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It appears that different agonists for GPR activate
2022-09-29
It appears that different agonists for GPR55 activate different signalling pathways [25]. GPR55 activation through LPI has been shown to trigger ERK 1/2 phosphorylation 22, 23, 25, 33. Conversely, endogenous cannabinoid compounds AEA and 2-AG have been shown to have no effect on ERK 1/2 signalling 2
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br Discussion Agonist and antagonist action at
2022-09-28
Discussion Agonist and antagonist action at the GluN1/GluN3 Irinotecan is known to be complex [4], [10]. Recombinant GluN1/GluN3 receptors produce only small excitatory currents in response to glycine, likely because of a combination of activation via GluN3 and desensitization via GluN1 [2], [3]
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br Results and discussion br Conclusion In conclusion our pr
2022-09-28
Results and discussion Conclusion In conclusion, our present results indicated that l-glutamate treatment could induce resistant to B. cinerea in postharvest tomatoes. The control effect was probably associated with up-regulating the glutamate receptor-like genes, PR genes and the accumulation
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br Author contribution br Declaration of interest br Acknowl
2022-09-28
Author contribution Declaration of interest Acknowledgements This work was supported by National Natural Science Foundation of China (Grants 81473093) and State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica (SIMM1601ZZ-02). Introduction Diabetes represents a majo
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Ning et al showed that LPC appeared to increase
2022-09-28
Ning et al. showed that LPC 18:1 appeared to increase insulin release through both GPR119-dependent and -independent mechanisms (Ning et al., 2008). In our study, we have shown that not only GPR119 but also GPR40 and GPR55 participate in LPC-stimulated insulin secretion (Fig. 4, Fig. 5) and target p
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br Materials and methods br Results Analysis of the post
2022-09-28
Materials and methods Results Analysis of the post-mortem human prefrontal cortex by western blotting indicated that GLAST expression was increased 1.6-fold in the extracts of alcoholic brains relative to controls (Fig. 1A and B). To resolve the distinct sub-pools of GLAST within our samples w
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Despite potent biological actions the
2022-09-28
Despite potent biological actions, the native hormone undergoes degradation by the enzyme dipeptidylpeptidase-IV (DPP-IV) [17] and is rapidly cleared from the bloodstream by renal filtration [18]. One such approach to prolong the biological half-life of GIP is through conjugation with a polyethylene
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Exposure of human and animals to MPTP
2022-09-28
Exposure of human and animals to MPTP can reproduce all the characteristic motor and non-motor signs of PD, in addition to mimicking the same responses and side effects to drugs used to treat PD [37], [38]. Anatomically, intoxication with MPTP induces the same selective loss of substantia nigra DA n
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Methoxyflavone and methoxyflavanone Fig both act as
2022-09-27
6-Methoxyflavone and 6-methoxyflavanone (Fig. 2) both act as flumazenil-insensitive positive allosteric modulators of GABA responses at human recombinant α1β2γ2L and α2β2γ2L GABAA receptors. However, unlike 6-methoxyflavone, 6-methoxyflavanone was relatively inactive at α1β2 GABAA receptors. Both fl
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br Acknowledgement This work was supported by
2022-09-27
Acknowledgement This work was supported by National Science Foundation (21475047, 21705051, 21874048), the Science and Technology Planning Project of Guangdong Province (2016B030303010), the Program for the Top Young Innovative Talents of Guangdong Province (2016TQ03N305) and the Foundation for H
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A relatively independent review of
2022-09-27
A relatively independent review of the history of the discovery of GABA (and L-glutamate) as neurotransmitters in the CNS can be found in ‘When and why amino acids?’ in the in 2010 by Kresimir Krnjevic , who spent a post-doc in Canberra in 1956–1958. Introduction The insect RDL GABA receptor is
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The highest metabolic stability observed for compound
2022-09-27
The highest metabolic stability observed for compound 4k (EC50=0.41μM corresponding to 218ng/mL) among the four selected frontrunner candidates was the principal decisive point in nominating this compounds for pharmacokinetic characterization in mice at the dosage of 10mg/kg (administered intravenou
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The highest metabolic stability observed for compound
2022-09-27
The highest metabolic stability observed for compound 4k (EC50=0.41μM corresponding to 218ng/mL) among the four selected frontrunner candidates was the principal decisive point in nominating this compounds for pharmacokinetic characterization in mice at the dosage of 10mg/kg (administered intravenou
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br Acknowledgments This work was supported by the National I
2022-09-22
Acknowledgments This work was supported by the National Institutes of Health (R01 A1084898) to M.V. Williams and M.E. Ariza. Introduction Female pattern hair loss (FPHL) has emerged as the preferred term for androgenetic alopecia (AGA) in women due to the uncertain relationship between androg
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After the synthesis of methylsulfonyl or tetrazole surrogate
2022-09-22
After the synthesis of methylsulfonyl or tetrazole surrogate derivatives, compounds synthesized by introducing hydrogen, fluoro, and methyl groups into the head group of GPR119 agonists were synthesized. Compounds – were synthesized by reacting hydroxybenzaldehyde with fluorine, hydrogen, or a methy
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