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Chemical Structure| 1953-04-4 Chemical Structure| 1953-04-4

Structure of Galanthamine HBr
CAS No.: 1953-04-4

Chemical Structure| 1953-04-4

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Galanthamine hydrobromide is a natural occuring AchE inhibitor with IC50 value of 410nM and allosteric potentiator at neuronal nAchRs, used for the treatment of cognitive decline in mild to moderate Alzheimer's disease and various other memory impairments.

Synonyms: Galantamine hydrobromide; Galanthamine hydrobromide; NSC 100058

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Product Details of Galanthamine HBr

CAS No. :1953-04-4
Formula : C17H22BrNO3
M.W : 368.27
SMILES Code : O[C@H]1C=C[C@@]23CCN(C)CC4=CC=C(OC)C(O[C@@]3([H])C1)=C24.Br
Synonyms :
Galantamine hydrobromide; Galanthamine hydrobromide; NSC 100058
MDL No. :MFCD00067672
InChI Key :QORVDGQLPPAFRS-XPSHAMGMSA-N
Pubchem ID :121587

Safety of Galanthamine HBr

GHS Pictogram:
Signal Word:Danger
Hazard Statements:H301
Precautionary Statements:P301+P310
Class:6.1
UN#:1544
Packing Group:

Isoform Comparison

Biological Activity

Target
  • AChE

    AChE, IC50:0.35 μM

In Vitro:

Cell Line
Concentration Treated Time Description References
HT-22 cells 10 μM 24 hours To investigate the effect of galantamine on Mi-sup-induced inflammatory response in HT-22 cells. Galantamine reduced the Mi-sup-induced increase in NF-κB p65 levels and expression of pro-inflammatory cytokines (IL-1β and IL-6). J Neuroinflammation. 2018 Apr 18;15(1):112
BV-2 cells 10 μM 24 hours To investigate the effect of galantamine on LPS-induced inflammatory response in BV-2 cells. Galantamine reduced the LPS-induced increase in NF-κB p65 levels. J Neuroinflammation. 2018 Apr 18;15(1):112
α7 nACh receptors stably expressed in HEK293 cells 10 nM to 10 μM 40 s pre-application (60 s for 0.01 μM), followed by 250 ms co-application with ACh To validate modulatory effects of galanthamine on α7 nACh receptors in HEK293 cells. Results aligned with oocyte experiments, showing no positive modulation and inhibition at high concentrations (100 μM). Br J Pharmacol. 2018 Jul;175(14):2911-2925
RAW 264.7 cells 10 μmol/L 24 hours To investigate the effect of Galanthamine on LPS-induced migration of RAW 264.7 cells, results showed that Galanthamine significantly inhibited LPS-induced cell migration. Acta Pharm Sin B. 2020 Oct;10(10):1926-1942

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Kunming mice LPS-induced neuroinflammation model Intraperitoneal injection 4 mg/kg Once daily for 14 days To investigate the effect of galantamine on LPS-induced cognitive impairment and neuroinflammation. Galantamine improved LPS-induced deficits in spatial learning and memory, reduced the expression of CD11b, GFAP, NF-κB p65, and pro-inflammatory cytokines in the hippocampus, and increased the levels of synapse-associated proteins (SYN and PSD-95). J Neuroinflammation. 2018 Apr 18;15(1):112
Wistar rats Adolescent intermittent ethanol (AIE) exposure model Intraperitoneal injection 4 mg/kg In the prevention study, administered 30 min prior to each gavage, totaling 16 doses; in the restoration study, administered daily for 2 weeks starting from P57 Galanthamine prevented and reversed AIE-induced neuroimmune signaling and loss of hippocampal neurogenesis. In the prevention study, galantamine pretreatment blocked AIE induction of CCL2, HMGB1, and COX-2, and prevented the reduction in neurogenesis. In the restoration study, galantamine treatment reversed AIE induction of these inflammatory markers and restored neurogenesis. J Neuroinflammation. 2021 Sep 16;18(1):212
Mice Caerulein-induced acute pancreatitis model Intraperitoneal injection 1, 4, or 6 mg/kg body weight Administered once 1 hour before the first caerulein injection and again 30 minutes after the third injection Galanthamine significantly attenuated pancreatic histologic injury, reflected by a reduction in serum amylase and pancreatic inflammatory cytokines and an increase in the anti-inflammatory cytokine IL-10 in the serum. These beneficial effects were not altered by bilateral subdiaphragmatic vagotomy, knockout of either choline acetyltransferase-positive T cells or α7nAChR, or administration of the nAChR ganglionic blocker mecamylamine or the more selective α7nAChR antagonist methyllycaconitine. Mol Med. 2023 Oct 31;29(1):149
Mice Opa1–/– mice and aged WT mice Oral 3.28 mg/kg bodyweight/d Daily for 90 days (Opa1–/– mice) or 18 weeks (aged mice) RJx-01 (containing Galanthamine) improved muscle function, reduced denervation, decreased inflammatory markers, ameliorated mitochondrial morphology and autophagy, and increased satellite cell content. JCI Insight. 2023 Aug 8;8(15):e168787
Mice FMF-KI mice (MefvV726A/V726A) Intraperitoneal injection 4-12 mg/kg (escalated by 4 mg every 2 weeks) Twice daily for 8 weeks To assess the impact of long-term Galanthamine on chronic inflammation in FMF-KI mice. Results demonstrated significant attenuation of splenomegaly, reduced inflammatory cell infiltration (e.g., spleen and subcutaneous air pouch), decreased serum amyloid A (SAA) levels, and improved anemia. Notably, Galanthamine's effects persisted in vagotomized or α7nAChR-KO mice, suggesting a mechanism independent of the classical cholinergic anti-inflammatory pathway. Mol Med. 2022 Dec 9;28(1):148
Sprague-Dawley rats Cardiac ischemia/reperfusion (I/R) model Isolated heart perfusion 5 × 10^-8 M 30 min ischemia followed by 40 min reperfusion To investigate the effect of galantamine on cardiac ischemia/reperfusion injury in isolated hearts. Results showed that galantamine treatment significantly improved left ventricular function (LVDP, ±dP/dt, WP) without affecting heart rate. Mol Med. 2017 Jul;23:120-133
Male adult Wistar rats Experimental model of dementia induced by scopolamine Intraperitoneal injection 1 mg/kg For 9 consecutive days To evaluate the neuroprotective effects of galantamine in scopolamine-induced dementia in rats. Results showed that galantamine significantly increased brain ACh levels, improved recognition memory and habituation, and restored the cholinergic system influence index. Antioxidants (Basel). 2022 Feb 12;11(2):374
NOD mice Type 1 diabetes model Intraperitoneal injection 1 mg/kg Daily for 20 weeks To study the preventive effects of galantamine in type 1 diabetes, results showed that galantamine significantly delayed the onset of hyperglycemia, reduced pancreatic islet inflammation, and decreased serum levels of anti-insulin antibodies. Mol Med. 2015 Nov;21(1):702-708

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT00236574 Dementia|Alzheimer Disease PHASE3 COMPLETED 2025-11-03 -
NCT00297362 Alzheimer Disease COMPLETED 2025-10-05 -
NCT00338117 Alzheimer's Disease|Dementia PHASE3 COMPLETED 1997-05-01 -
NCT00236431 Dementia|Alzheimer Disease PHASE3 COMPLETED 2025-12-03 -

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.72mL

0.54mL

0.27mL

13.58mL

2.72mL

1.36mL

27.15mL

5.43mL

2.72mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2
The prepared working fluid is recommended to be prepared now and used up as soon as possible in a short period of time. The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1

References

 

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