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생화학적/생리학적 작용
BMS-986122 is a positive allosteric modulator (PAM of the m-opioid receptor). BMS986122 displays little or no agonist activity alone, but dose dependently increases endomorphin-I induced b-arrestin recruitment, and inhibition of forskolin-induced adenyl cyclase activity. The compound also potentiates DAMGO-stimulated GTPgS receptor binding.
BMS-986122 may exhibit an antinociception effect in vivo by increasing the efficiency of Met-enkephalin (met-Enk) to inhibit γ aminobutyric acid (GABA) release in the periaqueductal gray region of the brain.
특징 및 장점
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신호어
Warning
유해 및 위험 성명서
Hazard Classifications
Eye Irrit. 2
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point (°F)
Not applicable
Flash Point (°C)
Not applicable
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시험 성적서(COA)
Lot/Batch Number
Ram Kandasamy et al.
Proceedings of the National Academy of Sciences of the United States of America, 118(16) (2021-04-14)
Positive allosteric modulators (PAMs) of the mu-opioid receptor (MOR) have been hypothesized as potentially safer analgesics than traditional opioid drugs. This is based on the idea that PAMs will promote the action of endogenous opioid peptides while preserving their temporal
Neil T Burford et al.
Proceedings of the National Academy of Sciences of the United States of America, 110(26), 10830-10835 (2013-06-12)
μ-Opioid receptors are among the most studied G protein-coupled receptors because of the therapeutic value of agonists, such as morphine, that are used to treat chronic pain. However, these drugs have significant side effects, such as respiratory suppression, constipation, allodynia
Kerri D Pryce et al.
Neuropharmacology, 195, 108673-108673 (2021-06-22)
Positive allosteric modulators (PAMs) of the μ-opioid receptor (MOR) have been proposed to exhibit therapeutic potential by maximizing the analgesic properties of clinically used opioid drugs while limiting their adverse effects or risk of overdose as a result of using
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