Involvement of the strychnine-sensitive glycine receptor in the anxiolytic effects of GlyT1 inhibitors on maternal separation-induced ultrasonic vocalization in rat pups

Komatsu, Hiroko; Furuya, Yasubumi; Sawada, Kohei; Asada, Takashi

doi:10.1016/j.ejphar.2014.11.024

Cited by 11 publications

(7 citation statements)

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“…They are playing important role in regulating respiratory rhythm, muscle tone, pain/sensory transmission and convulsion (Harvey et al ., 2004; Reinold et al ., 2005; Eichler et al ., 2008; Manzke et al ., 2010). A recent report has suggested a potential role of the strychnine-sensitive glycine receptor (Komatsu et al ., 2015) in the control of anxiety. In the present study, the intranasal taurine delivery increased the time to induce convulsion caused by strychnine, suggesting taurine may exert anti-anxiety action through the activation of strychnine-sensitive glycine receptors.…”

Section: Discussionmentioning

confidence: 99%

Anxiolytic Action of Taurine via Intranasal Administration in Mice

Jung

Kim

2019

Biomolecules & Therapeutics

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Taurine has a number of beneficial pharmacological actions in the brain such as anxiolytic and neuroprotective actions. We explored to test whether taurine could be transported to the central nervous system through the intranasal route. Following intranasal administration of taurine in mice, elevated plus maze test, activity cage test and rota rod test were carried out to verify taurine’s effect on anxiety. For the characterization of potential mechanism of taurine’s anti-anxiety action, mouse convulsion tests with strychnine, picrotoxin, yohimbine, and isoniazid were employed. A significant increase in the time spent in the open arms was observed when taurine was administered through the nasal route in the elevated plus maze test. In addition, vertical and horizontal activities of mice treated with taurine via intranasal route were considerably diminished. These results support the hypothesis that taurine can be transported to the brain through intranasal route, thereby inducing anti-anxiety activity. Taurine’s anti-anxiety action may be mediated by the strychnine-sensitive glycine receptor as evidenced by the inhibition of strychnine-induced convulsion.

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Section: Discussionmentioning

confidence: 99%

Anxiolytic Action of Taurine via Intranasal Administration in Mice

Jung

Kim

2019

Biomolecules & Therapeutics

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“…Truncating the sulfonamide n-propyl chain to ethyl (30) led to a 5-fold decrease in potency relative to 10, whereas further truncation to methyl (29) led to a more significant diminishment in potency. Introduction of bulkier iso-butyl (31), phenyl (32), or benzyl (33) sulfonamides was not well tolerated and also led to significant losses of potency relative to parent 10.…”

Section: ■ Results and Discussionmentioning

confidence: 99%

“…Compound 22 -((4,4-difluoro-1-(4-(propylsulfonyl)piperazin-1-yl)cyclohexyl)methyl)-4-fluoro-2-methoxy-6-methylbenzamide (23) -6-chloro-N-((1-(4-(methylsulfonyl)piperazin-1-yl)cyclohexyl)methyl)benzamide Hydrochloride (29). Compound 29 was prepared according to a similar procedure described for the synthesis of 10 using methylsulfonyl chloride.…”

Section: N-((44-difluoro-1-(4-(propylsulfonyl)piperazin-1-yl)cyclohementioning

confidence: 99%

“…37 The potency of each compound was assessed in inhibiting the uptake of radiolabeled glycine ( was generated on every plate as a positive control. 29 Plate performances were assessed using a combination of assay window, z' and IC 50 of positive control.…”

Section: Concurrent With This Campaign Sulfonamide Sar Exploration Omentioning

confidence: 99%

“…The results from this campaign revealed very narrow SAR for this region of the scaffold, which is highlighted in Table 2. Truncating the sulfonamide npropyl chain to ethyl (30) led to a 5-fold decrease in potency relative to 10, whereas further truncation to methyl (29) led to a more significant diminishment in potency.…”

mentioning

confidence: 99%

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