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The compounds are selective upstream inhibitors of FcεR1-dependent human mast cell degranulation and proved to be devoid of activity in downstream ionomycin mediated degranulation.
2-Fluoroethanol and ethanol were devoid of activity in both assays.
Six extracts were devoid of activity in either assay: alfalfa, borage, celery, chamomile, comfrey and stellaria.
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It has been speculated that calpains devoid of activity are involved in regulatory processes [14], [31], for instance, calpain-6 is involved in microtubules stabilization through a non-catalytic mechanism [32].
The in vivo preliminary pharmacological results showed that in the whole series only two compounds (15, 21) were devoid of activity, whereas other molecules revealed protection in at least one animal model of epilepsy (MES or/and scPTZ).
[d-Trp4]URP and [d-Tyr6]URP both induced a robust increase in [Ca2+]c in astrocytes while [Orn5]URP was totally devoid of activity.
A secreted version of the LAT-1 ectodomain (ΔTM1-7; Figure 2B) and in-frame deletions of the GPS are completely devoid of rescuing activity in both truncated (ΔGPS/TMΔ2-7) (Langethal et al., 2009) and full-length context (ΔGPS; Figures 4E, 4F, and Table S1), whereas surface expression of ΔGPS is intact (data not shown).
Lead compounds in this series were found to be devoid of activity at the dopamine transporter and were shown to be brain penetrant with high receptor occupancy.
The ethanolic extract from C. pallida leaves showed mutagenic activity in the TA98 strain (-S9), whereas dichloromethane fraction and stigmasterol were found devoid of activity.
This conclusion is strongly supported by the fact that the HS-binding disabled mutant γ-m2 is devoid of detectable activity in vivo despite it shows full agonist potency on CXCR4 in vitro.
The kidney images showed uptake primarily in the renal cortex, while the renal medulla was devoid of activity.
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Justyna Jupowicz-Kozak
CEO of Professional Science Editing for Scientists @ prosciediting.com