• br GLP R expression in the vascular endothelium

  2022-09-01

  

  GLP-1R expression in the vascular endothelium Immunohistochemistry studies utilizing GLP-1R antibodies that have now been demonstrated to be non-specific [46], initially identified GLP-1R protein expression in both mouse mesenteric artery SMCs and heart coronary SMCs [7]. However, evidence for VS

• Inhibitors of the G rdos effect include the

  2022-09-01

  

  Inhibitors of the Gárdos effect include the Ca2+-channel blocker nitrendipine with an IC50 of ∼103nM (Ellory et al., 1992, Ellory et al., 1992); its mode of action is likely to be from direct blockage of K+ flux through the Gárdos channel (Ellory et al., 1992, Ellory et al., 1992), and the peptidic

• Furthermore our results are the

  2022-09-01

  

  Furthermore, our results are the first to demonstrate that the stimulating effect of GALP on AVP release in rats is independent of galanin receptors. The same stimulatory GALP influence on AVP secretion has been also observed in the presence of galantide, an antagonist of Gal receptors in the incuba

• Since we were able to reach low

  2022-09-01

  

  Since we were able to reach low micromolar to sub-micromolar potency in both compound series (6 and 7), we were also keen on assessing the preliminary ADME profile (particularly with respect to plasma and liver microsomal stability) of the most active compounds from these series. As it is evident fr

• Following these discoveries the term

  2022-09-01

  

  Following these discoveries, the term ferroptosis was coined in 2012 [25], to describe this iron-dependent, non-apoptotic form cell death induced by erastin and RSL3. This discovery was accompanied by the development of the first small molecule ferroptosis inhibitor, termed ferrostatin-1, and the de

• br Introduction br Results br Discussion br Experimental br

  2022-09-01

  

  Introduction Results Discussion Experimental Acknowledgment Introduction Endocannabinoids, N-arachidonoylethanolamine (AEA) and 2-arachidonoylglycerol (2-AG) have been found in most mammalian tissues and they stimulate cannabinoid CB1 and CB2 receptor activity thereby modulating se

• In addition to Rabs several

  2022-09-01

  

  In addition to Rabs, several proteins have been shown to interact with Rabphilin3a, for instance the GluN2A subunit of the NMDA receptor, PSD-95 ([56,57] and references therein), Rabaptin-5, α-actinin [16] and SNAP-25 [21,23,41,61]. Only the latter has been reported to participate in the AR. Explori

• Several named antagonist ligands have figured noticeably in

  2022-08-31

  

  Several named antagonist ligands have figured noticeably in preclinical studies, with proved clear ability to release neurotransmitters and having efficacy in preclinical animal models. Consequently, this has encouraged ongoing research on improved agents with potency, selectivity, and better drug-l

• Histamine modulates an attentional state which might

  2022-08-31

  

  Histamine modulates an attentional state, which might affect performances in the object recognition test. Indeed, systemic injection of H3 receptor inverse agonists enhances the attentional state (41). However, the memory recovery in our study is unlikely to be due to the enhanced attentional state.

• br Conclusions and future perspectives br Declarations of

  2022-08-31

  

  Conclusions and future perspectives Declarations of interest Acknowledgements The authors thank Mrs. Kamala Pandey for the help in the preparation of this manuscript. This work was supported by NIH grants R01HL057531 and R01HL062147. Introduction Separation of short exons by long non-co

• As glucagon stimulated hepatic glucose production is a key

  2022-08-29

  

  As glucagon-stimulated hepatic dihydrofolate reductase inhibitor production is a key component of the normal response to hypoglycemia, the potential of a GCGr antagonist to delay or prevent recovery from a hypoglycemic state is a critical safety issue that must be addressed. Studies of the effects

• The usefulness of GIP R antagonism

  2022-08-29

  

  The usefulness of GIP-R antagonism for the treatment of obesity-diabetes has been revealed in numerous studies employing knockout or chemical blockade of GIP-R signalling.*88, 89, *90, 91, 92, 93, 94, 95, 96, *97 For example, sub-chronic daily administration of (Pro3)GIP to ob/ob mice results in sig

• No specific inhibitor of KCC has

  2022-08-29

  

  No specific inhibitor of KCC has progressed to clinical trials, however, although compounds like H74 were shown to specifically target KCC over the related Na+-K+-2Cl− cotransporter (NKCC) (Ellory et al., 1990). This molecule, or its related analogues, represent compounds of promise. Simple Mg suppl

• br Declarations of interest br Acknowledgements This work wa

  2022-08-29

  

  Declarations of interest Acknowledgements This work was supported by the National Natural Science Foundation of China (81673321, 21506099), the State Key Laboratory of Drug Research (SIMM1705KF-13), the Natural Science Foundation of Jiangsu Province (Grant No. BK20151541), and the Jiangsu Syne

• There are limited studies on

  2022-08-26

  

  There are limited studies on antibody responses against HIV-1 integrase antigen. According to previous studies, almost 5 percent of individuals infected with HIV never raise anti-integrase Fosaprepitant (Rikhtegaran Tehrani et al., 2015; Chang et al., 1985). If this rate is identical in individuals

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