-4-methylcoumarin 11,700 34,100 - [132] Galmic 34,200 > 100,000 - [133] SNAP 37889 (1-Phenyl-3-[[3-(trifluoromethyl)phenyl]imino]-1H-indol-2-one) > 10,000 > 10,000 17.4 [150] SNAP 398299 (1-[3-(2-(Pyrrolidin-1-yl)ethoxy)phenyl]-3-(3-(trifluoromethyl)phenylimino) indolin-2-one) > 1000 > 1000 5.3 [150] Displacement was performed on the rat galanin receptor unless marked (h)-human. *Presented as IC 50 values.…”

Section: Sch 202596mentioning

confidence: 99%

Galanin receptors as a potential target for neurological disease

Freimann

Kurrikoff

Langel

2015

Expert Opinion on Therapeutic Targets

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“…culture found in an abandoned uranium mine in Tuolemene County California, was found to have a modest affinity to GalR1 in vitro (Chu et al, 1997). Sch 202596 was characterized as a molecule with a spirocoumaranone skeleton and has only partly been synthesized so far (Katoh et al, 2002).…”

Section: Non-peptide Ligandsmentioning

confidence: 99%

Galanin Receptors and Ligands

Webling¹,

Runesson²,

Bartfai³

et al. 2012

Front. Endocrin.

116

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The neuropeptide galanin was first discovered 30 years ago. Today, the galanin family consists of galanin, galanin-like peptide (GALP), galanin-message associated peptide (GMAP), and alarin and this family has been shown to be involved in a wide variety of biological and pathological functions. The effect is mediated through three GPCR subtypes, GalR1-3. The limited number of specific ligands to the galanin receptor subtypes has hindered the understanding of the individual effects of each receptor subtype. This review aims to summarize the current data of the importance of the galanin receptor subtypes and receptor subtype specific agonists and antagonists and their involvement in different biological and pathological functions.

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A New Fungal Metabolite, Sch 202596, with Inhibitory Activity in the Galanin Receptor GALR1 Assay

Cited by 27 publications

References 3 publications

Detection of galanin receptors in the spinal cord in experimental autoimmune encephalomyelitis

Detection of galanin receptors in the spinal cord in experimental autoimmune encephalomyelitis

Galanin receptors as a potential target for neurological disease

Galanin Receptors and Ligands

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