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Chemical Structure| 101-26-8 Chemical Structure| 101-26-8

Structure of Pyridostigmine bromide
CAS No.: 101-26-8

Chemical Structure| 101-26-8

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Pyridostigmine Bromide is a reversible cholinesterase inhibitor to treat myasthenia gravis.

Synonyms: Pyridostigmine (bromide); Ro 1-5130; Pyridostigmine Br, Pyridostigmine

4.5 *For Research Use Only !

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Product Details of Pyridostigmine bromide

CAS No. :101-26-8
Formula : C9H13BrN2O2
M.W : 261.12
SMILES Code : C[N+]1=CC=CC(OC(N(C)C)=O)=C1.[Br-]
Synonyms :
Pyridostigmine (bromide); Ro 1-5130; Pyridostigmine Br, Pyridostigmine
MDL No. :MFCD00079283
InChI Key :VNYBTNPBYXSMOO-UHFFFAOYSA-M
Pubchem ID :7550

Safety of Pyridostigmine bromide

GHS Pictogram:
Signal Word:Danger
Hazard Statements:H300+H310+H330-H317-H410
Precautionary Statements:P260-P280-P284-P301+P310-P302+P350-P304+P340-P310
Class:6.1
UN#:2811
Packing Group:

Isoform Comparison

Biological Activity

Target
  • AChR

In Vitro:

Cell Line
Concentration Treated Time Description References
Colonic myenteric plexus neurons and glia 250 µM 3 hours To investigate the effects of PB and PEA on the activity of enteric neurons and glia. Results showed that PB pretreatment significantly reduced glial Ca2+ responses to PEA (61.0% decrease) and shifted the signaling mechanisms between neurons and glia from TRPV1-dependent to CB1 receptor- and PPARα-dependent pathways. Neuropharmacology. 2020 Nov 15;179:108264
Rat neural progenitor cells 200 µM 6 days To evaluate the effect of PY on cell viability, results showed PY did not affect cell viability at 200 μM Neurochem Res. 2015 Oct;40(10):2091-101

