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Chemical Structure| 77883-43-3 Chemical Structure| 77883-43-3

Structure of Doxazosin mesylate
CAS No.: 77883-43-3

Chemical Structure| 77883-43-3

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Doxazosin mesylate is a selective α1-adrenergic receptor blocker, used to treat high blood pressure and urinary retention associated with benign prostatic hyperplasia (BPH).

Synonyms: UK 33274 mesylate; Doxazosin (mesylate); UK 33274-27

4.5 *For Research Use Only !

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Product Details of Doxazosin mesylate

CAS No. :77883-43-3
Formula : C24H29N5O8S
M.W : 547.58
SMILES Code : O=C(N1CCN(C2=NC(N)=C3C=C(OC)C(OC)=CC3=N2)CC1)C4OC5=CC=CC=C5OC4.CS(=O)(O)=O
Synonyms :
UK 33274 mesylate; Doxazosin (mesylate); UK 33274-27
MDL No. :MFCD00216023
InChI Key :VJECBOKJABCYMF-UHFFFAOYSA-N
Pubchem ID :62978

Safety of Doxazosin mesylate

GHS Pictogram:
Signal Word:Danger
Hazard Statements:H372-H411
Precautionary Statements:P260-P273-P314-P391-P501
Class:6.1
UN#:2811
Packing Group:

Related Pathways of Doxazosin mesylate

GPCR

Isoform Comparison

Biological Activity

Target
  • α-adrenergic receptor

In Vitro:

Cell Line
Concentration Treated Time Description References
HL-1 cells 17.3 μM (EC50) 19.5 hours PMC3514767
HMVEC-L cells 10 μM 9 hours Evaluate the effect of DZ-50 on migration in HMVEC-L cells, results showed DZ-50 significantly inhibited endothelial cell migration PMC2194658
HUVEC cells 10 μM 24 hours To assess the biocompatibility of PP@T, results showed that even at higher concentrations, the viability of HUVEC cells remained above 85%. PMC2194658
DU-145 cells 10 μM 24 hours Evaluate the effect of DZ-50 on apoptosis in DU-145 cells, results showed DZ-50 at 10 μM did not induce classic apoptosis within 24 hours PMC2194658
PC-3 cells 10 μM 24 hours To evaluate the cytotoxic effects of EPI-001 and its derivatives on PC-3 cells. Results showed EPI-001 had no significant toxicity in PC-3 cells. PMC2194658
U3118shBMI1 5 µM 8 days To evaluate the effect of Doxazosin on the proliferation of U3118shBMI1 cells, results showed that Doxazosin had no significant effect on the proliferation of U3118shBMI1 cells PMC7082224
U3118shScr 5 µM 8 days To evaluate the effect of Doxazosin on the proliferation of U3118shScr cells, results showed that Doxazosin significantly inhibited the proliferation of U3118shScr cells PMC7082224
LX-2 cells 1, 5, 10, 20, 30, 40, 50, 60 μM 24 hours To evaluate the effect of Sophocarpine on TGF-β1-induced trans-differentiation of LX-2 cells. Results showed that Sophocarpine significantly inhibited the expression of TGF-β1, COL1A, Fibronectin, and TIMP1 in TGF-β1-treated LX-2 cells, indicating its antifibrotic effect. PMC8387324
PC3 cells 100 μM 1 hour To assess the effect of MYCi975 on MYC/MAX interaction, results showed that MYCi975 significantly disrupted the formation of MYC/MAX complex. PMC5432519

