1. Neuronal Signaling
  2. AChE

Galanthamine (Synonyms: Galantamine)

Cat. No.: HY-76299 Purity: 99.78%
Data Sheet SDS Handling Instructions

Galanthamine is a potent acetylcholinesterase (AChE) inhibitor with IC50 of 500 nM.

For research use only. We do not sell to patients.
Galanthamine Chemical Structure

Galanthamine Chemical Structure

CAS No. : 357-70-0

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Other Forms of Galanthamine:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Galanthamine is a potent acetylcholinesterase (AChE) inhibitor with IC50 of 500 nM.

IC50 & Target

IC50: 0.5 μM (AChE)[1]

In Vitro

Galanthamine inhibits AChE and BChE with IC50 of 0.5 and 8.5 μM[1]. Galanthamine acts as a positive allosteric modulator (PAM) of human α4β2 AChRs expressed in permanently transfected HEK 293 cells. Galanthamine increases the response of (α4β2)2α5 AChRs to 1 μM ACh by up to 220% with very low concerntration(EC50=0.25 nM). Only small potentiation (20%) of either α4β2 or (α4β2)2β3 AChRs is detected using FLEXstation assays. Galanthamine at concentrations of 1 μM and above inhibits all three AChR subtypes[2].

In Vivo

Acute administration of Galantamine (0.3-3 mg/kg, i.p.) increases IGF2 mRNA levels in the hippocampus, but not in the prefrontal cortex, in time- and dose-dependent manner. Galantamine (3 mg/kg, i.p.) causes a transient increase in fibroblast growth factor 2 mRNA levels and a decrease in brain-derived neurotrophic factor mRNA levels in the hippocampus, while it does not affect the mRNA levels of other neurotrophic/growth factors. The Galantamine-induced increase in the hippocampal IGF2 mRNA levels is blocked by Mecamylamine, a nonselective nicotinic acetylcholine (ACh) receptor (nAChR) antagonist, and Methyllycaconitine, a selective α7 nAChR antagonist, but not by Telenzepine, a preferential M1muscarinic ACh receptor antagonist. Moreover, the selective α7 nAChR agonist PHA-543613 increasea the IGF2 mRNA levels, while Donepezil, an acetylcholinesterase inhibitor, does not. Galantamine also increases hippocampal IGF2 protein, which is blocked by Methyllycaconitine[2].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT00297362 Janssen Cilag Pharmaceutica S.A.C.I., Greece Alzheimer Disease June 2004 Phase 4
NCT00216593 Janssen Pharmaceutica N.V., Belgium Dementia|Alzheimer Disease December 2003 Phase 3
NCT00416169 Johnson & Johnson Pharmaceutical Research & Development, L.L.C. Frontotemporal Dementia|Pick Complex May 2003 Phase 2
NCT00077727 Johnson & Johnson Pharmaceutical Research & Development, L.L.C. Schizophrenia March 2003 Phase 3
NCT00236431 Johnson & Johnson Pharmaceutical Research & Development, L.L.C. Dementia|Alzheimer Disease May 2001 Phase 3
NCT00261573 Johnson & Johnson Pharmaceutical Research & Development, L.L.C. Alzheimer Disease|Vascular Dementia December 1998 Phase 3
NCT00216515 Janssen Korea, Ltd., Korea Alzheimer Disease March 2004 Phase 4
NCT00253214 Johnson & Johnson Pharmaceutical Research & Development, L.L.C. Alzheimer Disease|Dementia March 2001 Phase 3
NCT00236574 Johnson & Johnson Pharmaceutical Research & Development, L.L.C. Dementia|Alzheimer Disease May 2001 Phase 3
NCT00253227 Johnson & Johnson Pharmaceutical Research & Development, L.L.C. Alzheimer Disease|Dementia July 1997 Phase 3