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Adult male Sprague Dawley rats Acute diisopropylfluorophosphate (DFP) intoxication model Intramuscular injection 0.1 mg/kg Single dose, 30 minutes before DFP injection To evaluate the effect of PB pretreatment on survival and brain AChE activity in DFP-intoxicated rats. Results showed no significant effect of PB pretreatment on 24-hour survival or brain AChE activity. Neurotoxicology. 2019 Jul;73:81-84
Wistar rats Myocardial infarction model Drinking water administration 0.14 mg/mL Daily administration for 12 weeks To evaluate the effects of PYR alone or combined with exercise on left ventricle dimensions and function, baroreflex sensitivity, autonomic parameters, and systemic and tissue inflammatory profile after myocardial infarction. Results showed that PYR alone or combined with exercise improved the deleterious effects of MI, with additional benefits in skeletal muscle anti-inflammatory state when combined with resistance training. Front Physiol. 2018 Feb 12;9:53
Rats Gulf War Illness model Oral gavage 1.3 mg/kg Once daily for 14 days To evaluate the effects of pyridostigmine bromide and stress on immune function and cholinergic neurochemistry. Results showed that pyridostigmine bromide and stress interact to enhance immune responses and alter cholinergic neurochemistry. Brain Behav Immun. 2019 Aug;80:384-393
Male Sprague Dawley rats Gulf War Illness (GWI) model Oral gavage 1.3 mg/kg Once daily for 14 days To assess the long-term effects of pyridostigmine bromide and repeated restraint stress on the cholinergic anti-inflammatory pathway. Results showed that PB treatment led to enhanced cholinergic responses and paradoxical increases in pro-inflammatory cytokine release in the prefrontal cortex and hippocampus. Neurobiol Stress. 2022 Apr 15;18:100446
Sprague Dawley rats Gulf War Illness model Oral gavage 1.3 mg/kg Once daily for 14 days To investigate the effects of PB and repeated restraint stress (RRS) on glutamatergic neurochemistry, showing that PB and stress interacted to produce brain-region specific effects on glutamate neurochemistry. Neurobiol Stress. 2019 Dec 31;12:100210
Rats Gulf War Illness model Oral gavage 1.3 mg/kg Once daily for 14 days To evaluate the effects of pyridostigmine bromide and stress on cognitive function in a model of Gulf War Illness. Results showed that PB-treated rats exhibited hippocampal-dependent memory deficits at a delayed timepoint. Brain Behav Immun. 2023 Oct;113:248-258
Mice Anti-muscle-specific kinase (MuSK) myasthenia gravis model Subcutaneous minipump 16 mg/kg/day Continuous for 7–9 days Pyridostigmine treatment exacerbated the anti-MuSK-induced reductions in postsynaptic acetylcholine receptor density and endplate potential (EPP) amplitude. J Physiol. 2013 May 15;591(10):2747-62
Male C57BL/6J mice Gulf War Illness model Subcutaneous injection 2 mg/kg Once daily for 14 days To evaluate the long-term effects of pyridostigmine bromide on behavior and neuroinflammation in a Gulf War Illness model. Results showed that pyridostigmine bromide, in combination with other chemicals, led to hyperactivity, impaired sensorimotor function, and altered gait in mice. Brain Behav Immun Health. 2022 Nov 8;26:100553
Mice Pressure overload heart failure model Subcutaneous osmotic pump 2-10 mg/kg/day Once daily for 28 days To study the effects of PYR on cardiac function and rhythmicity in heart failure mice, results showed PYR improved cardiac contractile performance and rhythmic activity J Cell Mol Med. 2021 May;25(10):4637-4648
Mice Rosa26-DTMlc2v-Cre mouse model Subcutaneous osmotic pump 3 mg/kg/d Continuous administration for 7 days, followed by 3-5 days post-DT injection To investigate the effect of pyridostigmine on inflammatory responses following myocardial injury. Results showed that pyridostigmine treatment significantly reduced mortality, cardiac inflammation, and infiltration of MHC-IIloCCR2+ monocytes in DT-injected Rosa26-DTMlc2v-Cre mice, and decreased CCL2/7 mRNA and protein expression. JCI Insight. 2019 Jun 4;5(14):e128961
C57BL/6J mice Chronic Chagasic cardiomyopathy mouse model Oral 30 mg/kg Daily for 30 days To assess the effects of pyridostigmine bromide on electrocardiographic, autonomic, histopathological, immunoinflammatory, and parasitological parameters in chronic Chagas disease in mice. Results showed that pyridostigmine bromide significantly reduced myocardial inflammatory infiltration, fibrosis, and hypertrophy, accompanied by a decrease in serum IFN-γ levels, suggesting a shift toward an anti-inflammatory immune response. Mediators Inflamm. 2014;2014:475946
Sprague Dawley rats Cardiac hypertrophy induced by abdominal aorta constriction Oral 31 mg/kg/day Once daily for 8 weeks Pyridostigmine increased acetylcholine levels by inhibiting acetylcholinesterase, significantly attenuated cardiac hypertrophy, improved cardiac function, inhibited the CaN/NFAT3/GATA4 pathway, and suppressed Orai1/STIM1 complex formation. J Cell Mol Med. 2017 Sep;21(9):2106-2116
Spontaneous hypertensive rats (SHRs) Acute myocardial infarction model Gavage 40 mg/kg Once daily for seven days Pyridostigmine treatment increased parasympathetic tone, reduced M1/M2 macrophage ratio, decreased TNF levels in heart and spleen, and improved cardiac remodeling. Sci Rep. 2021 May 5;11(1):9563
Spontaneously hypertensive rats Spontaneously hypertensive rat model Oral (via drinking water) 5 mg/kg/day and 15 mg/kg/day Daily administration for 2 weeks To evaluate the effects of pyridostigmine bromide on hemodynamic, cardiac morphofunctional, and cardiovascular autonomic adaptations in spontaneously hypertensive rats. Results showed that pyridostigmine bromide reduced BP and HR, increased vagal participation in cardiac autonomic tonic balance, and improved cardiac function parameters. Sci Rep. 2021 Aug 25;11(1):17141
C57BL/6 mice Gulf War Illness model Drinking water 90 μg/mL 7 consecutive days To evaluate the long-term effects of PB on gastrointestinal motility and neuroimmune function. Results showed that PB exposure alone did not cause significant long-term changes at 5 months but dramatically altered the effects of subsequent PEA exposure, leading to significant changes in gut motility, ENS function, and immune responses, which were sex-dependent. Neuropharmacology. 2020 Nov 15;179:108264

