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IRL-1620

CAS No. : 142569-99-1

MCE 站：IRL-1620

产品活性：IRL-1620 是高效，选择性的内啡肽受体 (endothelin receptor) B 型激动剂，K_i 值为 16 pM。

研究领域：GPCR/G Protein

作用靶点：Endothelin Receptor

In Vitro: IRL-1620 is the most potent and specific ligand for the ETB receptor (K_iETA/ K_iETB=120,000) as judged by the K_i values for ETA (19 μM) and ETB (16 PM) receptors.
IRL-1620 is 60 times more selective for the ETB receptor than ET-3 (K_iETA/ K_iETB=1,900).

In Vivo: IRL-1620 (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 (1-100 nM) increases cytosolic Ca²⁺ 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 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, 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.

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