Chemistry:Ignavine
Ignavine is a naturally occurring diterpene alkaloid found in Aconiti tuber.[1][2][3][4][5] It has been reported to act as a μ-opioid receptor (MOR) positive allosteric modulator (PAM).[1][3][4][6] The drug potentiated responses to the selective MOR agonist DAMGO at low concentrations but inhibited DAMGO at high concentrations.[1][4][6] Ignavine alone has been found to produce analgesic effects in animals, but with a biphasic dose–response curve.[4][1] Although described as a MOR PAM, other research suggests that ignavine is a ligand of the orthosteric site of the MOR and does not act as a PAM.[1] Instead, it may be a MOR partial agonist.[1] However, more research is necessary to clarify its MOR actions.[1] Ignavine was first isolated by 1952[5] and its reported MOR PAM activity was first reported by 2016.[2][6]
See also
- BMS‐986122
- BMS-986187
References
- ↑ 1.0 1.1 1.2 1.3 1.4 1.5 1.6 "Allostery at opioid receptors: modulation with small molecule ligands". Br J Pharmacol 175 (14): 2846–2856. July 2018. doi:10.1111/bph.13823. PMID 28419415.
- ↑ 2.0 2.1 "Recent Advances in the Realm of Allosteric Modulators for Opioid Receptors for Future Therapeutics". ACS Chem Neurosci 8 (6): 1147–1158. June 2017. doi:10.1021/acschemneuro.7b00090. PMID 28368571.
- ↑ 3.0 3.1 "New opioid receptor modulators and agonists". Best Pract Res Clin Anaesthesiol 32 (2): 125–136. June 2018. doi:10.1016/j.bpa.2018.06.009. PMID 30322454.
- ↑ 4.0 4.1 4.2 4.3 "Analysis of natural product regulation of opioid receptors in the treatment of human disease". Pharmacol Ther 184: 51–80. April 2018. doi:10.1016/j.pharmthera.2017.10.021. PMID 29097308.
- ↑ 5.0 5.1 "Pharmacological studies of ignavine, an aconitum alkaloid". Chem Pharm Bull (Tokyo) 30 (5): 1844–1850. May 1982. doi:10.1248/cpb.30.1844. PMID 7116516.
- ↑ 6.0 6.1 6.2 "Ignavine: a novel allosteric modulator of the μ opioid receptor". Sci Rep 6. August 2016. doi:10.1038/srep31748. PMID 27530869. Bibcode: 2016NatSR...631748O.
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