344579-12-0Relevant academic research and scientific papers
Synthesis of diphenylmethyl analogues and their affinity for the melanocortin-4 receptor and the serotonin transporter
Nozawa, Dai,Okubo, Taketoshi,Ishii, Takaaki,Chaki, Shigeyuki,Okuyama, Shigeru,Nakazato, Atsuro
, p. 1044 - 1050 (2008/02/13)
While examining antagonists of the melanocortin-4 receptor (MC4 receptor), we found that compound 12b, containing a diphenylmethyl moiety, had a relatively high affinity for the MC4 receptor. When diphenylmethyl analogues were further examined, compounds
PHARMACOLOGICAL CHAPERONES FOR TREATING OBESITY
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Page/Page column 5/18, (2008/06/13)
The invention relates to methods of enhancing normal melanocortin-4 receptor (MC4R) activity, and to enhancing activity of an MC4R having a mutation which affects protein folding and/or processing of the MC4R. The invention provides a method of treating an individual having a condition in which increased activity of an MC4R at the cell surface would be beneficial, for example in obesity, by administering an effective amount of a pharmacological chaperone for the MC4R. The invention provides MC4R pharmacological chaperones which enhance the activity of MC4R. The invention further provides a method of screening to identify pharmacological chaperones which enhance folding of an MC4R in the endoplasmic reticulum (ER), in order to enhance the activity of the MC4R at the cell surface.
Remedial agent for anxiety neurosis or depression and piperazine derivative
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, (2008/06/13)
There are provided a therapeutic preparation for anxiety neurosis or depression which comprises a MC4 receptor antagonist as an effective ingredient; and a piperazine derivative represented by Formula [1]: [wherein Ar1 is a phenyl gr
Structure-activity relationship of (1-Aryl-2-piperazinylethyl) piperazines: Antagonists for the AGRP/melanocortin receptor binding
Arasasingham, Premilla N.,Fotsch, Christopher,Ouyang, Xiaohu,Norman, Mark H.,Kelly, Michael G.,Stark, Kevin L.,Karbon, Bill,Hale, Clarence,Baumgartner, James W.,Zambrano, Martha,Cheetham, Janet,Tamayo, Nuria A.
, p. 9 - 11 (2007/10/03)
Agouti-related protein (AGRP) is an endogenous antagonist of the melanocortin action. In the hypothalamus, melanocortin peptide agonists act as satiety-inducing factors that mediate their action through the melanocortin-4 receptor (MC4R) whereas AGRP is a
