Methyllycaconitine
Based on 48 publication(s) in Google Scholar
Methyllycaconitine (MLA) is a potent, selective, CNS-penetrant, competitive α7nAChR antagonist. Methyllycaconitine alleviates amyloid-β peptides-induced cytotoxicity in SH-SY5Y cells. Methyllycaconitine prevents methamphetamine-induced effects in mouse striatum. Methyllycaconitine can be used for neurological disease research, such as Alzheimer’s disease .
For research use only. We do not sell to patients.
- CAS No.: 21019-30-7
- Formula: C37H50N2O10
- Molecular Weight:682.80
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications Citing Use of MedChemExpress (MCE) Methyllycaconitine
More- Adv Sci (Weinh). 2025 Aug 14:e00945. [Abstract]
- Diabetologia. 2025 Dec 15. [Abstract]
- J Neuroinflammation. 2026 May 25. [Abstract]
- J Neuroinflammation. 2021 Dec 17;18(1):291. [Abstract]
- Acta Pharmacol Sin. 2024 Jul;45(7):1349-1365. [Abstract]
- Br J Pharmacol. 2025 Nov;182(21):5409-5429. [Abstract]
- Cell Death Discov. 2022 Mar 30;8(1):141. [Abstract]
- Cell Death Discov. 2022 Feb 8;8(1):54. [Abstract]
- Cell Death Discov. 2021 Mar 29;7(1):63. [Abstract]
- Neurotherapeutics. 2024 May 13:e00369. [Abstract]
- Cell Rep. 2022 Aug 30;40(9):111308. [Abstract]
- Biochem Pharmacol. 2021 Aug:190:114600. [Abstract]
- J Ethnopharmacol. 2024 Jul 4:118509. [Abstract]
- Inflamm Res. 2023 Apr;72(4):879-892. [Abstract]
- Life Sci. 2026 Mar 1:388:124199. [Abstract]
- Respir Res. 2026 Apr 1;27(1):206. [Abstract]
- Int J Mol Sci. 2024 Apr 12;25(8):4286. [Abstract]
- Eur J Pharm Sci. 2025 May 25:211:107143. [Abstract]
- Bioorg Chem. 2024 Nov:152:107716. [Abstract]
- Eur J Pharmacol. 2023 Feb 5:940:175478. [Abstract]
- Eur J Pharmacol. 2021 Jun 5:900:174067. [Abstract]
- Exp Gerontol. 2023 May:175:112139. [Abstract]
- Mediators Inflamm. 2026 Jan 21:2026:4652344. [Abstract]
- Mediators Inflamm. 2020 Sep 29:2020:1320278. [Abstract]
- iScience. 2025 Jan 17;28(2):111831. [Abstract]
- iScience. 2023 Jul 27;26(8):107477. [Abstract]
- J Integr Med. 2026 May;24(3):429-442. [Abstract]
- J Integr Med. 2026 Jan 28.
- Neurochem Res. 2025 Mar 29;50(2):131. [Abstract]
- Neurochem Res. 2021 Apr;46(4):888-904. [Abstract]
- Cell Signal. 2024 Jun 26:111275. [Abstract]
- Heliyon. 2024 Apr 9;10(8):e29426. [Abstract]
- Cardiovasc Drugs Ther. 2025 Apr 7. [Abstract]
- Ren Fail. 2026 Dec;48(1):2657652. [Abstract]
- Neurogastroenterol Motil. 2024 Dec 1:e14971. [Abstract]
- J Cell Biochem. 2024 Jul 16:e30630. [Abstract]
- Hereditas. 2025 Dec 29;162(1):239. [Abstract]
- J Pain Res. 2021 Feb 15:14:441-452. [Abstract]
- Epilepsy Res. 2025 Nov 21:219:107712. [Abstract]
- Neurosci Lett. 2023 Jan 18:794:136995. [Abstract]
- Neurosci Lett. 2020 Jun 21;730:135031. [Abstract]
- bioRxiv. 2026 May 20.
- bioRxiv. 2025 Dec 21:2025.12.19.695021. [Abstract]
- bioRxiv. 2025 Sep 11.
