• Overall we partially confirmed our predictions and when comp

  2022-02-18

  

  Overall, we partially confirmed our predictions, and, when compared to the other existing dataset exploring the interaction among CRFR1, FAAH, and anxiety, our data are somewhat confirmatory. Demers and colleagues (Demers et al., 2016) found one (protective) CRFR1 minor allele (rs110402) and the (le

• Increasing trans epithelial transport efficiency is another

  2022-02-18

  

  Increasing trans-epithelial transport efficiency is another area where different strategies are being developed for overcoming transcytosis. Enhancing the affinity for the basal membrane and weakening apical exocytosis through the optimisation of surface hydrophobicity have been demonstrated [79]. S

• Endotoxin induced pulmonary hypertension is a

  2022-02-18

  

  Endotoxin induced-pulmonary Digoxin is a reproducible finding in various animal models Leeper-Woodford et al., 1991, Weitzberg et al., 1993 and is also a feature of human sepsis where it may affect right ventricular function (Vincent, 1998). Mechanisms such as vasoconstriction and leukocyte aggrega

• Compounds and were evaluated for their

  2022-02-18

  

  Compounds and were evaluated for their pharmacokinetic properties in rats and the results are summarized in . Following intravenous (IV) administration, both compounds displayed low clearance (CL), short half-lives (t) and low volumes of distribution (V). When dosed orally as a solution, exposure

• At baseline Hdc KO mice have

  2022-02-18

  

  At baseline, Hdc-KO mice have alterations in the examined signaling cascades that resemble those seen in WT mice after RAMH challenge. Specifically, 6015 of MSK1 at T581 and of rpS6 ad S235/236 are elevated in dMSNs to a similar extent after saline in KO mice and after RAMH challenge in WT siblings

• On the other hand imidazolylcyclopropane derivatives

  2022-02-18

  

  On the other hand, imidazolylcyclopropane derivatives and having a 2-substituted benzimidazolyl group showed moderate binding affinities for both the HR and HR. Replacement of 4-chlororbenzylamino group of with a benzimidazolyl group () led to increase the affinity for the HR more than 5-fold ( =

• It is important to mention that the IC of

  2022-02-18

  

  It is important to mention that the IC50 of cetirizine needed to achieve histamine H2 receptor desensitization was 0.43 µM or 170 ng/ml (Fig. 1B), becoming clinically relevant since pharmacokinetic studies after oral administration of the clinically used dose (10 mg/day) reported a maximal plasma co

• We demonstrated that bilirubin the

  2022-02-17

  

  We demonstrated that bilirubin, the product of heme metabolism by HO-1, exerted a potent suppression of NADPH oxidase activity (Fig. 2B). Different from the down-regulation of NADPH oxidase subunit by HO-1 induction in macrophages [24], the protein levels of the NADPH oxidase subunits in vascular en

• Since we found miR b p to

  2022-02-17

  

  Since we found miR-15b-5p to be differentially expressed along the porcine intestine in 31 day old piglets in a former study [10], the entire miRNA family was analyzed in terms of interaction with potential target-genes. In silico analysis predicted miR-15 family members to target the hedgehog signa

• br Modulators of the GUCY C

  2022-02-17

  

  Modulators of the GUCY2C/cGMP/PDEs signaling pathways for CRC prevention and therapy (pre-clinical and clinical development) Several modulators of the GUCY2C/cGMP/PDEs signaling pathways, including GUCY2C agonists and PDEs inhibitors, have been developed and explored as chemopreventive agents for

• Main Text There are over

  2022-02-17

  

  Main Text There are over 200 small GTPases that play critical roles in diverse fundamental cellular processes such as signal transduction, Glycopyrrolate dynamics, and intracellular trafficking. Most of the GTPases act as switch-like molecules by cycling between the guanosine triphosphate (GTP)-bo

• br Action of GPR in metabolically

  2022-02-17

  

  Action of GPR55 in metabolically active tissues In addition to being highly expressed by discrete brain regions, as described in Section 2, GPR55 is also expressed in a wide range of peripheral tissues, including spleen, adrenals and bone (Sawzdargo et al., 1999, Ryberg et al., 2007, Whyte et al.

• We suggest that the FRET enhancement

  2022-02-17

  

  We suggest that the FRET enhancement observed when the modified mD1 protein containing Acd at position 28 was excited at 260nm (), may differ from the diminution in fluorescence observed following excitation at 280nm due to the excitation of different transitions in Trp (i.e., the L and L transition

• Due to the therapeutic potential of

  2022-02-17

  

  Due to the therapeutic potential of GlyT1 inhibitors, numerous drug screening campaigns have been started - and are still going on - which aimed at the identification of compounds with biological activity at or affinity for this drug target. For characterization of biological activity at GlyT1, tran

• In parallel we were also preparing and evaluating other pipe

  2022-02-17

  

  In parallel, we were also preparing and evaluating other piperidine bioisosteres and modifications to – to further access additional novel intellectual property (IP) space. Modeling work suggested that 4-position homologated piperidines, as well as 3-position homologated azetidines overlapped favora

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