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Nude mice Human prostate cancer xenograft model Oral gavage 200 mg/kg Once daily for 2 weeks Evaluate the inhibitory effect of DZ-50 on prostate tumor growth, results showed DZ-50 significantly suppressed the growth of PC-3 and DU-145 xenografts PMC2194658
NODSCID mice U3118 xenograft model Subcutaneous injection 100 mg/kg Daily for 16 weeks To evaluate the effect of Doxazosin on U3118shScr and U3118shBMI1 xenograft tumors, results showed that Doxazosin significantly reduced the volume and proliferation of U3118shScr tumors, but had no significant effect on U3118shBMI1 tumors PMC7082224
Mice Stargardt disease model mice Intraperitoneal injection 1 mg/kg, 2 mg/kg, 3 mg/kg, 10 mg/kg Single dose, 30 minutes before light exposure Evaluate the protective effect of α1-AR antagonists on bright light-induced retinopathy, results showed DOX significantly protected retinal morphology and function PMC3859412
CD-1 mice Paracetamol-induced hepatotoxicity model Intraperitoneal injection 35.7 mmol/kg Single dose, 1 hour before paracetamol To evaluate the protective effect of doxazosin against paracetamol-induced hepatotoxicity. Results showed that doxazosin significantly reduced serum ALT activity, indicating hepatoprotective effects. PMC2259197
C57BL/6 mice Carbon tetrachloride (CCl4)-induced mouse liver fibrosis model Gavage 2.5, 5, 10 mg/(kg*day) Once daily for 20 weeks Doxazosin improved the survival rates of CCl4-induced mice and alleviated pathological damage associated with liver fibrosis. PMC8387324
Zebrafish larvae Adgrl3.1 mutant model System water 0.1 µM, 1 µM, 10 µM, 30 µM, 100 µM Single administration, 1 hour before recording To evaluate the rescue effect of Doxazosin on the hyperactive phenotype of adgrl3.1 mutant zebrafish larvae. Results showed that all tested doses significantly reduced the average distance moved in mutant larvae. PMC10267219

