IRL-1620 (TFA) is the most potent and specific ligand for the ETB receptor (KiETA/ KiETB=120,000) as judged by the Ki values for ETA (19 μM) and ETB (16 PM) receptors. IRL-1620 (TFA) is 60 times more selective for the ETB receptor than ET-3 (KiETA/ KiETB=1,900).
体内研究
IRL-1620 (TFA) (1-100 nM) induces contractions of the guinea pig trachea. The effective concentration that produces 30 % of 60 mM KCI-induced contraction is estimated to be 28 nM for IRL-1620.
IRL-1620 (TFA) (1-100 nM) increases cytosolic Ca in the vascular endothelium ([Ca]E) with little effect on resting muscle tone, and relaxes the norepinephrine-stimulated tone with an increase in [Ca]E, in rat aorta,.
IRL-1620 (TFA) improves both acquisition (learning) and retention (memory) on the water maze task and enhances angiogenic and neurogenic remodeling. Rats treated with IRL-1620 significantly reduces the cognitive impairment induced by Aβ. IRL-1620 treatment enhances the number of blood vessels labeled with VEGF compared to vehicle treatment.
IRL-1620 (TFA), restores analgesic tolerance to morphine and oxycodone, but it does not affect morphine and oxycodone induced decrease in NGF/PI3K expression. IRL-1620 attenuates opioid tolerance without the involvement of NGF/PI3K pathway.
运输条件
Room temperature in continental US; may vary elsewhere.