M871 is a type 2-selective galanin receptor antagonist (GalR2/GalR1 Ki = 13.1/410 nM by competitive binding against 0.1 nM porcine galanin using membranes from CHO expressing respective human receptors; GalR2/GalR1 Ki = 2.5/1.1 nM in case of rat galanin) that potently blocks 10 nM rat galanin-induced inositol phosphate production in human GalR2-expressing CHO cells (by 100% with 0.1, 1 or 10 nM M871). M871 is widely employed in cultures (0.1 nM-2.5 μM) and in mice and rats in vivo via ip., brain region- or other site-specific injections.
Selective galanin receptor type 2 (GalR2) antagonist with in vitro and in vivo efficacy.
Biochimica et biophysica acta. Molecular and cell biology of lipids, 1863(10), 1228-1236 (2018-10-12)
Spexin (SPX, NPQ) is a novel peptide involved in the regulation of energy metabolism. SPX inhibits food intake and reduces body weight. In obese humans, SPX is the most down-regulated gene in fat. Therefore, SPX might be involved in the
Status epilepticus (SE) in rats, along with chronic epilepsy, leads to the development of behavioral impairments resembling depressive disorder and/or attention deficit/hyperactivity disorder (ADHD), thus reflecting respective comorbidities in epilepsy patients. Suppressed neurotransmitter tone in the raphe nucleus (RN)-prefrontal cortex
In this study, we investigated temporal changes in galanin receptor type 2 (GalR2) expression in NF200-, galanin-, neuropeptide Y (NPY)-, and neuronal nitric oxide synthase (nNOS)-like immunoreactive (LI) dorsal root ganglion (DRG) neurons after median nerve chronic constriction injury (CCI)
M871-A Novel Peptide Antagonist Selectively Recognizing the Galanin Receptor Type 2
Sollenberg UE, Lundstrom L, Bartfai T, Langel U
International Journal of Peptide Research and Therapeutics, 12, 115-119 (2006)
Galanin is a neuropeptide distributed in human and rat brain regions that are involved with emotional regulation, such as the dorsal raphe nucleus (DRN). Galanin effects in the DRN are mediated by GAL1 and GAL2 receptors. Intracerebral infusion of a
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