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT03619759 - Recruiting August 31, 2019 Korea, Republic of ... More >> Ajou university school of medicine Recruiting Suwon, Gyeonggi-do, Korea, Republic of, 16377 Contact: In Kyong Yi, MD Less <<
NCT00624663 Rivastigmine Toxicity Not Applicable Completed - Israel ... More >> Tel Aviv Sourasky Medical Center Tel Aviv, Israel Tasmc Clinical Research Center Tel-Aviv, Israel, 64239 Less <<
NCT03468452 - Completed - -
NCT02070198 Female Infertility ... More >> Poor Responder Less << Phase 4 Unknown December 2014 Italy ... More >> Bioroma Recruiting Rome, Italy, 00197 Contact: Mauro Schimberni    +39063334266    bioroma@bioroma.net    Principal Investigator: Mauro Schimberni Less <<
NCT00004332 - Completed - -
NCT01727193 Myasthenia Gravis Phase 3 Recruiting January 2020 China, Guangdong ... More >> the first affiliated hospital,SUN YAT-SEN UNIVERSITY Recruiting GuangZhou, Guangdong, China, 510000 Contact: Liu Wei bin, dean    086-020-887755766 ext 8281    ranliuz@163.com    Principal Investigator: Liu Wei bin, dean Less <<
NCT02601508 Neuromuscular Blockade Not Applicable Unknown August 2017 Korea, Republic of ... More >> Chonnam University Hwasun Hospital Not yet recruiting Hwasun, Korea, Republic of, 519-763 Contact: Chanhong Park, BsC    +82-61-379-7598    cnuhpch@naver.com    Sub-Investigator: Seongheon Lee, MD, PhD          Sub-Investigator: Inje Kim, BsC          Sub-Investigator: Shi Young Chung, MD          Principal Investigator: Seongwook Jeong, MD, PhD Less <<
NCT00995722 Ocular Myasthenia Gravis Phase 3 Terminated(Slow recruitment ra... More >>te) Less << - United States, Connecticut ... More >> Yale University New Haven, Connecticut, United States, 06510 United States, Florida University of Miami Miami, Florida, United States, 33136 United States, Kansas University of Kansas Medical Center Kansas City, Kansas, United States, 66160 United States, New York University at Buffalo, Buffalo General Medical Center Buffalo, New York, United States, 14203 United States, North Carolina Duke University Medical Center Durham, North Carolina, United States, 27710 United States, Texas University of Texas Southwestern Medical Center Dallas, Texas, United States, 75390 United States, Vermont University of Vermont Burlington, Vermont, United States, 05401 United States, Virginia University of Virginia Charlottesville, Virginia, United States, 22908 Canada, Alberta University of Alberta Hospital Edmonton, Alberta, Canada, T6G 2P4 Canada, Ontario Toronto General Hospital Toronto, Ontario, Canada, M5G 2C4 Less <<
NCT00223691 Autonomic Failure ... More >> Orthostatic Hypotension Less << Phase 1 Completed - United States, Tennessee ... More >> Vanderbilt University Nashville, Tennessee, United States, 37232 Less <<
NCT00075101 Leukemia Phase 3 Completed - United States, Tennessee ... More >> St. Jude Children Research Hospital Memphis, Tennessee, United States, 38105 Less <<
NCT00997412 Myasthenia Gravis Not Applicable Unknown May 2011 -
NCT02329964 Muscle Relaxation Phase 4 Unknown September 2016 -
NCT02329964 - Unknown - -
NCT02573519 Diabetic Autonomic Neuropathy ... More >> Gastrointestinal Motility Disorder Diabetes Mellitus Change of Transit or Circulation Less << Not Applicable Recruiting August 2019 Denmark ... More >> Department of Hematology and Gastroenterology, Aarhus University Hospital Recruiting Aarhus, Denmark, 8000 Contact: Mette Winther Andersen    +45 22635197    meteader@rm.dk    Contact: Klaus Krogh, Professor    +45 23385937    klaukrog@rm.dk    Sub-Investigator: Anne-Mette Haase, P.hD.          Sub-Investigator: Lotte Fynne, P.hD. Less <<