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT00285519 Hypertension Phase 4 Completed - Japan ... More >> Division of Cardiovascular Medicine, Department of Medicine, Jichi Medical University School of Medicine Shimotsuke, Tochigi, Japan, 329-0498 Less <<
NCT00295542 Hypertension Phase 4 Completed - Spain ... More >> Hospital Clinico Universitario Santiago de Compostela, Spain, 15706 Less <<
NCT00741585 Essential Hypertension ... More >> Cardiovascular Disease Stroke Chronic Kidney Disease Less << Phase 4 Completed - Spain ... More >> CS Friol Friol, Lugo, Spain, 27220 CS Baiona Baiona, Pontevedra, Spain, 36300 CS Bueu Bueu, Pontevedra, Spain, 36930 CS A Estrada La Estrada, Pontevedra, Spain, 26680 CS A Guarda La Guardia, Pontevedra, Spain, 36780 CS Valmiñor Nigran, Pontevedra, Spain, 36250 CS Panxón Nigrán, Pontevedra, Spain, 36340 CS Tomiño Tomiño, Pontevedra, Spain, 36200 Bioengineering & Chronobilogy Labs., University of Vigo Vigo, Pontevedra, Spain, 36200 Hospital do Meixoeiro Vigo, Pontevedra, Spain, 36200 CS Calle Cuba Vigo, Pontevedra, Spain, 36202 CS A Doblada Vigo, Pontevedra, Spain, 36205 CS Coia Vigo, Pontevedra, Spain, 36209 CS Sardoma Vigo, Pontevedra, Spain, 36214 CS Teis Vigo, Pontevedra, Spain, 36216 CS Vilaboa Vilaboa, Pontevedra, Spain, 36141 CS San Roque Vilagarcía De Arousa, Pontevedra, Spain, 36600 CS Fingoi Lugo, Spain, 27002 Complexo Hospitalario Universitario de Ourense Orense, Spain, 32005 CS Lerez Pontevedra, Spain, 36156 Less <<
NCT00004266 Diabetic Nephropathy Phase 3 Completed - United States, Minnesota ... More >> Hennepin County Medical Center Minneapolis, Minnesota, United States, 55415 Less <<
NCT00661895 Hypertension Phase 4 Completed - United States, Nebraska ... More >> Creighton Community Health Center Omaha, Nebraska, United States, 68104 Less <<
NCT00563901 - Completed - United States, Minnesota ... More >> University of Minnesota Minneapolis, Minnesota, United States, 55455 United States, Texas University of Texas Houston Houston, Texas, United States, 77030 Less <<
NCT00000522 Cardiovascular Diseases ... More >> Heart Diseases Hypertension Vascular Diseases Less << Phase 2 Completed - -
NCT00661895 - Completed - -
NCT01323998 - Completed - -
NCT00535925 Diabetic Nephropathy Phase 4 Unknown September 2012 Italy ... More >> Department of Clinical and Experimental Medicine, Second University of Naples Naples, Italy, I-80131 Less <<
NCT01323998 - Completed - -
NCT01819220 Hypertension Phase 4 Completed - Korea, Republic of ... More >> Yonsei universty medical center Seoul, Korea, Republic of, 120-752 Less <<
NCT00684489 Hypertension Not Applicable Completed - -
NCT00000542 Cardiovascular Diseases ... More >> Coronary Disease Diabetes Mellitus Heart Diseases Hypercholesterolemia Hypertension Myocardial Infarction Myocardial Ischemia Heart Failure Less << Phase 3 Completed - -
NCT01332487 - Completed - -
NCT01332435 - Completed - -
NCT01332487 - Completed - -
NCT01386983 - Completed - -
NCT00141596 Hypertension Not Applicable Terminated(Insufficient accrua... More >>l rate) Less << - United Kingdom ... More >> Blood Pressure Unit, Dept. Cardiac & Vascular Sciences, SGUL London, United Kingdom, SW17 0RE Less <<
NCT01390870 - Completed - -
NCT01332435 - Completed - -
NCT01435954 - Completed - -
NCT00424801 Microvascular Angina ... More >> Hypertension Less << Not Applicable Terminated(Due to recent findi... More >>ngs relating MRI contrast to nephrogenic systemic fibrosis) Less << December 2008 Denmark ... More >> Aarhus Hospital Aarhus, Denmark, 8000 Less <<
NCT01589484 Urolithiasis ... More >>Urinary Lithiasis Kidney Calculi Less << Not Applicable Completed - Brazil ... More >> University of Sao Paulo Sao Paulo, SP, Brazil Less <<
NCT01589484 - Completed - -
NCT01386983 - Completed - -
NCT00687388 Benign Prostatic Hyperplasia Phase 4 Withdrawn(in order to prepare ... More >>a new clinical trial to evaluate with pathological change) Less << - Korea, Republic of ... More >> Severance Hospital Seoul, Korea, Republic of, 120-752 Samsung Medical Center Seoul, Korea, Republic of, 135-710 Asan Medical Center Seoul, Korea, Republic of, 138-736 Less <<