- SSRN. 2023 Jul 25.
- Research Square Preprint. 2023 May 30.
- Research Square Print. September 22nd, 2022.
- Research Square Preprint. 2021 Apr.
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In Vivo Imaging
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RT-PCR
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WB
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Histological Imaging/Staining
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WB
Biological Activity
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α7nAChR |
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 21019-30-7
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Molecular Weight 682.80
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Formula C37H50N2O10
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SMILES
CO[C@@H]1[C@@]23[C@@]4([H])[C@](CN([C@]2([H])[C@]([C@H]4OC)([C@@]5([C@]6([H])[C@@]3([H])C[C@@]([C@H](C5)OC)([H])[C@@H]6OC)O)O)CC)(CC1)COC(C7=C(N8C(C[C@@H](C8=O)C)=O)C=CC=C7)=O
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Synonyms
MLA
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Structure Classification
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Initial Source
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (48)
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Journal Impact Factor
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Most Recent
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Adv Sci (Weinh)
Sleep Deprivation Aggravates Periodontitis Through Trigeminal-Periodontal Neuroimmune Pathway Mediated by the AChE-ACh-α7nAChR Axis. [Abstract]2025 Aug 14:e00945. PMID: 40810704
Methyllycaconitine purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Aug 14:e00945. [Abstract]
3D reconstruction of micro-CT scanned images of the mouse alveolar bone. GTS-21 or MLA were administered in combination with EA in the LIP + SD + EA group, GTS-21 inhibited the progression of bone resorption, whereas Methyllycaconitine (MLA; 6 mg/kg; i.p. daily for 7 d) exacerbated it.
Methyllycaconitine purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Aug 14:e00945. [Abstract]
Mouse periodontal tissues mRNA expression of pro-inflammatory-related genes IL-1β), IL-6, TNF-α, and anti-inflammatory-related gene IL-10. LIP+SD (LIP with sleep deprivation); EA (10 Hz, 1 mA, square wave) ; GTS-21 (4 mg/kg; i.p. daily for 7 d); Methyllycaconitine (MLA; 6 mg/kg; i.p. daily for 7 d).
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Diabetologia
α7 Nicotinic acetylcholine receptor activation rescues mitochondrial dysfunction in gestational diabetes mellitus by competing with p66Shc for VDAC1 binding. [Abstract]2025 Dec 15. PMID: 41396300
Methyllycaconitine purchased from MedChemExpress. Usage Cited in: Diabetologia. 2025 Dec 15. [Abstract]
Immunoblot analysis of α7nAChR after co-IP with an anti-VDAC1 antibody in HTR8/SVneo cells treated with NG (Normal glucose), HG (High glucose), HG + PNU-282987 or HG + MLA (Methyllycaconitine; 24 h).
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J Neuroinflammation
PVNOXT regulates acinar cell-mediated inflammatory response via DMVACh projections to the acinar cell. [Abstract]2026 May 25. PMID: 42186091 -
J Neuroinflammation
Mechanisms underlying antidepressant effect of transcutaneous auricular vagus nerve stimulation on CUMS model rats based on hippocampal α7nAchR/NF-κB signal pathway. [Abstract]2021 Dec 17;18(1):291. PMID: 34920740
Methyllycaconitine purchased from MedChemExpress. Usage Cited in: J Neuroinflammation. 2021 Dec 17;18(1):291. [Abstract]
Immunofluorescence staining of hippocampal sections in each group rats (IL-1β). The microglia transform from ameboid form (α7nAchR(−/−) + taVNS group and Hi MLA (Methyllycaconitine; (80 μg/kg; 1-week continuous unilaterally local infusions)) + taVNS group) to ramified state (Hi saline + taVNS). Compared with α7nAchR(−/−) + taVNS group and Hi MLA + taVNS group, the co-expression between pro-inflammatory cytokine IL-1β (green) and microglia (red) decreased in Hi saline + taVNS group. IL-1β (green), Iba-1 (red), DAPI (blue), Merge (yellow).
