• Importantly other aspects of platelet function

  2022-06-27

  

  Importantly, other aspects of platelet function (aggregation, spreading, in vitro and in vivo thrombosis) important for haemostasis and thrombosis were unaltered in Ral DKO platelets and mice. Beyond haemostasis and thrombosis however, platelets have been implicated in numerous pathophysiological pr

• In summary we have designed and optimized a new series

  2022-06-27

  

  In summary, we have designed and optimized a new series of 1,4-dioxycyclohexane GPR119 agonists. SAR studies led to the discovery of the preferred molecule that has potent and efficacious GPR119 activity across species. This lead compound exhibited an excellent ADME and safety profile, and demonstr

• In addition to their functional activation of GPR

  2022-06-27

  

  In addition to their functional activation of GPR109A, compounds of the pyrazolopyrimidine class also enhanced the binding of nicotinic Cycloheximide to the receptor. For instance, increased the binding of H-nicotinic acid to the receptor (black curve) in a concentration-dependent manner, whereas

• Introduction Substantial body of evidence supports the

  2022-06-24

  

  Introduction Substantial body of evidence supports the notion that GABA, the dominant inhibitory neurotransmitter in the hypothalamus of mammals, affects GnRH release by two classes of membrane receptors: GABAA (GABAAR) [1] and GABAB (GABAB R) [2]. Studies in rodents and sheep have documented that

• The SLC A mutations identified in both families appear to

  2022-06-24

  

  The SLC45A1 mutations identified in both families appear to be hypomorphic given that they resulted in a reduction but not abolition of intracellular glucose transport by SLC45A1 in our in vitro assay. It is tempting to speculate that recessive mutations causing a more severe dysfunction of the tran

• Octopamine HCl br Regulation of the GLI code

  2022-06-24

  

  Regulation of the GLI code by non-HH signals and by the oncogenic load The GLI code may be seen as the essential parameter to regulate canonical HH output. Its regulation first appeared to be strictly dependent on the presence of specific levels of HH ligands. Indeed, GLI1 transcription is so far

• br Ghrelin actions in the central nervous system br Ghrelin

  2022-06-24

  

  Ghrelin actions in the central nervous system Ghrelin induces thymopoeisis GHS-R1a is expressed in immune cells, including thymocytes and T-cells [13]. Infusion of ghrelin increases the number of thymocytes and thymus size in 14-, 20-, and 24-month-old mice, and with decreased thymic adiposity

• By association a possible mechanism which may underlie

  2022-06-24

  

  By association, a possible mechanism which may underlie the progression of seizures is long-term potentiation (LTP). Indeed, LTP shares many common mechanisms with seizures activity both anatomically and physiologically, and has been implicated as a mechanism of acute epileptogenesis (Wasterlain et

• At the end of experiments rats were injected high dose

  2022-06-24

  

  At the end of experiments rats were injected high dose of sodium pentobarbital (90mg/kg) and the rat’s head was cut and frozen in −20°C for 20min with the injecting tube in situ before section. The location of the tip of the injecting tube was verified and all the tips of the injecting tube were in

• br Materials Aspergillus oryzae GS U

  2022-06-24

  

  Materials Aspergillus oryzae βGS (8.4 U mg−1 solid) was obtained from Sigma-Aldrich Chemicals Co. (USA). o-Nitrophenyl β-d-galactopyranoside (ONPG), sodium carbonate, zinc chloride, manganese chloride, calcium chloride and potassium chloride were procured from Sisco Research Laboratories (SRL), M

• Determination of enzyme activity differs from other analytic

  2022-06-24

  

  Determination of enzyme activity differs from other analytical procedures. In this peptide receptors case, instead of enzyme concentration, a substrate depletion or product accumulation should be monitored. Such approach allows calculating activity basis of calibration curves performed for enzymati

• Studies on FXR knockout mice demonstrated that

  2022-06-24

  

  Studies on FXR knockout mice demonstrated that FXR activity is necessary to maintain a proper integrity of intestinal tight junction [18]. HF diet-induced bowel dysfunction impaired FXR activity and affected fecal BA profile. Generally, it augmented the concentration of secondary BAs in the colon e.

• With the nitrogen containing heterocycle components

  2022-06-24

  

  With the nitrogen-containing heterocycle components and the acidic components in hand, the final products were synthesized according to the procedure as depicted in . Reaction of – with various β-substituted phenylpropionic AMG 487 (, and ), followed by deprotection by TFA, smoothly provided the c

• As a part of our continuing efforts towards discovery of

  2022-06-24

  

  As a part of our continuing efforts towards discovery of new class of compounds against different therapeutic areas and based on the literature reports, we designed a dual pharmacophore which possess a long aliphatic chain of free fatty acids and a phenyl propanoid part of known GPR40 agonists. Here

• Several transgenic and knockout congenic mouse models

  2022-06-24

  

  Several transgenic and knockout/congenic mouse models have been generated in order to assess the role of FFAR1 for proper insulin secretion and maintenance of glucose homeostasis. The results obtained with three different receptor knockout mouse models were not consistent. The protection against hig

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