Synthesis of diphenylmethyl analogues and their affinity for the melanocortin-4 receptor and the serotonin transporter

…, T Ishii, S Chaki, S Okuyama, A Nakazato

Index: Nozawa, Dai; Okubo, Taketoshi; Ishii, Takaaki; Chaki, Shigeyuki; Okuyama, Shigeru; Nakazato, Atsuro Chemical and Pharmaceutical Bulletin, 2007 , vol. 55, # 7 p. 1044 - 1050

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Abstract

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 12c and 18 were also found to exhibit a high affinity for the MC4 receptor (IC 50= 46.7 nM and 33.2 nM, respectively). Furthermore, compound 12c was also found to show a high affinity for the ...