Methyllycaconitine purchased from MedChemExpress. Usage Cited in: J Neuroinflammation. 2021 Dec 17;18(1):291. [Abstract]
The effect of α7nAchR in the hippocampus on the body mass and behavioral experiments of CUMS rats intervened by taVNS at different time points. MLA (Methyllycaconitine; 80 μg/kg; 1-week continuous unilaterally local infusions); taVNS (transcutaneous auricular vagus nerve stimulation).
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Acta Pharmacol Sin
Vagus nerve stimulation as a promising neuroprotection for ischemic stroke via α7nAchR-dependent inactivation of microglial NLRP3 inflammasome. [Abstract]2024 Jul;45(7):1349-1365. PMID: 38504011
Methyllycaconitine purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2024 Jul;45(7):1349-1365. [Abstract]
TTC staining and quantification showing the blockade of VNS-induced reduction in infarct volume in the MLA (Methyllycaconitine; 2.5 mg/kg; i.p. 1 h before tMCAO model)-treated mice subjected to tMCAO model. Scale bar: 1.0 cm, n = 6.
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Br J Pharmacol
Cholinergic G protein-coupled bile acid receptor 1 (TGR5/GPBA) in the medial septal orchestrates adult hippocampal neurogenesis and cognition in Alzheimer's disease mice. [Abstract]2025 Nov;182(21):5409-5429. PMID: 40926398 -
Cell Death Discov
Alpha-7 nicotinic acetylcholine receptor agonist alleviates psoriasis-like inflammation through inhibition of the STAT3 and NF-κB signaling pathway. [Abstract]2022 Mar 30;8(1):141. PMID: 35351863 -
Cell Death Discov
Vagus nerve stimulation alleviated cerebral ischemia and reperfusion injury in rats by inhibiting pyroptosis via α7 nicotinic acetylcholine receptor. [Abstract]2022 Feb 8;8(1):54. PMID: 35136042 -
Cell Death Discov
Vagus nerve stimulation enhances the cholinergic anti-inflammatory pathway to reduce lung injury in acute respiratory distress syndrome via STAT3. [Abstract]2021 Mar 29;7(1):63. PMID: 33782389 -
Neurotherapeutics
Electroacupuncture improves gastrointestinal motility through a central-cholinergic pathway-mediated GDNF releasing from intestinal glial cells to protect intestinal neurons in Parkinson's disease rats. [Abstract]2024 May 13:e00369. PMID: 38744625 -
Cell Rep
Enterobacter ludwigii protects DSS-induced colitis through choline-mediated immune tolerance. [Abstract]2022 Aug 30;40(9):111308. PMID: 36044853 -
Biochem Pharmacol
Cynandione A and PHA-543613 inhibit inflammation and stimulate macrophageal IL-10 expression following α7 nAChR activation. [Abstract]2021 Aug:190:114600. PMID: 33992630 -
J Ethnopharmacol
α7nAChR-mediated astrocytic activation: a novel mechanism of Xiongzhi Dilong decoction in ameliorating chronic migraine. [Abstract]2024 Jul 4:118509. PMID: 38971346 -
Inflamm Res
Activating α7nAChR helps post-myocardial infarction healing by regulating macrophage polarization via the STAT3 signaling pathway. [Abstract]2023 Apr;72(4):879-892. PMID: 36912917
Methyllycaconitine purchased from MedChemExpress. Usage Cited in: Inflamm Res. 2023 Apr;72(4):879-892. [Abstract]
PNU-282987 (3 mg/kg; i.p.; single daily for consecutively 28 days) signifcantly decreases the expression levels of collagen I, collagen III, and α-SMA in myocardial infarction (MI) rats model, while Methyllycaconitine citrate (MLA; 3 mg/kg; i.p.; single daily for consecutively 28 days) increases these proteins levels.
