| Name | AT-121 |
| Description | AT-121 is a dual μ-opioid and neuropeptide receptor partial agonist (Kis 16.49 and 3.67 nM, respectively). It stimulates [35S]GTPγS binding to cell membranes expressing either μ-opioid receptors or neuropeptide receptors (EC50s of 19.6 and 34.7 nM, respectively.) AT-121 (0.003-0.03 mg/kg) reduced capsaicin-induced thermal anisocoria in a dose-dependent manner, but did not increase scratching activity in rhesus monkeys. In rhesus monkey drug self-administration tests, AT-121 at doses of 0.3 to 10 μg/kg per injection lacked reinforcing effects (a potential marker of abuse) and did not reduce the reinforcing effects of food pellets.AT-121 (0.01 or 0.03 mg/kg) did not induce hyperalgesia, a marker of tolerance, in rhesus monkeys.AT-121 is a safe non-addictive pain reliever with anti-injury and analgesic effects. |
| In vivo | AT-121 (0.003-0.03 mg/kg; s.c.; rhesus monkeys) decreases capsaicin-induced thermal allodynia dose-dependently without increasing scratching activity or inducing hyperalgesia, a marker of tolerance development, in doses of 0.01 or 0.03 mg/kg in rhesus monkeys. [1] |
| Storage | 02 | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 55 mg/mL (118.88 mM), Sonication is recommended.
Chloroform : 9 mg/mL (19.45 mM), Sonication is recommended.
DMF : Miscible
Ethanol : Miscible
Ethanol:PBS (pH 7.2) (1:20) : 50 μg/mL, Sonication is recommended.
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| Keywords | μ-opioid receptor | OpioidReceptor | Opioid Receptor | AT-121 | AT121 | AT 121 |
| Inhibitors Related | Docusate sodium | Bevenopran | Mirtazapine | Matrine | (-)-Menthol | Cuminaldehyde | Progesterone | Naltrexone hydrochloride | Cebranopadol | BTRX-335140 | Bisacodyl | Mianserin hydrochloride |
| Related Compound Libraries | Bioactive Compound Library | Anti-Neurodegenerative Disease Compound Library | Pain-Related Compound Library | Neuronal Signaling Compound Library | Membrane Protein-targeted Compound Library | Neurotransmitter Receptor Compound Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Cancer Compound Library |
United States