NCT00216502 Janssen-Cilag S.p.A. Alzheimer Disease|Dementia|Mental Disorders|Brain Diseases August 2001 Phase 3
NCT00338117 Johnson & Johnson Pharmaceutical Research & Development, L.L.C.|Shire Alzheimer's Disease|Dementia August 1995 Phase 3
NCT00253201 Johnson & Johnson Pharmaceutical Research & Development, L.L.C. Alzheimer Disease|Dementia Phase 3
NCT00253188 Johnson & Johnson Pharmaceutical Research & Development, L.L.C. Alzheimer Disease|Dementia February 1997 Phase 3
NCT00240695 Johnson & Johnson Pharmaceutical Research & Development, L.L.C. Cognition Disorder|Nervous System Diseases|Mental Disorders|Brain Diseases May 2003 Phase 3
NCT01845961 Abramson Cancer Center of the University of Pennsylvania Treatment-seeking Smokers, Reporting Consumption of at Least 10 Cigarettes|Per Day for at Least the Past 6 Months January 2013 Phase 2
NCT01548638 University of Pennsylvania Nicotine Addiction February 2012 Phase 2
NCT01734395 Janssen Korea, Ltd., Korea Alzheimer's Disease March 2007 Phase 4
NCT01417429 Yale University|National Institute on Drug Abuse (NIDA) Smoking|Tobacco Withdrawal March 2010 Phase 1
NCT01039194 Bristol-Myers Squibb Alzheimer Disease January 2010 Phase 1
NCT00741598 Icahn School of Medicine at Mount Sinai|National Institute of Mental Health (NIMH)|Massachusetts General Hospital Bipolar Disorder September 2008 Phase 4
NCT01100775 University of Maryland|National Institute of Mental Health (NIMH) Schizophrenia May 2010 Phase 2
NCT00299676 Janssen-Cilag Pty Ltd Alzheimer Disease|Dementia|Galantamine May 2005 Phase 4
NCT01054976 Janssen Korea, Ltd., Korea Alzheimer's Disease October 2006 Phase 4
NCT00232349 Seattle Institute for Biomedical and Clinical Research Schizophrenia|Psychotic Disorder February 2005 Phase 4
NCT00645190 Xian-Janssen Pharmaceutical Ltd. Alzheimer Disease March 2004 Phase 3
NCT01190761 Actavis Inc. Healthy December 2004 Phase 1
NCT01190748 Actavis Inc. Healthy November 2004 Phase 1
NCT01129479 University of North Carolina, Chapel Hill|Ortho-McNeil Neurologics, Inc. Aphasia|Stroke October 2004
NCT00645554 Xian-Janssen Pharmaceutical Ltd. Pharmacokinetics Phase 1
NCT00606801 Yale University|National Institute on Drug Abuse (NIDA) Cocaine Abuse June 2007
NCT01029132 Samsung Medical Center|Janssen Korea, Ltd., Korea Dementia April 2007
NCT00969696 Yale University|National Institute on Drug Abuse (NIDA)|VA Office of Research and Development Memory August 2009 Phase 1
NCT02234752 Sheppard Pratt Health System Schizophrenia|Schizoaffective Disorder September 2014 Phase 2
NCT00809835 Yale University|National Institute on Drug Abuse (NIDA) Cocaine Dependence December 2007 Phase 2
NCT00035204 Johnson & Johnson Pharmaceutical Research & Development, L.L.C.|Ortho-McNeil Neurologics, Inc. Alzheimer Disease Phase 4
NCT01012167 University of Maryland|National Institute of Mental Health (NIMH) Schizophrenia February 2010 Phase 2
NCT01508494 Institut National de la Santé Et de la Recherche Médicale, France Stroke|Cognitive Impairment November 2011 Phase 2
NCT01478633 Janssen Pharmaceutical K.K. Alzheimer's Disease September 2011 Phase 4
NCT01181921 Janssen-Cilag, S.A. Alzheimer Disease May 2011 Phase 4
NCT00679627 Janssen Research & Development, LLC Alzheimer's Disease June 2008 Phase 3
