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In the late s Solvay Pharmaceuticals discontinued the
2024-07-12

In the late ‘90s, Solvay Pharmaceuticals discontinued the Phase 2 development of a promising potent and highly selective A1AR antagonist based on the pyrrolopyrimidine scaffold, SLV320 [43] (2, Chart 1, also named derenofylline; Ki hA1AR = 1 nM), for the treatment of acute heart failure [24]. In the
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Our previous work fails to show
2024-07-11

Our previous work fails to show any maternal effect with blockade of 5-HT2A receptor, as acute and repeated treatment of MDL100907 does not alter maternal behavior at the behaviorally active doses (Chen et al., 2014). In the present study, MDL100907 pretreatment attenuated the maternal disruptive ef
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shows the complexes resulting from interaction of the propos
2024-07-11

shows the complexes resulting from interaction of the proposed anion receptors with the anions F, Cl, NO, and SO. No imaginary frequency was observed for the optimized complexes indicating the complexes are in potential minima and they are not transition state structures. summarizes the calculated
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Quetiapine Fumarate sale Antioxidative enzymes such as SOD a
2024-07-11

Antioxidative enzymes such as SOD and CAT play prominent roles in protecting against oxidative stress and extending food freshness due to their ability in scavenging active oxygen species for maintaining cell membrane integrity. Evidence shows that activities of SOD and CAT are positively affected b
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NVP-CGM097 It is reported that calpain plays a
2024-07-11

It is reported that calpain-2 plays a critical role in BDNF-induced signaling and memory formation, and knockdown of calpain-2, but not calpain-1, completely suppresses BDNF-induced pathway activation and protein translation (Briz et al., 2013). BDNF prevents neuronal apoptosis or death (Ferrer et a
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br Consequences of central apelin APJ modulation
2024-07-11

Consequences of central apelin/APJ modulation Regarding extra-hypothalamic actions, recent data demonstrate that the central apelin/APJ system could be a potential new target for the regulation of memory (Han et al., 2014). Then, intracerebroventricular (icv) apelin administration in mice impairs
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This progressive behaviour is summarized in Fig which depict
2024-07-11

This progressive behaviour is summarized in Fig. 4, which depicts the variation in convexity of the obtained cut-off patterns for the series of six antioxidants. The form and degree of convexity of the obtained cut-off curves should in principle correlate with the AOs hydrophobicities, and therefor
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PHA-680632 br Materials and methods br Results
2024-07-11

Materials and methods Results and discussion Conclusion The preparation of acrylic nanoparticles as aminosugar carriers could not be achieved by direct functionalization of poly(t-butyl acrylate) particles with saccharide groups. A four-step procedure starting from a protected derivative of
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PF is orally bioavailable and has appropriate pharmacokineti
2024-07-11

PF-06409577 is orally bioavailable and has appropriate pharmacokinetic properties for use in rodents, allowing us to evaluate its impact on lipid and cholesterol biosynthesis in vivo (Cameron et al., 2016). PF-06409577 lowered the incorporation of 14C-acetate into hepatic lipids in vivo in a dose de
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Hepatic inflammation and fibrosis are hallmarks
2024-07-11

Hepatic Gadodiamide and fibrosis are hallmarks of the NASH phenotype and are thought to occur in a subset of patients with NAFLD. While it is hypothesized that therapeutic lowering of hepatic lipids will be sufficient to improve hepatic fibrosis and inflammation secondarily, this remains controversi
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Perhaps the first evidence of AMPKs
2024-07-11

Perhaps the first evidence of AMPKs therapeutic ability in DM1 came from Thomas Cooper’s laboratory where they demonstrated that insulin-independent glucose uptake was unaffected in human DM1 muscle methylphenidate hcl australia treated with MET, an AMPK activator and first-line therapy for type 2
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Scutellaria moniliorrhiza Komarov Labiatae is a perennial
2024-07-11

Scutellaria moniliorrhiza Komarov (Labiatae) is a perennial herb and mainly distributed in Jilin province, China. In traditional Chinese medicine, the whole plants have been used to clear away heat-evil, expel superficial evils, eliminate stasis and reduce edema (He et al., 2012). In previous phytoc
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Curcumin is able to upregulate the protein level of NGF
2024-07-10

Curcumin is able to upregulate the protein level of NGF through cannabinoid receptor CB1, where the activation of Akt pathway probably plays an important part in the CB1-mediated signal transmission [9,10]. This finding suggested that the protection of curcumin in spinal motor neurons of SNI rats is
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The subdivision of HT receptors started in the s
2024-07-10

The subdivision of 5-HT receptors started in the 1950s by Gaddum and colleagues, when they realised that in the guinea pig ileum, the effects of 5-HT could be blocked in part by morphine (M), and in part by dibenzyline (D). Gaddum and Picarelli proposed two receptor classes, 5-HT M and 5-HT D (1957)
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br A Rs which were cloned and
2024-07-10

A3Rs, which were cloned and then pharmacologically identified in the early 1990s, are expressed in multiple organs and peripheral tissues including Pentostatin involved in inflammatory responses (Gessi et al., 2008, Borea et al., 2014). While low levels are expressed in the CNS, A3R agonists produ
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