Identification and characterization of a selective radioligand for melanin-concentrating hormone 1-receptor (MCH1R).
We have developed and characterized [(35)S]4a as a potent and selective radioligand for melanin-concentrating hormone 1-receptor (MCH1R). Compound [(35)S]4a showed appreciable specific signals in brain slices prepared from wild-type mice but not from MCH1R deficient mice, confirming the specificity and utility of [(35)S]4a as a selective MCH1R radioligand for ex vivo receptor occupancy assays.
Ito
Masahiko
M
Department of Metabolic Disorder, Tsukuba Research Institute, BANYU Pharmaceutical Co., Ltd, Okubo, Ibaraki, Japan. masahiko_ito2@merck.com
Sakamoto
Toshihiro
T
Suzuki
Takao
T
Egashira
Shinichiro
S
Moriya
Minoru
M
Ishihara
Akane
A
Iwaasa
Hisashi
H
Matsushita
Hiroko
H
Nakase
Kazuho
K
Wallace
Michael A
MA
Dean
Dennis
D
Sato
Nagaaki
N
Tokita
Shigeru
S
Kanatani
Akio
A
D000595:Amino Acid Sequence; D000818:Animals; D001572:Benzofurans / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D001921:Brain / Q000378:metabolism; D016466:CHO Cells; D006224:Cricetinae; D003412:Cricetulus; D006801:Humans; D007700:Kinetics; D051379:Mice; D018345:Mice, Knockout; D017481:Receptors, Somatostatin / Q000037:antagonists & inhibitors / Q000172:deficiency / Q000378:metabolism*; D013141:Spiro Compounds / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D013449:Sulfonamides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology
D001572:Benzofurans; C103263:MCHR1 protein, human; C491209:Mchr1 protein, mouse; D017481:Receptors, Somatostatin; D013141:Spiro Compounds; D013449:Sulfonamides