NCT01669538 University of Pennsylvania|National Institutes of Health (NIH)|National Cancer Institute (NCI)|National Center for Research Resources (NCRR)|National Institute on Drug Abuse (NIDA) Tobacco Use Disorder August 2012 Phase 2
NCT00082602 Johnson & Johnson Pharmaceutical Research & Development, L.L.C.|Ortho-McNeil Neurologics, Inc. Alzheimer's Disease May 2004 Phase 3
NCT01009476 Janssen-Cilag G.m.b.H Dementia|Alzheimer Disease|Dementia, Vascular March 2006 Phase 4
NCT00195845 Cambridge Health Alliance|Northwestern University Bipolar Disorder April 2003 Phase 4
NCT00814658 Janssen-Cilag Farmaceutica Ltda. Dementia June 2008 Phase 4
NCT00750529 University Hospital, Clermont-Ferrand|Janssen-Cilag Farmaceutica Ltda. Alzheimer's Disease November 2008 Phase 1
NCT00814801 Janssen Pharmaceutical K.K. Alzheimer's Disease February 2007 Phase 3
NCT00164242 Caroff, Stanley N., M.D.|Ortho-McNeil Neurologics, Inc. Tardive Dyskinesia January 2002 Phase 4
NCT02283242 University of Sao Paulo|University of Nove de Julho|Feinstein Institute for Medical Research Abdominal Obesity Metabolic Syndrome March 2014 Phase 4
NCT00304629 Johnson & Johnson Pharmaceutical Research & Development, L.L.C. Alzheimer Disease March 2000 Phase 3
NCT00463879 Yale University|National Alliance for Research on Schizophrenia and Depression Schizophrenia September 2005 Phase 2|Phase 3
NCT00230997 Neurological Research Center|Ortho-McNeil Neurologics, Inc. Lewy Body Disease December 2002 Phase 3
NCT00181675 Massachusetts General Hospital ADHD December 2002 Phase 4
NCT00252603 University of Medicine and Dentistry of New Jersey|National Alliance for Autism Research|Rutgers, The State University of New Jersey Autism|Childhood Autism April 2004 Phase 3
NCT02420327 University of Maryland Basic Science Study of the Mechanisms of Attentional Enhancement by Compounds Acting on the Nicotinic Receptor September 2014
NCT00226824 Parkinson's Disease and Movement Disorders Center|Ortho-McNeil Neurologics, Inc. Tourette's Syndrome|Motor Tic Disorder|Vocal Tic Disorder September 2005 Phase 4
NCT00000172 Janssen, LP|National Institute on Aging (NIA) Alzheimer Disease Phase 3
NCT00211588 Memorial Hospital of Rhode Island|Ortho-McNeil Neurologics, Inc. Parkinson's Disease June 2004
NCT00320736 North Suffolk Mental Health Association|Janssen Medical Affairs Schizophrenia|Schizoaffective Disorder January 2004 Phase 4
NCT00176423 University of Maryland|Stanley Medical Research Institute|Ortho-McNeil Neurologics, Inc. Schizophrenia|Schizoaffective Disorder May 2002 Phase 4
NCT00309725 Johnson & Johnson Pharmaceutical Research & Development, L.L.C. Alzheimer's Disease Phase 3
NCT00301574 Janssen Pharmaceutical K.K. Alzheimer Disease April 2001 Phase 3
NCT00035191 Johnson & Johnson Pharmaceutical Research & Development, L.L.C. Dementia, Vascular October 2001 Phase 3
NCT00161044 University of Maryland Chronic Schizophrenia September 2004
NCT02872857 The University of Texas Health Science Center, Houston Subarachnoid Hemorrhage September 2016 Phase 1|Phase 2
NCT00227994 University of Pittsburgh|National Institute of Mental Health (NIMH) Cerebrovascular Accident April 2003 Phase 4
NCT00423969 Indiana University School of Medicine|Indiana University Depression November 2003 Phase 4
NCT00219869 Rapoport, Alan, M.D.|Ortho-McNeil Neurologics, Inc. Post-Traumatic Headache|Head Trauma,Closed|Retention Disorders,Cognitive July 2005 Phase 4
