• Compounds and possessed relatively low clogP values

  2020-03-16

  

  Compounds 11–13 and 15 possessed relatively low clogP values and tended to show relatively weak antagonist activity regardless of their potent EP1 receptor affinity. Compounds 2–4, which were selected based on their potent in vivo antagonist activity, were found to be effective in an animal model.

• Emergence of antibiotic resistant strains of Mtb

  2020-03-16

  

  Emergence of antibiotic resistant strains of Mtb alongwith the inefficacy of widely used Bacillus Calmette-Guerin (BCG) vaccine in adults are major challenges in the treatment and prevention of TB. Elucidation and characterization of new vaccine and drug candidates are therefore required in order to

• In Fig results of this experiment are

  2020-03-16

  

  In Fig. 1 results of this experiment are shown as the contour plots of endopeptidase activity. Optimal for the enzyme production by this strain concentrations of peptone and inorganic phosphate were found to be 24 and 0.3g/l, respectively. For specific activity, the optima close to those for glutamy

• In conclusion we have found that Egr can play an

  2020-03-13

  

  In conclusion, we have found that Egr1 can play an inhibitory role on DBH promoter-driven transcription. This inhibition requires a newly identified Egr1 response EHNA hydrochloride at the −227/−224 region of DBH promoter. This inhibition appears to result from Egr1 directly bound to the DBH promot

• A previous study suggested that DARs

  2020-03-13

  

  A previous study suggested that DARs and octopamine/tyramine receptors (OARs/TARs) have close pharmacological properties (Beggs et al., 2011). Their relationships were also supported by phylogenetic analyses (Balfanz et al., 2005, Hauser et al., 2008, Wu et al., 2014), indicating that some of DAR an

• br Role of CRF receptors

  2020-03-13

  

  Role of CRF1 receptors in the BNST in stress-induced relapse to cocaine seeking The seminal work of Stewart and co-workers [19] showed that rats that have extinguished their auto-administration of different drugs of abuse relapse to drug-seeking behaviour when exposed to footshock, even after a 4

• These cognitive deficits may suggest that cognitive

  2020-03-13

  

  These cognitive deficits may suggest that cognitive therapy and pharmacotherapy for gambling behavior may ultimately wish to consider genotyping as a means of better targeting treatment approaches. If core cognitive deficits are shown consistently in certain subgroups of gamblers based on genotype,

• The role of activation of xenosensor nuclear receptors such

  2020-03-13

  

  The role of activation of xenosensor nuclear receptors such as PPARα, CAR, and PXR in producing hepatomegaly and liver tumors in rodents has been well-established (Klaunig et al., 2003, Lake, 2009). In the case of PPARα, the increase in liver weight results from increased peroxisomal mass and expans

• br Materials and methods br Results br

  2020-03-12

  

  Materials and methods Results Discussion GOS potently inhibited SRD5A1 in COS-1 cells (Fig. 4A) and rat Leydig cells (Fig. 4B), possibly attenuating testosterone activation into DHT. It has been reported that gossypol inhibited human SRD5A1 with IC50 of 7 × 10−6 M [28]. Interestingly, gossy

• In the original ELF study patients were

  2020-03-12

  

  In the original ELF study [7], patients were considered eligible if they were due to undergo liver biopsy for the investigation of chronic liver disease, defined as abnormal biochemical liver function tests persisting for more than 6 months, ability to provide informed consent and age between 18 and

• Cubic equations of state CEoS are particularly popular due t

  2020-03-12

  

  Cubic equations of state (CEoS) are particularly popular due to their simplicity and relatively good accuracy in predicting vapour-liquid equilibrium and liquid-liquid equilibrium for small, non-polar, non-associating molecules, such as light hydrocarbons. CEoS can match the phase boundaries (L/LL a

• In we studied normal rational

  2020-03-12

  

  In [1] we studied normal, rational -varieties X of complexity one, where the latter means that X comes with an effective torus action such that holds. We showed that for affine X with and at most log terminal singularities, the iteration of Cox rings is possible. In the present article, we charac

• Animal studies investigating the role of D dopamine receptor

  2020-03-12

  

  Animal studies investigating the role of D1 dopamine receptors in the PFC have focused on delayed response tasks, which require online maintenance of a previously presented stimulus. Striatal dopamine is thought to be important for flexibility and updating goal representations when new information i

• Both progesterone and the calcium

  2020-03-12

  

  Both progesterone and the calcium ionophore A23187 rely on the synthesis of cAMP by sAC to elicit exocytosis in human sperm (Fig. 2E-H and [8], [60]). We had reported earlier that digestion of endogenous cAMP with recombinant cAMP-specific phosphodiesterase 4D [9] or inhibition of its synthesis with

• br Structure and function of EPAC isoforms EPACs are

  2020-03-12

  

  Structure and function of EPAC isoforms EPACs are guanine nucleotide exchange factors (GEFs) for the Ras-like GTPases Rap1 and Rap2 [9]. There are two mammalian EPAC isoforms, EPAC1 and EPAC2 1, 2 (Figure 1). Whereas EPAC1 displays a wide tissue distribution, the expression of EPAC2 is more restr

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