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
ACAT(3)
Angiotensin Receptor(27)
Antibacterial(545)
Bombesin Receptor(13)
Bradykinin Receptor(23)
Calcium Channel(197)
cAMP(16)
Cannabinoid Receptor(88)
CaSR(18)
CGRP Receptor(18)
Chemokine Receptor(104)
Cholecystokinin Receptor(24)
CRF Receptor(15)
Dopamine Receptor(182)
Endothelin Receptor(28)
FFAR(5)
Galanin Receptor(1)
GHSR(20)
Glucagon Receptor(51)
GPCR19(9)
GPR119(3)
Hedgehog (Hh)(35)
Histamine Receptor(139)
Imidazoline Receptor(1)
Leukotriene Receptor(15)
LHR(1)
LPA Receptor(19)
Lysophospholipid Receptor(13)
mAChR(25)
MCHR(8)
Melanocortin Receptor(28)
Melatonin Receptor(7)
Motilin Receptor(4)
Neurokinin Receptor(43)
Neuropeptide Y Receptor(44)
Neurotensin Receptor(11)
Orexin Receptor(16)
Other Targets(3)
OXTR(2)
P2Y Receptor(14)
PAR(28)
Platelet-activating Factor Receptor(2)
Prostaglandin Receptor(79)
PTH Receptor(1)
S1P Receptor(35)
SGLT(26)
Somatostatin Receptor(16)
Urotensin Receptor(4)
Vasopressin Receptor(20)
MCHR
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GW-803430
产品货号 : M33378
cas no: 515141-51-2
GW-803430 (GW-3430) 是一种有效的选择性黑色素浓缩激素受体 1 (MCH R1) 拮抗剂,pIC50 为 9.3。GW-803430 在肥胖动物模型中具有口服活性。 -
TC-MCH 7c
产品货号 : M33138
cas no: 864756-35-4
TC-MCH 7c 是一种苯基吡啶酮衍生物,一种口服有效的,选择性的且可穿透血脑屏障的 MCH1R 拮抗剂,对 hMCH1R 的 IC50 为 5.6 nM。TC-MCH 7c 对人和小鼠 MCH1R 的 Ki 分别为 3.4 nM 和 3.0 nM。 -
[Ala17]-MCH
产品货号 : 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)
产品货号 : M22355
cas no: 128315-56-0
黑色素浓缩激素 (MCH) 受体的有效内源性激动剂(MCH1 和 MCH2 受体的 IC50 值分别为 0.3 和 1.5 nM,EC50 值分别为 3.9 和 0.1 nM)。增加体内食物摄入量。 -
SNAP 94847 hydrochloride
产品货号 : M21140
cas no: 1781934-47-1
SNAP 94847 Hydrochloride 是一种黑色素浓缩激素受体 1 (MCHR1) 拮抗剂 (Ki= 2.2 nM)。