HEK293 cells, transfected

When assayed in HEK293 cells transfected with the cloned human, rat and guinea pig TRPVl, (23a) showed similar potencies. Not unexpeetedly, (23a) showed poor metabolic stability and a structure-activity study to optimize potency and drug-like properties was initiated. Modification on the left-handed A -aryl section showed that ... 

FIGURE 3.10 Sodium nitroprusside increases protein tau phosphorylation in HEK293 cells transfected with mutated tau441 (B) when compared to untreated cells (A). GSK-3(3 is one of the protein kinases involved in tau phosphorylation. Inhibition of GSK-3(3 by LiCl markedly reduces tau phosphorylation (C). The results are expressed as the means S.D. (N = 3). Source Redrawn from Zhang et al. 

Fig. 1. P2X currents in smooth muscle cells resemble heterologously expressed P2Xi currents. A. Currents evoked by purinergic agonists in single vas deferens smooth muscle cells. B. Currents from HEK293 cells transfected with P2Xi cDNA. Current desensitization and response to the selective agonist, -me-ATP are similar. From Surprenant et al, 1995 (Figure 3)...

An azetidine motif was also present in two series of CBi antagonist compounds disclosed by Vernalis Research [335, 336]. In the former, compound (560) was claimed to have an affinity of 285 nM in transfected HEK293 cells using tritium-labelled (382). Among the preferred indications were psychosis, schizophrenia, smoking cessation and eating disorders associated with excessive food intake. Compound (561) was claimed to have an affinity of 0.8 nM in the same binding assay [336]. 

A number of compounds activate TRPA1 without any apparent ability to form covalent adducts, including nonelectrophilic fenamate nonsteroidal anti-inflammatory drugs (NSAIDs), such as flufenamic acid (17, FFA), niflumic acid (18, NFA), and mefenamic acid (19, MFA) [13]. Phenols such as thymol (20) and 2-ferf-butyl-5-methylphenol (21) have been shown to activate human TRPA1 with micromolar EC50 values in stably transfected HEK293 cells [14]. 

O Farrell, C., et al., Transfected synphilin-1 forms cytoplasmic inclusions in HEK293 cells. Brain Res Mol Brain Res, 2001, 97/3/, 94-102. 

The HaloTag-CLl expression plasmid was used for the transfection of HEK293 cells in the 96-well plate according to the method described in Subheading 3.3.1. 

P/Q-type channels with CAG expansion transfected in HEK293 cells results in perinuclear aggregates and cell death (Ishikawa et al., 1999)... 

Querfurth, H. W., Jiang, J., Geiger, J. D., and Selkoe, D. J. (1997). Caffeine stimulates amyloid beta-peptide release from beta-amyloid precursor protein-transfected HEK293 cells. J Neurochem 69, 1580-1591. 

The primary signaling linkage of the 5-HT6 receptors is to the stimulation of AC (355,356,360,369). Native 5-HT6 receptors stimulate AC activities in pig caudate membranes and in striatal neurons (370). 5-HT6 receptors also increase cellular levels of cAMP when transfected into JEG-3, COS-7, and HEK293 cells (357,371). In HEK293 cells, the increases in cAMP levels are... 

---