NCT03124355 Postural Tachycardia Syndrome Phase 1 Recruiting December 2020 United States, Tennessee ... More >> Autonomic Dysfunction Center/ Vanderbilt University Medical Center Recruiting Nashville, Tennessee, United States, 37232 Contact: Misty Hale, CCRP    615-322-2931    misty.hale@vanderbilt.edu    Sub-Investigator: Bonnie K Black, RN          Sub-Investigator: Luis E Okamoto, MD          Sub-Investigator: David Robertson, MD          Principal Investigator: Italo Biaggioni, MD          Sub-Investigator: Alfredo Gamboa, MD          Sub-Investigator: Cyndya A Shibao, MD          Sub-Investigator: Andre Diedrich, MD, PhD          Sub-Investigator: jorge Celedonio, MD Less <<
NCT02308124 Orthostatic; Hypotension, Neur... More >>ogenic Less << Phase 4 Completed - Korea, Republic of ... More >> Seoul National University Hospital Seoul, Korea, Republic of Less <<
NCT00995722 - Terminated(Slow recruitment ra... More >>te) Less << - -
NCT02308124 - Completed - -
NCT03261570 Postural Orthostatic Tachycard... More >>ia Syndrome (POTS) POTS Orthostatic Intolerance Less << Early Phase 1 Recruiting September 1, 2021 United States, New York ... More >> New York Medical College/Bradhurst building Recruiting Hawthorne, New York, United States, 10532 Contact: Courtney R. Terilli, RN. BSN    914-593-8888    courtney_terilli@nymc.edu    Contact: Julian M. Stewart, M.D., Ph.D.    914-593-8888    julian_stewart@nymc.edu    Principal Investigator: Julian M. Stewart, M.D., Ph.D.          Sub-Investigator: Marvin S. Medow, Ph.D. Less <<
NCT02850276 HIV Disease Early Phase 1 Completed - United States, New York ... More >> Icahn School of Medicine at Mount Sinai New York, New York, United States, 10029 Less <<
NCT00535587 Fibromyalgia Phase 2 Completed - United States, Oregon ... More >> Oregon Health & Science University Portland, Oregon, United States, 97219 Less <<
NCT00535587 - Completed - -
NCT02307526 - Completed - -
NCT03674541 Preload Failure ... More >> Chronic Fatigue Syndrome Myalgic Encephalomyelitis Fibromyalgia Dyspnea Less << Phase 3 Not yet recruiting October 15, 2019 -
NCT02893553 Spinal Cord Injury ... More >> Autonomic Dysreflexia Baroreceptor Integrity Sympathetic Integrity Vagal Integrity Autonomic Integrity Hypotensive Cognitive Function Cerebral Blood Flow Blood Pressure Less << Phase 2 Recruiting December 2019 United States, New Jersey ... More >> Kessler Foundation Research Center Recruiting West Orange, New Jersey, United States, 07052 Contact: Alexander T Lombard, MS    973-324-3588    alombard@kesslerfoundation.org    Contact: Caitlyn G Katzelnick, MS    973-324-3588    ckatzelnick@kesslerfoundation.org    Principal Investigator: Jill M Wecht          United States, New York James J Peters VAMC Recruiting Bronx, New York, United States, 10468 Contact: Matthew T Maher, MS    718-584-9000 ext 3122    Matthew.Maher@va.gov    Principal Investigator: Jill M Wecht, EdD Less <<
NCT02307526 Hypotension, Postural Phase 2 Completed - United States, New Jersey ... More >> Kessler Institute for Rehabilitation West Orange, New Jersey, United States, 07052 Less <<
NCT02364180 - Completed - -
NCT00409435 Postural Tachycardia Syndrome Not Applicable Recruiting February 2019 United States, Minnesota ... More >> Mayo Clinic Recruiting Rochester, Minnesota, United States, 55905 Contact: Toni Gehrking    507-284-0336    adc.research@mayo.edu    Principal Investigator: Phillip A. Low, M.D. Less <<
NCT02364180 Muscle Weakness Not Applicable Completed - United States, Ohio ... More >> University of Toledo, Health Science Campus Toledo, Ohio, United States, 43614 Less <<
