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生化／生理作用
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.
特點和優勢
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訊號詞
Warning
危險聲明
危險分類
Eye Irrit. 2
儲存類別代碼
11 - Combustible Solids
水污染物質分類（WGK）
WGK 3
閃點（°F）
Not applicable
閃點（°C）
Not applicable
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
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
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