NCT00713739 Kidney Stones Phase 3 Unknown December 2012 United States, California ... More >> Naval Medical Center San Diego Recruiting San Diego, California, United States, 92134 Contact: Brian K Auge, M.D.    619-532-7200       Contact: Sean P. Stroup, M.D.    619-532-7200       Principal Investigator: Brian K. Auge, M.D.          Principal Investigator: Sean P. Stroup, M.D. Less <<
NCT00006294 - Completed - United States, Kentucky ... More >> University of Kentucky Lexington, Kentucky, United States, 40536 Less <<
NCT03043612 Urolithiasis Not Applicable Completed - Hong Kong ... More >> Prince of Wales/Chinese University of Hong Kong Sha Tin, Hong Kong Less <<
NCT01661621 Bladder Outlet Obstruction Phase 4 Completed - Taiwan ... More >> Buddhist Tzu Chi General Hospital Hualien, Taiwan, 970 Less <<
NCT02266537 Healthy Phase 1 Completed - -
NCT01661621 - Completed - -
NCT01390870 - Completed - -
NCT01798992 - Completed - -
NCT01798992 Idiopathic Dilated Cardiomyopa... More >>thy Less << Phase 4 Completed - United States, Colorado ... More >> University of Colorado Hospital Denver, Colorado, United States, 80220 United States, Utah University of Utah Medical Center Salt Lake City, Utah, United States, 84132 Less <<
NCT00021814 Prostatic Hyperplasia ... More >> Prostatic Hypertrophy, Benign Less << Phase 3 Completed - United States, California ... More >> University of California La Jolla, California, United States, 92093-0694 United States, Colorado Univ of Colorado Health Sciences Center Aurora, Colorado, United States, 80010-0510 United States, Connecticut Yale University New Haven, Connecticut, United States, 06520 United States, District of Columbia Walter Reed Army Medical Center Washington, District of Columbia, United States, 20307 United States, Georgia Emory University Atlanta, Georgia, United States, 30322 United States, Illinois Northwestern University Chicago, Illinois, United States, 60611 United States, Iowa University of Iowa Hospitals Clinics Iowa City, Iowa, United States, 52242 United States, Maryland University of Maryland Baltimore, Maryland, United States, 21201 United States, Michigan Henry Ford Health Systems Detroit, Michigan, United States, 48202 United States, Minnesota Mayo Foundation Rochester, Minnesota, United States, 55905 United States, Missouri Washington University Saint Louis, Missouri, United States, 63141 United States, New York New York University School of Medicine New York, New York, United States, 10010 Columbia Presbyterian Medical Center New York, New York, United States, 10032 United States, Tennessee Vanderbilt University Nashville, Tennessee, United States, 37232-2765 United States, Texas UT Southwestern Medical Center Dallas, Texas, United States, 5235-9110 Baylor College of Medicine Houston, Texas, United States, 77005 Brooke Army Medical Center San Antonio, Texas, United States, 78234-6200 Less <<
NCT00517179 Prostatic Hyperplasia ... More >> Impotence Less << Not Applicable Completed - China ... More >> Prince of Wales Hospital Hong Kong, China Less <<
NCT00645034 Benign Prostatic Hyperplasia Phase 2 Completed - United States, California ... More >> Pfizer Investigational Site Laguna Woods, California, United States, 92653 Pfizer Investigational Site Newport Beach, California, United States, 92660 Less <<
NCT00563485 Prostatic Hyperplasia ... More >> Urinary Retention Less << Not Applicable Terminated - China ... More >> Prince of Wales Hospital Hong Kong, China Less <<
NCT00648323 Prostate Phase 4 Completed - Taiwan ... More >> Pfizer Investigational Site Kaohsiung, Taiwan, 813 Pfizer Investigational Site Taichung, Taiwan Pfizer Investigational Site Taipei, Taiwan Pfizer Investigational Site Taoyuan, Taiwan Less <<
NCT02538744 Cocaine Dependence Phase 1 Unknown - United States, Texas ... More >> Michael Debakey VA Medical Center Recruiting Houston, Texas, United States, 77030 Contact: Thomas Newton, MD    713-791-1414 ext x6498    tnewton@bcm.edu    Principal Investigator: Thomas Newton, MD Less <<
NCT00130156 High Blood Pressure Phase 4 Completed - Taiwan ... More >> National Taiwan University Hospital. Taipei, Taiwan Less <<
NCT00295555 Diabetes Mellitus ... More >> Essential Hypertension Renal Failure Less << Phase 4 Completed - Japan ... More >> Yokohama City University Center Hospital Yokohama, Japan, 232-0024 Less <<