NCT00509067 Georgetown University|National Institute of Mental Health (NIMH)|Washington D.C. Veterans Affairs Medical Center Schizophrenia November 2007 Phase 2
NCT00523666 Ludwig-Maximilians - University of Munich Alzheimer's Disease September 2006 Phase 4
NCT01194336 U.S. Army Medical Research and Materiel Command|Walter Reed Army Institute of Research (WRAIR) Biomarkers, Pharmacological February 2012
NCT01416948 INTRuST, Post-Traumatic Stress Disorder - Traumatic Brain Injury Clinical Consortium|U.S. Army Medical Research and Materiel Command Posttraumatic Stress Disorder|Traumatic Brain Injury August 2011 Phase 2
NCT00181636 Massachusetts General Hospital Bipolar Disorder
NCT01531153 Yale University|National Institute on Drug Abuse (NIDA) Addiction September 2011
NCT01880099 Yale University Nicotine Dependence December 2013
NCT03014323 Vanderbilt University Medical Center Insulin Sensitivity|Oxidative Stress January 2017 Phase 1
NCT02365285 Vanderbilt University Medical Center|Doris Duke Charitable Foundation Obesity March 2015 Phase 1|Phase 2
NCT01921972 Charite University, Berlin, Germany|German Federal Ministry of Education and Research Alzheimer's Disease November 2004 Phase 4
NCT02098824 VU University Medical Center Mild Cognitive Impairment (Vascular)|Mild Cognitive Disorder (Vascular)|Vascular Dementia February 2014 Phase 2|Phase 3
NCT03124355 Vanderbilt University Medical Center Postural Tachycardia Syndrome July 2017 Phase 1
NCT01362686 Indiana University|Agency for Healthcare Research and Quality (AHRQ) Dementia|Alzheimer's Disease April 2011
NCT01944436 Sunnybrook Health Sciences Centre Lewy Body Disease September 2006
NCT00348140 GlaxoSmithKline Alzheimer's Disease July 2006 Phase 3
NCT01677754 Hoffmann-La Roche Alzheimer's Disease October 24, 2012 Phase 2
NCT02374567 Hannover Medical School Dementia|Depression|Schizophrenia|Psychosomatic Disorders|Anxiety Disorders January 2015 Phase 3
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References
Preparing Stock Solutions
Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
1 mM 3.4801 mL 17.4004 mL 34.8008 mL
5 mM 0.6960 mL 3.4801 mL 6.9602 mL
10 mM 0.3480 mL 1.7400 mL 3.4801 mL
Animal Administration
[2]

Galanthamine is dissolved in saline (0.9 % solution of NaCl) (Mice)[2].

Mice[2]
Eight-week-old male ddY mice are housed in cages (24 cm×17 cm×12 cm) in each group of five to six animals under controlled environmental conditions (22±1°C; 12:12-h light-dark cycle, lights on at 0800 hours, food and water ad libitum) for 1 week before use in the experiments. 453 mice are used in total and in single use for each purpose. The following drugs are used: mecamylamine, methyllycaconitine, oxotremorine, and telenzepine, and Galantamine, Donepezil, and PHA-543613. All drugs are dissolved in saline (0.9 % solution of NaCl). Drugs are administered in a volume of 10 mL/kg intraperitoneally (i.p.) (Galantamine, Donepezil, Mecamylamine, Methyllycaconitine, Oxotremorine) or subcutaneously (s.c.) (PHA-543613, Telenzepine). MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

287.35

Formula

C₁₇H₂₁NO₃

CAS No.

357-70-0

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 59 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 99.78%

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Galanthamine
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