A dual μ-opioid and nociceptin receptor partial agonist (Kis = 16.49 and 3.67 nM

AT-121 – 500 µg

Brand:
Cayman
CAS:
2099681-31-7
Storage:
-20
UN-No:
De Minimis - 1888 / 6.1

AT-121 is a dual μ-opioid and nociceptin receptor partial agonist (Kis = 16.49 and 3.67 nM, respectively).{35507} It stimulates [35S]GTPγS binding to cell membranes expressing μ-opioid or nociceptin receptors (EC50s = 19.6 and 34.7 nM, respectively). AT-121 (0.003-0.03 mg/kg) decreases capsaicin-induced thermal allodynia without increasing scratching activity in rhesus monkeys in a dose-dependent manner. It lacks reinforcing effects, a marker of abuse potential, and reduces oxycodone, but not food pellet, reinforcement in a drug self-administration assay in rhesus monkeys when administered at doses ranging from 0.3 to 10 μg/kg per injection. AT-121 (0.01 or 0.03 mg/kg) does not induce hyperalgesia, a marker of tolerance development, in rhesus monkeys.  

 

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SKU: 26150 - 500 µg Category:

Description

A dual μ-opioid and nociceptin receptor partial agonist (Kis = 16.49 and 3.67 nM, respectively); stimulates [35S]GTPγS binding to cell membranes expressing μ-opioid or nociceptin receptors (EC50s = 19.6 and 34.7 nM, respectively); decreases capsaicin-induced thermal allodynia without increasing scratching activity in rhesus monkeys from 0.003-0.03 mg/kg; lacks reinforcing effects and reduces oxycodone reinforcement in a drug self-administration assay in rhesus monkeys from 0.3-10 μg/kg per injection; does not induce hyperalgesia in rhesus monkeys at 0.01 or 0.03 mg/kg

Formal name: N-[2-[1,2-dihydro-1′-[cis-4-(1-methylethyl)cyclohexyl]-3-oxospiro[isoquinoline-4(3H),4′-piperidin]-2-yl]ethyl]-sulfamide

Synonyms: 

Molecular weight: 462.6

CAS: 2099681-31-7

Purity: ≥95%

Formulation: A solution in chloroform

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

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