Design, synthesis and structure–affinity relationships of aryloxyanilide derivatives as novel peripheral benzodiazepine receptor ligands

T Okubo, R Yoshikawa, S Chaki, S Okuyama… - Bioorganic & medicinal …, 2004 - Elsevier
Since the peripheral benzodiazepine receptor (PBR) has been primarily found as a high-affinity
binding site for diazepam in rat kidney, numerous studies of it have been performed. …

Neuropharmacological profile of peripheral benzodiazepine receptor agonists, DAA1097 and DAA1106

…, S Chaki, R Yoshikawa, S Ogawa, Y Suzuki, T Okubo… - Life sciences, 1999 - Elsevier
Receptor binding and behavioral profiles of N-(4-chloro-2-phenoxyphenyl)-N-(2-isopropoxybenzyl)acetamide
(DAA1097) and N-(2,5-dimethoxybenzyl)-N-(5-fluoro-2-phenoxyphenyl)…

Development of a method for evaluating drug-likeness and ease of synthesis using a data set in which compounds are assigned scores based on chemists' intuition

…, S Yamanobe, H Kakinuma, T Okubo… - Journal of chemical …, 2003 - ACS Publications
The concept of drug-likeness, an important characteristic for any compound in a screening
library, is nevertheless difficult to pin down. Based on our belief that this concept is implicit …

Anxiolytic-like and antidepressant-like activities of MCL0129 (1-[(S)-2-(4-fluorophenyl)-2-(4-isopropylpiperadin-1-yl) ethyl]-4-[4-(2-methoxynaphthalen-1-yl) butyl] …

…, T Funakoshi, Y Suzuki, S Suetake, T Okubo… - … of Pharmacology and …, 2003 - ASPET
We investigated the effects of a novel melanocortin-4 (MC4) receptor antagonist,1-[(S)-2-(4-fluorophenyl)-2-(4-isopropylpiperadin-1-yl)ethyl]-4-[4-(2-methoxynaphthalen-1-yl)butyl]…

Receptor binding, behavioral, and electrophysiological profiles of nonpeptide corticotropin-releasing factor subtype 1 receptor antagonists CRA1000 and CRA1001

…, SI Ogawa, A Nakazato, T Kumagai, T Okubo… - … of Pharmacology and …, 1999 - ASPET
Receptor binding, behavioral, and electrophysiological profiles of 2-[N-(2-methylthio-4-isopropylphenyl)-N-ethylamino]-4-[4-(3-fluorophenyl)-1,2,3,6-tetrahydropyridin-1-yl)-6-…

Binding characteristics of [3H] DAA1106, a novel and selective ligand for peripheral benzodiazepine receptors

…, R Yoshikawa, S Okuyama, T Okubo… - European journal of …, 1999 - Elsevier
Here, we investigated the binding characteristics of [ 3 H ]N-(2,5-dimethoxybenzyl)-N-(5-fluoro-2-phenoxyphenyl)acetamide
([ 3 H ]DAA1106), a potent and selective ligand for …

Design, synthesis, and structure–activity relationships of novel tetracyclic compounds as peripheral benzodiazepine receptor ligands

T Okubo, R Yoshikawa, S Chaki, S Okuyama… - Bioorganic & medicinal …, 2004 - Elsevier
The peripheral benzodiazepine receptor (PBR) is pharmacologically distinct from the central
benzodiazepine receptor (CBR) and has been identified in a wide range of peripheral …

Melanocortin-4 receptor antagonists for the treatment of depression and anxiety disorders

S Chaki, T Okubo - Current topics in medicinal chemistry, 2007 - ingentaconnect.com
Derived from proopiomelanocortin by proteolytic processing, melanocortins have been
implicated in a wide range of physiological processes. Melanocortins exert their physiological …

Non-monoamine-based approach for the treatment of depression and anxiety disorders

S Chaki, T Okubo, Y Sekiguchi - Recent Patents on CNS Drug …, 2006 - ingentaconnect.com
Although currently prescribed antidepressants with actions mediated through alteration of
monoaminergic transmission have been proven to be useful for the treatment of depressive …

MCL0042: a nonpeptidic MC4 receptor antagonist and serotonin reuptake inhibitor with anxiolytic-and antidepressant-like activity

…, S Ogawa, T Funakoshi, T Shimazaki, T Okubo… - Pharmacology …, 2005 - Elsevier
In the present study, we examined the anxiolytic and antidepressant effects of MCL0042, a
novel compound showing activity in both MC4 receptor antagonism and serotonin transporter …