NCT01370512 Orthostatic Hypotension Phase 2 Recruiting June 2019 United States, Minnesota ... More >> Mayo Clinic in Rochester Recruiting Rochester, Minnesota, United States, 55905 Contact: Tonette Gehrking    507-284-0336    adc.research@mayo.edu    Principal Investigator: Phillip A. Low, MD Less <<
NCT02227823 Spinal Muscular Atrophy Type 3 Phase 2 Unknown July 2017 Belgium ... More >> Centre de référence des maladies neuromusculaire, Centre Hospitalier Régional de la Citadelle Recruiting Liège, Belgium, 4000 Contact: Stephanie Delstanche       stephanie.delstanche@chrcitadelle.be    Contact: Severine Denis       severine.denis@chrcitadelle.be    Principal Investigator: Stephanie Delstanche Less <<
NCT00953914 Diabetes Complications Not Applicable Completed - Brazil ... More >> Hospital de Clínicas de Porto Alegre Porto Alegre, Rio Grande do Sul, Brazil Less <<
NCT02171988 Postural Orthostatic Tachycard... More >>ia Syndrome Less << Phase 4 Completed - Korea, Republic of ... More >> Seoul National University Hospital Seoul, Korea, Republic of Less <<
NCT03510546 Myasthenia Gravis Phase 4 Recruiting August 31, 2021 Denmark ... More >> Department of Neurology Aarhus University Hospital Recruiting Aarhus, Midtjylland, Denmark, 8000 Contact: Jan LS Thomsen, MD    +45 7846 6647    jathms@rm.dk    Contact: Henning Andersen, MD PhD DMSc    +45 7846 6647    hennande@rm.dk Less <<
NCT03312244 HIV-1-infection ... More >> CD4+ T Lymphocytopenia Immune Deficiency Immuno-senescence Less << Phase 2 Active, not recruiting June 30, 2020 Mexico ... More >> Instituto Nacional de Ciencias Médicas y Nutrición Salvador Zubirán Tlalpan, Ciudad de México, Mexico, 14080 Less <<
NCT00276406 Constipation ... More >>Diabetes Mellitus Colonic Transit Gastric Emptying Less << Phase 1 Phase 2 Completed - United States, Minnesota ... More >> Mayo Clinic Rochester, Minnesota, United States, 55905 Less <<
NCT03063515 Diabetes Mellitus Phase 1 Recruiting March 30, 2019 United States, Florida ... More >> Diabetes Research Institute Recruiting Miami, Florida, United States, 33136 Contact: Maria Solano    305-243-6145       Principal Investigator: Maria del Pilar Solano, MD Less <<
NCT00276406 - Completed - -
NCT01415921 - Completed - -
NCT01993680 Autonomic Disturbances in Park... More >>inson`s Disease Less << Phase 2 Unknown January 2016 Switzerland ... More >> University Hospital Zurich, Division of Neurology Zurich, ZH, Switzerland, 8091 Less <<
NCT01415921 Heart Failure Phase 2 Completed - United States, New York ... More >> New York University Langone Medical Center New York, New York, United States, 10016 Less <<
NCT02941328 Spinal Muscular Atrophy ... More >> SMA Kugelberg-Welander Disease Less << Phase 2 Completed - Netherlands ... More >> University Medical Center of Utrecht (UMCU) Utrecht, Netherlands, 3584 CX Less <<
NCT02357225 Pompe Disease Early Phase 1 Terminated(The drug was ineffe... More >>ctive in improving function in Pompe's disease) Less << - United States, Florida ... More >> University of Florida Clinical Research Center Gainesville, Florida, United States, 32610 Less <<
NCT00518154 HIV Infections Phase 2 Completed - Mexico ... More >> Departments of Immunology, and Infectious Diseases, INNSZ Mexico City, DF, Mexico, 14000 Less <<
NCT02157545 - Withdrawn(No eligible subjects... More >> identified. Study closed with IRB.) Less << - United States, Ohio ... More >> University of Toledo, Health Science Campus Toledo, Ohio, United States, 43614 Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.83mL

0.77mL

0.38mL

19.15mL

3.83mL

1.91mL

38.30mL

7.66mL

3.83mL

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

 

Historical Records

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