Akito Yasuhara
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Explore the profile of Akito Yasuhara including associated specialties, affiliations and a list of published articles.
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14
Citations
183
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Recent Articles
1.
Yamamoto S, Ohta H, Abe K, Kambe D, Tsukiyama N, Kawakita Y, et al.
Chem Pharm Bull (Tokyo)
. 2016 Nov;
64(11):1630-1640.
PMID: 27803474
We previously identified 3-chloro-N-{(S)-[3-(1-ethyl-1H-pyrazol-4-yl)phenyl][(2S)-piperidine-2-yl]methyl}-4-(trifluoromethyl)pyridine-2-carboxamide (5, TP0439150) as a potent and orally available glycine transporter 1 (GlyT1) inhibitor. In this article, we describe our identification of 1-methyl-N-(propan-2-yl)-N-({2-[4-(trifluoromethoxy)phenyl]pyridin-4-yl}methyl)-1H-imidazole-4-carboxamide (7n) as a structurally...
2.
Hikichi H, Hiyoshi T, Marumo T, Tomishima Y, Kaku A, Iida I, et al.
J Pharmacol Sci
. 2015 Apr;
127(3):352-61.
PMID: 25837934
Glutamatergic dysfunction has been implicated in psychiatric disorders such as schizophrenia. The stimulation of metabotropic glutamate (mGlu) 2 receptor has been shown to be effective in a number of animal...
3.
Hiyoshi T, Marumo T, Hikichi H, Tomishima Y, Urabe H, Tamita T, et al.
J Pharmacol Exp Ther
. 2014 Oct;
351(3):642-53.
PMID: 25277141
Excess glutamatergic neurotransmission has been implicated in the pathophysiology of schizophrenia, and the activation of metabotropic glutamate 2 (mGlu2) receptor may exert antipsychotic effects by normalizing glutamate transmission. In the...
4.
Yasuhara A, Chaki S
Open Med Chem J
. 2010 Dec;
4:20-36.
PMID: 21160908
Metabotropic glutamate receptors (mGlu receptors) have emerged as new therapeutic targets for psychiatric disorders, such as schizophrenia, depression and anxiety with their regulatory roles in glutamatergic transmissions. To date, several...
5.
Sakagami K, Yasuhara A, Chaki S, Yoshikawa R, Kawakita Y, Saito A, et al.
Bioorg Med Chem
. 2008 Mar;
16(8):4359-66.
PMID: 18348906
In this paper, we describe the synthesis of (+)-(1R( *),2R( *))-2-[(1S( *))-1-amino-1-carboxy-2-(9H-xanthen-9-yl)-ethyl]-1-fluorocyclopropanecarboxylic acid (+)-16a, a compound, that is, fluorinated at the alpha position of the carboxylic acid in the cyclopropane...
6.
Yasuhara A, Nakamura M, Sakagami K, Shimazaki T, Yoshikawa R, Chaki S, et al.
Bioorg Med Chem
. 2006 Feb;
14(12):4193-207.
PMID: 16487713
3-(3,4-Dichlorobenzyloxy)-2-amino-6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid 5 (MGS0039) is a highly selective and potent group II metabotropic glutamate receptor (mGluR) antagonist (antagonist activities for mGluR2; IC50=20.0 nM, mGluR3; IC50=24.0 nM) and is detected in...
7.
Yasuhara A, Sakagami K, Yoshikawa R, Chaki S, Nakamura M, Nakazato A
Bioorg Med Chem
. 2006 Jan;
14(10):3405-20.
PMID: 16431115
Chemical modification of the bicyclo[3.1.0]hexane ring C-3 position led to the discovery of 3-alkoxy-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid, 3-benzylthio-, and 3-benzylamino-2-amino-6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives, metabotropic glutamate receptor 2 (mGluR2) antagonists. In particular, 3-(3,4-dichlorobenzyloxy)-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid...
8.
Nakamura M, Kawakita Y, Yasuhara A, Fukasawa Y, Yoshida K, Sakagami K, et al.
Drug Metab Dispos
. 2005 Dec;
34(3):369-74.
PMID: 16326817
MGS0039 (3-(3,4-dichlorobenzyloxy)-2-amino-6-fluorobicyclo-[3.1.0]hexane-2,6-dicarboxylic acid) has been identified as a potent and selective antagonist for metabotropic glutamate receptors. However, the oral bioavailability of MGS0039 is 10.9% in rats, due to low absorption....
9.
Kawashima N, Karasawa J, Shimazaki T, Chaki S, Okuyama S, Yasuhara A, et al.
Neurosci Lett
. 2005 Mar;
378(3):131-4.
PMID: 15781145
Glutamatergic abnormalities play roles in several psychiatric disorders. Glutamate acts at two classes of receptors, ionotropic and metabotropic glutamate receptors (mGluR), the latter is classified into three group, based on...
10.
Nakazato A, Sakagami K, Yasuhara A, Ohta H, Yoshikawa R, Itoh M, et al.
J Med Chem
. 2004 Aug;
47(18):4570-87.
PMID: 15317467
Novel group II metabotropic glutamate receptor (mGluR) antagonists, 3-alkoxy-2-amino-6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives 11 and 12, were discovered by the incorporation of a hydroxy or alkoxyl group onto the C-3 portion of...