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GPR agonistic activity was evaluated for
2021-09-11
GPR119 agonistic activity was evaluated for the human GPR119 receptor in a cell-based cAMP assay. The results expressed the potency as EC values and the inherent activity (IA) as percentages which were compared to the test compound with oleoylethanolamide (OEA), an endogenous ligand of GPR119 (defin
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glucose transporter Cichlasoma dimerus as most teleost fish
2021-09-11
Cichlasoma dimerus, as most teleost fish species, present neurons expressing GnRH3 (Pandolfi et al., 2005). As in most glucose transporter species, the neurons expressing GnRH3 are mainly located in the NOR, although few neurons were detected in the olfactory bulb, ventral telencephalon and the POA
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Extending the issue of the species differences
2021-09-11
Extending the issue of the species differences, the role of neuroestradiol in the preovulatory GnRH/LH surge might be specific to primates or species with a luteal phase. For example, animals with a true luteal phase, such as monkeys and sheep, exhibit a long preovulatory GnRH surge, lasting well af
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br NMDA receptor LBDs The study of
2021-09-11
NMDA receptor LBDs The study of GluA2 was later expanded to include NMDA receptors [22]. NMDA receptors are obligate heterotetramers that are composed of two glutamate-binding subunits and two glycine-, or d-serine-, binding subunits. In this study, crystal structures of the NMDA receptor glycine
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Bedaquiline synthesis In this sense feline females are coitu
2021-09-11
In this sense, feline females are coitus-induced ovulators and regardless they get pregnant or not, serum progesterone levels increase over 1.5 ng/ml once ovulation has occurred [42]. On the other hand, queen embryos reach the uterus on days 6–8.5 after coitus [29]. Due to their small size, embryos
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A key limiting factor in the semi
2021-09-11
A key limiting factor in the semi-quantitative analysis of changes in the nuclear-to-cytoplasmic distribution of glucokinase is the large intercellular heterogeneity of AP24534 of glucokinase in both isolated hepatocytes in vitro and also in liver in vivo[13], [23], [24], [26], [36]. This necessita
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Previous attempts to minimize the contribution
2021-09-11
Previous attempts to minimize the contribution of the compensatory changes due to chronic loss of Gcgr, have used temporally-controlled reduction of glucagon levels by alpha-cell ablation, glucagon immunoneutralization, and the use of small molecule or antibody glucagon receptor antagonists [10], [3
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Given the actions of GIP analogues administered
2021-09-11
Given the actions of GIP analogues administered as a single dose to ob/ob mice, studies were performed to assess their ability to act in vivo as antagonists of GIP-induced insulinotropic and antihyperglycaemic actions. (Ala3)GIP, (Phe3)GIP, (Tyr3)GIP and (Pro3)GIP all counteracted the glucose-loweri
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ATN Ac PHSCN NH is a small peptide antagonist of
2021-09-10
ATN-161 (Ac-PHSCN-NH2) is a small peptide antagonist of integrin α5β1, a recently developed anticancer drug that interacts with the N-terminus of the β1 region of integrin α5β1 to lock integrin α5β1 in its non-activated conformation (Wang et al., 2016). The drug has been tested in Phase 2 clinical t
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br Venous thromboembolism VTE is a
2021-09-10
Venous thromboembolism (VTE) is a rare but potentially life-threatening complication of total joint arthroplasty (TJA) . With modern chemoprophylaxis, the incidence of VTE after primary total hip (THA) or total knee (TKA) arthroplasty is commonly estimated between 0.5% and 1%, and VTE is now consi
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br Methods br Results br Discussion In the general
2021-09-10
Methods Results Discussion In the general population BNP has been established as a marker for casein kinase 2 inhibitor failure diagnosis. Moreover, there is growing evidence that elevated levels of natriuretic-peptides may improve CV risk prediction in the general population above traditi
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Several named antagonist ligands have figured noticeably in
2021-09-10
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
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br We are now ready to prove the counterpart of
2021-09-10
We are now ready to prove the counterpart of Proposition 6.4 for κ-collectionwise normality. This is the pointfree counterpart of the classical result, originally proved in [23], that κ-collectionwise normality is hereditary with respect to -sets. (It may be worth emphasizing that the localic p
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The second approach to optimizing microsomal stability
2021-09-10
The second approach to optimizing microsomal stability in this series involved the strategic positioning of steric bulk along the tether as a means of encumbering the access of oxidative enzymes to the methylene bridge. This approach has been employed in other P2-P4 macrocyclic inhibitors of NS3/4A
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Assays can perform differently by genotype and under
2021-09-10
Assays can perform differently by Eltrombopag australia and under-quantification of HCV GTs has been seen with HCV assays [8], [9], [10], [11]. Under-quantification of GT4 has been reported in some early studies of the VERIS Assay [7], [12] where a bias greater than −0.5 log10IU/mL was seen. In two
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