Chicago sky blue 6B, a vesicular glutamate transporters inhibitor, attenuates methamphetamine-induced hyperactivity and behavioral sensitization in mice

He, Zongsheng; Yan, Lingdi; Zheng, Yongchang; Dong, Zhaoqi; Dong, Honglin; Gong, Ze‐Hui

doi:10.1016/j.bbr.2012.11.003

Cited by 18 publications

(11 citation statements)

References 22 publications

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“…Indeed, sulfasalazine, rosiglitazone, and zafirlukast, are more selective for NTCP, while chicago sky blue 6B and TRIAC were as effective for ASBT as for NTCP. Chicago sky blue 6B was also identified as an inhibitor for vesicular glutamate transporters (VGLUTs), completely unrelated transporters, further demonstrating its low specificity 35 . Although species-specific differences have been found for drugs bosentan 36 and rosuvastatin 37 , only minor differences in drug specificity between mouse and human NTCP were found for sulfasalazine, rosiglitazone, and zafirlukast.…”

Section: Discussionmentioning

confidence: 99%

Reduced hepatitis B and D viral entry using clinically applied drugs as novel inhibitors of the bile acid transporter NTCP

Donkers¹,

Zehnder

Westen

et al. 2017

Sci Rep

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The sodium taurocholate co-transporting polypeptide (NTCP, SLC10A1) is the main hepatic transporter of conjugated bile acids, and the entry receptor for hepatitis B virus (HBV) and hepatitis delta virus (HDV). Myrcludex B, a synthetic peptide mimicking the NTCP-binding domain of HBV, effectively blocks HBV and HDV infection. In addition, Myrcludex B inhibits NTCP-mediated bile acid uptake, suggesting that also other NTCP inhibitors could potentially be a novel treatment of HBV/HDV infection. This study aims to identify clinically-applied compounds intervening with NTCP-mediated bile acid transport and HBV/HDV infection. 1280 FDA/EMA-approved drugs were screened to identify compounds that reduce uptake of taurocholic acid and lower Myrcludex B-binding in U2OS cells stably expressing human NTCP. HBV/HDV viral entry inhibition was studied in HepaRG cells. The four most potent inhibitors of human NTCP were rosiglitazone (IC50 5.1 µM), zafirlukast (IC50 6.5 µM), TRIAC (IC50 6.9 µM), and sulfasalazine (IC50 9.6 µM). Chicago sky blue 6B (IC50 7.1 µM) inhibited both NTCP and ASBT, a distinct though related bile acid transporter. Rosiglitazone, zafirlukast, TRIAC, sulfasalazine, and chicago sky blue 6B reduced HBV/HDV infection in HepaRG cells in a dose-dependent manner. Five out of 1280 clinically approved drugs were identified that inhibit NTCP-mediated bile acid uptake and HBV/HDV infection in vitro.

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Section: Discussionmentioning

confidence: 99%

Reduced hepatitis B and D viral entry using clinically applied drugs as novel inhibitors of the bile acid transporter NTCP

Donkers¹,

Zehnder

Westen

et al. 2017

Sci Rep

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“…Exogenous VGLUT inhibitors, such as Chicago sky blue 6B (CSB6B), have been shown to inhibit the loading of glutamate into synaptic vesicles upon intracerebroventricular application [287], resulting in the inhibition of the methamphetamine induced hyperlocomotion and behavioural sensitization [288]. Interestingly, in an older study, Beirith et al [289] evaluated the role of a systemically delivered CSB6B in animals receiving an intraplantar injection of glutamate and found that the use of the VGLUT inhibitor results in a considerable reduction of glutamate-induced nociception.…”

Section: Could Vgluts Become Pharmacological Targets For the Contrmentioning

confidence: 99%

VGLUTs in Peripheral Neurons and the Spinal Cord: Time for a Review

Brumovsky

2013

ISRN Neurology

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Vesicular glutamate transporters (VGLUTs) are key molecules for the incorporation of glutamate in synaptic vesicles across the nervous system, and since their discovery in the early 1990s, research on these transporters has been intense and productive. This review will focus on several aspects of VGLUTs research on neurons in the periphery and the spinal cord. Firstly, it will begin with a historical account on the evolution of the morphological analysis of glutamatergic systems and the pivotal role played by the discovery of VGLUTs. Secondly, and in order to provide an appropriate framework, there will be a synthetic description of the neuroanatomy and neurochemistry of peripheral neurons and the spinal cord. This will be followed by a succinct description of the current knowledge on the expression of VGLUTs in peripheral sensory and autonomic neurons and neurons in the spinal cord. Finally, this review will address the modulation of VGLUTs expression after nerve and tissue insult, their physiological relevance in relation to sensation, pain, and neuroprotection, and their potential pharmacological usefulness.

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“…We validated these results using a different echocardiography system (Supplemental Figure 1, A and B). Previous studies showed that CSB has several biological effects (37,(42)(43)(44)(45)(46). Therefore, we examined the mice for adverse side effects at the end of the in vivo experiment, 21 days after MI.…”

Section: Resultsmentioning

confidence: 99%

“…CSB was shown to have several biological targets, including VGLUT (46), MIF (38), CaMKP (62), RAD51 (39), ubiquitin (40), and the Prion protein (63). In vivo, CSB was shown to attenuate methamphetamine-induced hyperac- tivity (46), to have antinociceptive effects (44), to attenuate secondary injuries in the spinal cord (45), and to modulate feeding in broilers (42).…”

Section: Discussionmentioning

confidence: 99%

The small molecule Chicago Sky Blue promotes heart repair following myocardial infarction in mice

Yifa¹,

Weisinger²,

Bassat³

et al. 2019

JCI Insight

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Chicago sky blue 6B, a vesicular glutamate transporters inhibitor, attenuates methamphetamine-induced hyperactivity and behavioral sensitization in mice

Cited by 18 publications

References 22 publications

Reduced hepatitis B and D viral entry using clinically applied drugs as novel inhibitors of the bile acid transporter NTCP

Reduced hepatitis B and D viral entry using clinically applied drugs as novel inhibitors of the bile acid transporter NTCP

VGLUTs in Peripheral Neurons and the Spinal Cord: Time for a Review

The small molecule Chicago Sky Blue promotes heart repair following myocardial infarction in mice

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