MCHR
Melanin-concentrating hormone (MCH) is a cyclic peptide, isolated and sequenced originally from salmon pituitary. The rat MCH is 19 amino acids long, two amino acids longer than its salmon counterpart, and is identical to the human MCH, the sequence of which was deduced by cloning. In rodents, MCH is prominently expressed in the perikarya of the lateral hypothalamus and the zona incerta, and projects broadly throughout the central nervous system(CNS). MCHR exhibits several different structures. First, under its original name of somatostatin-like receptor (SLC)-1 or GPR24, it has been described as a 402 amino acid-long human GPCR that was discovered by genomic cloning and delineated by an assigned start codon. In addition to the SLC-1 form of the MCHR, two other MCHR cDNAs were found in a human embryonic brain cDNA library. MCH may function as a neurotransmitter/neuromodulator in a broad array of behavioral responses. MCHR receptor is in fact SLC-1, an orphan G-protein-coupled receptor (GPCR). The SLC-1 GPCR was discovered as an expressed sequence tag exhibiting about 40% homology in its hydrophobic domains to the five somatostatin receptors.SLC-1 reactivity was monitored in three different ways: (1) by intracellular changes in calcium influxes upon coexpression of a Gaq/i3 chimeric protein engineered to force SLC-1 coupling to the phospholipase C pathway; (2) by inhibition of intracellular cAMP accumulation; and (3) by G-protein-gated inwardly rectifying potassium channels (GIRKs) in Xenopus oocytes injected with SLC-1 cRNAs.
References
1.Saito Y, et al. Trends Endocrinol Metab. 2000;11(8):299–303.
References
1.Saito Y, et al. Trends Endocrinol Metab. 2000;11(8):299–303.
GPCR/G Protein
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LHR(1)
LPA Receptor(19)
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MCHR(8)
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MCHR
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GW-803430
catalog no : M33378
cas no: 515141-51-2
GW-803430 (GW-3430) is an orally active and selective melanin-concentrating hormone receptor 1 (MCH R1) antagonist used in the study of obesity. -
TC-MCH 7c
catalog no : M33138
cas no: 864756-35-4
TC-MCH 7c is an oral, selectable and blood-brain barrier penetrating MCH1R antagonist with IC50 performance of 5.6 nM against hMCH1R, and TC-MCH 7c is a phenylpyridone derivative with MCH1R Ki of 3.4 nM against human. In mice, MCH1R Ki was 3.0 nM. -
[Ala17]-MCH
catalog no : M30637
cas no: 359784-84-2
Potent melanin-concentrating hormone (MCH) receptor agonist (EC50 values are 17 and 54 nM at MCH1 and MCH2 receptors respectively). Displays some selectivity towards MCH1 over MCH2 (Ki values are 0.16 and 34 nM respectively). -
MCH (human, mouse, rat)
catalog no : M22355
cas no: 128315-56-0
Potent endogenous agonist at melanin-concentration hormone (MCH) receptors (IC50 values are 0.3 and 1.5 nM and EC50 values are 3.9 and 0.1 nM at MCH1 and MCH2 receptors respectively). Increases food intake in vivo. -
SNAP 94847 hydrochloride
catalog no : M21140
cas no: 1781934-47-1
SNAP 94847 hydrochloride is a melanin-concentrating hormonereceptor1 (MCHR1) antagonist(Ki= 2.2 nM).