A functionally-selective μ-opioid receptor agonist; functionally selective for G protein-coupled receptor signaling (EC50 = 97 nM) over β-arrestin 2 recruitment (EC50 = >10

SR 17018 – 5 mg

Brand:
Cayman
CAS:
2134602-45-0
Storage:
-20
UN-No:
Non-Hazardous - /

SR 17018 is an orally bioavailable and brain-penetrant agonist of μ-opioid receptors.{40627} It is functionally selective for G protein-coupled receptor signaling (EC50 = 97 nM for GTPγS binding in CHO cells expressing μ-opioid receptors) over β-arrestin 2 recruitment (EC50 = >10,000 nM) at the μ-opioid receptor. SR 17018 increases latency to withdraw in the hot plate and warm water tail-flick assay (ED50s = 6.9 and 7.7 mg/kg, respectively) without inducing respiratory depression in mice when administered at doses up to 48 mg/kg. SR 17018 was designed for this biased agonism at the μ-opioid receptor to potentially widen the therapeutic window and reduce adverse effects of μ-opioid receptors, such as respiratory depression.  

 

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SKU: 24480 - 5 mg Category:

Description

A functionally-selective μ-opioid receptor agonist; functionally selective for G protein-coupled receptor signaling (EC50 = 97 nM) over β-arrestin 2 recruitment (EC50 = >10,000 nM) at the μ-opioid receptor; increases latency to withdraw in the hot plate and warm water tail-flick assay (ED50s = 6.9 and 7.7 mg/kg, respectively) without inducing respiratory depression in mice at up to 48 mg/kg

Formal name: 5,6-dichloro-1-[1-[(4-chlorophenyl)methyl]-4-piperidinyl]-1,3-dihydro-2H-benzimidazol-2-one

Synonyms: 

Molecular weight: 410.7

CAS: 2134602-45-0

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Neuroscience|Pain Research

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