NCT02369081 Hypertension, Resistant to Con... More >>ventional Therapy Less << Phase 4 Unknown August 2015 United Kingdom ... More >> NHS Ayrshire Ayrshire, United Kingdom University Hospitals Birmingham NHS Foundation Trust Birmingham, United Kingdom University of Birmingham Birmingham, United Kingdom University of Cambridge - Addenbrookes Hospital Cambridge, United Kingdom, CB2 2QQ NHS Tayside/University of Dundee Dundee, United Kingdom NHS Lothian/University of Edinburgh Edinburgh, United Kingdom Royal Devon & Exeter NHS Foundation Trust Exeter, United Kingdom NHS Greater Glasgow and Clyde/University of Glasgow Glasgow, United Kingdom Ixworth GP Practice Ixworth, United Kingdom University Hospitals of Leicester NHS Trust Leicester, United Kingdom Barts and the London School of Medicine and Dentistry London, United Kingdom Guys and St Thomas' NHS Foundation Trust London, United Kingdom Imperial College Healthcare NHS Trust London, United Kingdom Central Manchester University Hospitals NHS Foundation Trust Manchester, United Kingdom Norfolk and Norwich University Hospital NHS Trust Norwich, United Kingdom West Hertfordshire Hospitals NHS Trust Watford, United Kingdom Less <<
NCT03176693 Pheochromocytoma ... More >> Paraganglioma Less << Phase 3 Recruiting May 2024 United States, California ... More >> University of California, Los angeles Recruiting Los Angeles, California, United States, 90025 Principal Investigator: Masha J Livhits, MD          Sub-Investigator: Eric J Kuo, MD Less <<
NCT01678313 - Completed - -
NCT01100021 Erectile Dysfunction Phase 1 Completed - United States, Arizona ... More >> MDS Pharma Services Inc., Tempe, Arizona, United States, 85283 Less <<
NCT01678313 Benign Prostatic Hyperplasia Phase 2 Completed - Taiwan ... More >> Buddhist Tzu Chi General Hospital Hualien, Taiwan, 970 Less <<
NCT02563405 Hypertension Phase 2 Phase 3 Unknown October 2018 China, Heilongjiang ... More >> uric acid test and 24-hour ambulatory BP monitoring Recruiting Harbin, Heilongjiang, China, 150001 Contact: Yujiao Pan, MM    86-451-85555671    panyujiao@163.com Less <<
NCT01946035 Allergic Rhinitis Phase 4 Completed - United Kingdom ... More >> Brian Lipworth Dundee, United Kingdom, DD1 3AU Less <<
NCT01389609 Hypertension Phase 1 Completed - Japan ... More >> Pfizer Investigational Site Shinjuku-ku, Tokyo, Japan Less <<
NCT03415581 Opioid-use Disorder Phase 2 Recruiting March 30, 2020 United States, New York ... More >> Jermaine Jones Recruiting Manhattan, New York, United States, 10032 Contact: Jermaine Jones    646-774-6113    jermaine.jones@NYSPI.Columbia.edu    Principal Investigator: Sandra D Comer, PhD Less <<
NCT02785393 Substance-Related Disorders Phase 1 Completed - United States, Texas ... More >> Michael Debakey VA Medical Center Houston, Texas, United States, 77030 Less <<
NCT01953432 Cocaine Dependence Phase 2 Completed - United States, Texas ... More >> Michael E. DeBakey VA Medical Center, Houston, TX Houston, Texas, United States, 77030 Less <<
NCT00730418 Benign Prostatic Hyperplasia Not Applicable Completed - Korea, Republic of ... More >> Samsung Medical Center SEoul, Korea, Republic of, 135-710 Less <<
NCT02308202 PTSD Phase 1 Recruiting December 31, 2018 United States, Texas ... More >> Baylor College of Medicine Recruiting Houston, Texas, United States, 77030 Less <<
NCT01371851 Methamphetamine or Cocaine Dep... More >>endence Less << Phase 1 Phase 2 Completed - United States, Arkansas ... More >> UAMS Psychiatric Research Institute Little Rock, Arkansas, United States, 72205 Less <<
NCT00922506 Overactive Bladder ... More >> Benign Prostatic Hyperplasia Less << Phase 4 Unknown November 2015 Korea, Republic of ... More >> Samsung Medical Center Recruiting Seoul, Korea, Republic of, 135-710 Contact: Kyu-Sung Lee, Ph.D    82-2-3410-3554    ksleedr@skku.edu    Principal Investigator: Kyu-Sung Lee, Ph.D Less <<
NCT00646841 Hypertension Phase 4 Completed - Italy ... More >> Pfizer Investigational Site Brescia, Italy, 25123 Pfizer Investigational Site Monza (Milan), Italy, 20052 Pfizer Investigational Site Padova, Italy, 35128 Spain Pfizer Investigational Site Palamos, Gerona, Spain, 17230 Pfizer Investigational Site Madrid, Spain, 28041 United Kingdom Pfizer Investigational Site London, United Kingdom, EC1M 6BQ Less <<
