• br Funding This work was supported by Arena Pharmaceuticals

  2025-02-11

  

  Funding This work was supported by Arena Pharmaceuticals, Inc, San Diego, CA, USA. Introduction 5-hydroxytryptamine 1B (5-HT1B) receptors are widely distributed in the central nervous system (CNS); they have various modulatory functions in drug reinforcement, appetitive behaviors, stress, moo

• Application of the broad acting HTR antagonist methiothepin

  2025-02-11

  

  Application of the broad-acting 5-HTR antagonist methiothepin (Bard et al., 1996, Hoyer et al., 1994, Peroutka, 1990) converted the TBS-induced response of both thalamocortical and intracortical A1 synapses from LTP to LTD, an effect that was mimicked by the selective 5-HT2R antagonist ketanserin (L

• ache inhibitors The link between HPV infection and neoplasia

  2025-02-11

  

  The link between HPV infection and neoplasia has been well established. HPV encodes two oncogenes (E6 and E7) that drive ache inhibitors progression by controlling the functions of tumor suppressor proteins p53 and Rb [7]. HPV is associated with more than 99% of cervical CESC cases [8]. CESC remain

• The GRAVY value for a protein is calculated

  2025-02-11

  

  The GRAVY value for a protein is calculated as the sum of hydropathy values of all the amino acids, divided by the number of residues in the sequence (Kyte and Doolittle, 1982). According to Kyte and Doolittle (1982) integral membrane proteins typically have higher GRAVY scores than do globular prot

• Previously using a P lacZ reporter gene system it has

  2025-02-11

  

  Previously, using a P-lacZ reporter gene system, it has been shown that the β-galactosidase activity was 9-fold higher in the stationary phase psoralen synthesis when compared with those of the exponential phase [15]. Furthermore, inositol supplementation did not have a major effect on the expressio

• In this paper we described synthesis biological evaluation a

  2025-02-11

  

  In this paper, we described synthesis, biological evaluation and docking study of 3-aroyl-1-(4-sulfamoylphenyl)thiourea derivatives 4a–o as 15-lipoxygenase inhibitors. Results and discussion Conclusion We designed and synthesized a novel of thiourea derivatives containing phenylsulfonamide mo

• Several structural classes of ASK inhibitors

  2025-02-11

  

  Several structural hiv protease inhibitors of ASK1 inhibitors, mostly from industry but also from academia, have been identified over the last decade. In 2012, Terao et al. (Takeda) reported imidazo[1,2-α]pyridine () as a potent ASK1 inhibitor derived from structure-based drug design. GSK, Merck a

• The approach of enzymatically converting an analyte and dete

  2025-02-11

  

  The approach of enzymatically converting an analyte and detecting it by the resulting small pH changes near the reduced graphene oxide (rGO) surface has successfully been pursued in case of urea (Piccinini et al., 2017). Furthermore, this work reported that electrostatic layer-by-layer (LbL) assembl

• Many naphthoquinone derivatives have been previously obtaine

  2025-02-11

  

  Many naphthoquinone derivatives have been previously obtained from fungi in the genus Fusarium isolated from various sources, F. oxysporum from the root of citrus (Nagia and El-Mohamedy, 2007), Fusarium sp. (No. b77) from the mangrove plant (Shao et al., 2010), F. solani and F. oxysporum from fibrou

• Tumor tissues often experience hypoxia owing to accelerated

  2025-02-11

  

  Tumor tissues often experience hypoxia owing to accelerated growth rates of malignant cells, accumulation of metabolic products, disorganization of tumor blood vessels, and high interstitial fluid pressures (Makino et al., 2001). In response to AAD treatment, tumor vascular density often decreases t

• Corticosterone induced inhibition of OCT mediated transport

  2025-02-10

  

  Corticosterone-induced inhibition of OCT-mediated transport is rapid and appears to involve direct interaction of the steroid with the transporter at a specific site. Volk et al. (2003) studied OCT2-mediated transport by measuring substrate-induced currents using patch clamp of Xenopus oocytes exoge

• Tension within the network could be

  2025-02-10

  

  Tension within the network could be explained by two potential mechanisms: the more classical contractility that is dependent on motor proteins that are pulling sphingosine kinase inhibitor filaments towards each other [10]; or contractility that is caused by disassembly of a crosslinked network of

• Tacrine an aminoacridine derivative Fig A

  2025-02-10

  

  Tacrine, an aminoacridine derivative (Fig. 1, A), was the first AChE inhibitor approved for treatment of AD [12], [13]. This compound was withdrawn from the market due to its hepatotoxicity [14]. In spite of tacrine's side effects, it is still an attractive lead compound for medicinal chemists due t

• br AChE variants and their functions The AChE gene

  2025-02-10

  

  AChE variants and their functions The AChE gene generates several splice variants of AChE which are designated as hydrophobic (H), readthrough (R) and tailed (T) forms differing in membrane association and also localisation on a tissue and sub-cellular level. They all undergo significant posttran

• The present study showed for the

  2025-02-10

  

  The present study showed, for the first time, that hirsutine, hirsuteine, rhynchophylline, isorhynchophylline, corynoxeine, and isocorynoxeine in yokukansan can inhibit the 5-HT3 receptor current. These data indicate that part of the effect of yokukansan against the behavioral and psychological symp

16115 records 21/1075 page Previous Next First page 上5页 2122232425 下5页 Last page