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Life Sci
Sinomenine ameliorates myocardial ischemia/reperfusion injury by inhibiting mitochondrial oxidative stress-mediated PANoptosis and ferroptosis via α7nAChR. [Abstract]2026 Mar 1:388:124199. PMID: 41520699 -
Respir Res
Activation of α7nAChR prevents maladaptive right ventricular remodeling via inhibiting the recruitment of CCR2+ macrophages in experimental pulmonary arterial hypertension. [Abstract]2026 Apr 1;27(1):206. PMID: 41923075 -
Int J Mol Sci
KYNA Ameliorates Glutamate Toxicity of HAND by Enhancing Glutamate Uptake in A2 Astrocytes. [Abstract]2024 Apr 12;25(8):4286. PMID: 38673879 -
Eur J Pharm Sci
Intra-aortic infusion of nicotine can induce a novel mouse model of abdominal aortic aneurysm. [Abstract]2025 May 25:211:107143. PMID: 40425130 -
Bioorg Chem
Identification of O-arylated huperzinines as novel cholinergic anti-inflammatory pathway agonists against gout arthritis. [Abstract]2024 Nov:152:107716. PMID: 39178707 -
Eur J Pharmacol
Administration of Huperzine A microspheres ameliorates myocardial ischemic injury via α7nAChR-dependent JAK2/STAT3 signaling pathway. [Abstract]2023 Feb 5:940:175478. PMID: 36563953 -
Eur J Pharmacol
Activation of alpha7 nicotinic acetylcholine receptor protects bovine endometrial tissue against LPS-induced inflammatory injury via JAK2/STAT3 pathway and COX-2 derived prostaglandin E2. [Abstract]2021 Jun 5:900:174067. PMID: 33811838 -
Exp Gerontol
Activation of α7nAChR by PNU282987 improves cognitive impairment through inhibiting oxidative stress and neuroinflammation in D-galactose induced aging via regulating α7nAChR/Nrf2/HO-1 signaling pathway. [Abstract]2023 May:175:112139. PMID: 36898594 -
Mediators Inflamm
Nicotine Regulates LPS-Induced Inflammatory Responses in HMC3 Microglia and Exerts Neuronal Protection. [Abstract]2026 Jan 21:2026:4652344. PMID: 41583120 -
Mediators Inflamm
Exploring the Mechanism on the Medullary Visceral Zone Inhibiting the Cholinergic Anti-inflammatory Pathway Induced by Sepsis. [Abstract]2020 Sep 29:2020:1320278. PMID: 33061821 -
iScience
Stimulation of TRPV1+ peripheral somatosensory nerves suppress inflammation via the somato-autonomic reflex. [Abstract]2025 Jan 17;28(2):111831. PMID: 39967868 -
iScience
Targeting CD36 determines nicotine derivative NNK-induced lung adenocarcinoma carcinogenesis. [Abstract]2023 Jul 27;26(8):107477. PMID: 37599821 -
J Integr Med
Acupuncture alleviates inflammatory pain by regulating microglial polarization through α7nAchR-mediated autophagy. [Abstract]2026 May;24(3):429-442. PMID: 41826216 -
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Neurochem Res
SAM Alleviates Neuroinflammation by Regulating M1/M2 Polarization of Microglia Through α7nAChR/Nrf2/HO-1 Signaling Pathway. [Abstract]2025 Mar 29;50(2):131. PMID: 40156718 -
Neurochem Res
S-oxiracetam Facilitates Cognitive Restoration after Ischemic Stroke by Activating α7nAChR and the PI3K-Mediated Pathway. [Abstract]2021 Apr;46(4):888-904. PMID: 33481205 -
Cell Signal
2024 Jun 26:111275. PMID: 38942343 -
Heliyon
Electroacupuncture ameliorates gastrointestinal dysfunction by modulating DMV cholinergic efferent signals to drive the vagus nerve in p-MCAO rats. [Abstract]2024 Apr 9;10(8):e29426. PMID: 38638995 -
Cardiovasc Drugs Ther
Transcutaneous Auricular Vagus Nerve Stimulation Ameliorates Heart Failure with Preserved Ejection Fraction Through Regulating Macrophage Polarization Mediated by Alpha7nAChR. [Abstract]2025 Apr 7. PMID: 40193005 -
Ren Fail
Curcumin regulates ferroptosis by activating α7 nicotinic acetylcholine receptor to improve sepsis-induced acute kidney injury. [Abstract]2026 Dec;48(1):2657652. PMID: 42015821 -