NCT01379898 Pheochromocytoma Phase 4 Completed - Netherlands ... More >> Department of Endocrinology, University Medical Center Groningen Groningen, Netherlands, 9700 RB Less <<
NCT02901977 Hypertension Phase 4 Completed - Sweden ... More >> Karolinska Institutet, Daprtment of Clinical Sciences, Danderyd Hospital, Cardiovascular Research Laboratory Stockholm, Sweden, SE-182 88 Less <<
NCT02989493 Alcoholism Phase 2 Recruiting December 2020 United States, Wisconsin ... More >> University of Wisconsin Recruiting Madison, Wisconsin, United States, 53706 Contact: John J Curtin, PhD    608-262-0387    jjcurtin@wisc.edu    Principal Investigator: John J Curtin, PhD Less <<
NCT00880997 Cocaine Dependence Phase 1 Completed - United States, Texas ... More >> Baylor College of Medicine - Michael E. DeBakey VA Medical Center Houston, Texas, United States, 77030 Less <<
NCT01730846 - Completed - -
NCT01386177 Mood Disorder ... More >> Substance-Related Disorders Amphetamine-Related Disorders Less << Phase 1 Completed - Switzerland ... More >> University Hospital Basel Basel, Switzerland, 4031 Less <<
NCT01437046 Alcohol Dependence ... More >> Anxiety Less << Phase 2 Completed - United States, Rhode Island ... More >> Brown University Center for Alcohol and Addiction Studies Providence, Rhode Island, United States, 02903 Less <<
NCT01730846 Smoking Phase 2 Completed - United States, Connecticut ... More >> Yale Center for Clinical Investigations, Yale University New Haven, Connecticut, United States, 06519 Less <<
NCT01145183 Cocaine Dependence Phase 2 Completed - United States, Texas ... More >> Baylor College of Medicine Houston, Texas, United States, 77030 Less <<
NCT02500602 Posttraumatic Stress Disorder ... More >> Alcohol Use Disorders Less << Phase 2 Recruiting March 1, 2019 United States, South Carolina ... More >> Ralph H. Johnson VA Medical Center, Charleston, SC Recruiting Charleston, South Carolina, United States, 29401-5799 Contact: Nichole N Mazzulo, MS BA    843-577-5011 ext 7193    nichole.mazzulo@va.gov    Principal Investigator: Sudie E. Back, PhD Less <<
NCT03398252 Alcohol Use Disorder Phase 1 Not yet recruiting January 2021 United States, Texas ... More >> The University of Texas Health Science Center at Houston Not yet recruiting Houston, Texas, United States, 77030 Contact: Jin Ho Yoon, PhD    713-486-2858    Jin.Ho.Yoon@uth.tmc.edu Less <<
NCT01371851 - Completed - -
NCT01062945 Cocaine Addiction ... More >> Cocaine Abuse Cocaine Dependence Substance Abuse Less << Phase 1 Completed - United States, Texas ... More >> Michael Debakey VA Medical Center Houston, Texas, United States, 77030 Less <<
NCT01959022 Stress Disorders, Post-Traumat... More >>ic Less << Phase 4 Completed - United States, California ... More >> San Francisco Veterans Affairs Medical Center San Francisco, California, United States, 94121 Less <<
NCT02492334 PTSD Alcohol ... More >>Use Disorder Less << Phase 1 Phase 2 Recruiting March 2019 United States, South Carolina ... More >> Addiction Sciences Division-Medical University of South Carolina Recruiting Charleston, South Carolina, United States, 29425 Contact: Megan M Moran-Santa Maria, Ph.D.       moranm@musc.edu    Contact: Francis M Beylotte, MS    8437922522 ext Beylotte    beylott@musc.edu    Sub-Investigator: Julianne Flanagan, Ph.D.          Principal Investigator: Sudie Back, Ph.D. Less <<
NCT03339258 Stress Disorders, Post-Traumat... More >>ic Less << Phase 2 Recruiting June 2021 United States, California ... More >> San Francisco VA Medical Center Recruiting San Francisco, California, United States, 94121 Contact: Andrew Levihn-Coon, B.A.    415-221-4810 ext 23809    andrew.levihn-coon@va.gov Less <<
NCT01003886 - Completed - -
NCT01003886 - Completed - -

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.83mL

0.37mL

0.18mL

9.13mL

1.83mL

0.91mL

18.26mL

3.65mL

1.83mL

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

References

 

Historical Records

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