Neurogastroenterol Motil
Electroacupuncture at Zusanli (ST36) Alleviate Intestinal Ischemia-Reperfusion Injury by Regulating the Cholinergic-miRNA 124 Pathway. [Abstract]2024 Dec 1:e14971. PMID: 39618028 -
J Cell Biochem
Activation of α7 Nicotinic Acetylcholine Receptor Improves Muscle Endurance by Upregulating Orosomucoid Expression and Glycogen Content in Mice. [Abstract]2024 Jul 16:e30630. PMID: 39014907 -
Hereditas
Involvement of α7nAChR in the hepatic-protective effect of remifentanil preconditioning in ischemia/reperfusion rats. [Abstract]2025 Dec 29;162(1):239. PMID: 41466476 -
J Pain Res
The Spinal α7-Nicotinic Acetylcholine Receptor Contributes to the Maintenance of Cancer-Induced Bone Pain. [Abstract]2021 Feb 15:14:441-452. PMID: 33623426 -
Epilepsy Res
Long-term administration of EQU-001 (ivermectin) suppresses spasms in a rat model of infantile epileptic spasms syndrome. [Abstract]2025 Nov 21:219:107712. PMID: 41275582 -
Neurosci Lett
Inhibiting specificity protein 1 attenuated sevoflurane-induced mitochondrial stress and promoted autophagy in hippocampal neurons through PI3K/Akt/mTOR and α7-nAChR signaling. [Abstract]2023 Jan 18:794:136995. PMID: 36464148 -
Neurosci Lett
α7nAchR mediates transcutaneous auricular vagus nerve stimulation-induced neuroprotection in a rat model of ischemic stroke by enhancing axonal plasticity. [Abstract]2020 Jun 21;730:135031. PMID: 32416113 -
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bioRxiv
2025 Dec 21:2025.12.19.695021. PMID: 41446203 -
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Protocol
Cells are plated in 96-well plates containing complete medium and cultured for 24 h. Then cells are treated with Methyllycaconitine at the indicated concentrations for specified times. After drug treatment, cell viability is measured by MTT assay. Briefly, 10 µL of the MTT solution (5 mg/mL) is added to each well and incubated for 4 h at 37°C. After removing the supernatant, 100 µL DMSO is added into each well. The absorbance is measured at 570 nm with a microplate reader. All experiments are repeated 3 times[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Adult male Swiss CD-1 mice are used in all experiments. They are housed at 22±1°C under a 12-h light/dark cycle with free access to food and drinking water. Climbing behavior is measured. Briefly, mice of 20 to 26 g are intraperitoneally administered saline (5 mL/kg) or Methyllycaconitine (MLA) (6 mL/kg) at the beginning of the test. Twenty minutes later, the animals receive a single dose of saline or methamphetamine (METH) (1 mL/kg) subcutaneously and are placed individually, for habituation, into the experimental chamber consisting of a cylindrical cage with the wall made of plastic bars and covered with a lid. After a 20-min period of exploratory activity, stereotypy measurement is performed for a period of 30 min. Climbing behavior is scored by an observer who is blind to the drug treatment, and the time spent on climbing the wall (time during which almost two limbs are off the floor) is measured[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
References
[1]. Zheng X, et al. Methyllycaconitine alleviates amyloid-β peptides-induced cytotoxicity in SH-SY5Y cells. PLoS One. 2014 Oct 31;9(10):e111536. [Content Brief]
[2]. Escubedo E, et al. Methyllycaconitine prevents methamphetamine-induced effects in mouse striatum: involvement of alpha7 nicotinic receptors. J Pharmacol Exp Ther. 2005 Nov;315(2):658-67. [Content Brief]
[3]. Lockman PR, et al. Chronic nicotine exposure alters blood-brain barrier permeability and diminishes brain uptake of methyllycaconitine. J Neurochem. 2005 Jul;94(1):37-44. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)