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Chemical Structure| 117928-94-6 Chemical Structure| 117928-94-6

Structure of Rapastinel
CAS No.: 117928-94-6

Chemical Structure| 117928-94-6

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Rapastinel is a putative NMDAR functional glycine-site partial agonist.

Synonyms: GLYX-13; BV-102; TPPT-amide

4.5 *For Research Use Only !

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Product Details of Rapastinel

CAS No. :117928-94-6
Formula : C18H31N5O6
M.W : 413.47
SMILES Code : O=C([C@@H]1CCCN1C([C@H]([C@@H](C)O)N)=O)N2CCC[C@H]2C(N[C@@H]([C@@H](C)O)C(N)=O)=O
Synonyms :
GLYX-13; BV-102; TPPT-amide
MDL No. :MFCD12912477
InChI Key :GIBQQARAXHVEGD-BSOLPCOYSA-N
Pubchem ID :14539800

Safety of Rapastinel

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
CA1 pyramidal cells 1 μM 25–30 min GLYX-13 reduced inhibitory input onto CA1 pyramidal cells and increased synaptically driven pyramidal cell excitability. PMC5879689
Rat cortical neurons 10-300 nM Rapastinel enhanced NMDA-induced calcium influx PMC6403082
HEK cells 30-100 nM Rapastinel enhanced NMDAR-dependent neuronal intracellular calcium mobilization PMC6403082

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Long-term isoflurane exposure-induced cognitive impairment model Intravenous injection 1 mg/kg Single dose, lasting 2 hours GLYX-13 pretreatment alleviates isoflurane-induced cognitive dysfunction by protecting against perturbation of the NR2B/CaMKII/CREB signaling pathway PMC6862406
Rats Depression model Subcutaneous injection 10 and 30 mg/kg Single dose Rapastinel produced rapid and sustained antidepressant-like effects in rat mPFC PMC6403082
Mice Chronic unpredictable stress (CUS) model Intravenous injection 0.5, 5, and 10 mg/kg 3 consecutive days Rapastinel significantly reversed CUS-induced depression-like behaviors and produced antidepressant effects by enhancing ERK/mTOR/VGF/BDNF/TrkB signaling. PMC9780240

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT01234558 Major Depressive Disorder PHASE2 COMPLETED 2025-07-12 Mulitple, Evanston, Illinois, ... More >>60201, United States Less <<
NCT03668600 Depressive Disorder, Major PHASE3 TERMINATED 2019-07-03 University of Alabama at Birmi... More >>ngham, Birmingham, Alabama, 35294, United States|Harmonex Neuroscience Research, Dothan, Alabama, 36303, United States|NoesisPharma, Phoenix, Arizona, 85016, United States|Woodland International Research Group, Little Rock, Arkansas, 72211, United States|Woodland Research Northwest, Rogers, Arkansas, 72758, United States|California Pharmaceutical Research Institute, Inc, Anaheim, California, 92804, United States|Southern California Research LLC., Beverly Hills, California, 90036, United States|ATP Clinical Research Inc., Costa Mesa, California, 92626, United States|ProScience Research Group, Culver City, California, 90230, United States|Pharmacology Research Institute, Encino, California, 91316, United States|Behavioral Research Specialists, LLC, Glendale, California, 91206, United States|Sun Valley Research Center, Imperial, California, 92251, United States|Irvine Center for Clinical Research, Inc, Irvine, California, 92614, United States|Synergy Clinical Research Center of Escondido, Lemon Grove, California, 91945, United States|Pharmacology Research Institute, Los Alamitos, California, 90720, United States|CITrials, Riverside, California, 92506, United States|California Neuroscience Research, Sherman Oaks, California, 91403, United States|Viking Clinical Research, Temecula, California, 92591, United States|Pacific Clinical Research Medical, Upland, California, 91786, United States|Comprehensive Psychiatric Care, Norwich, Connecticut, 06360, United States|Gulfcoast Clinical Research Center, Fort Myers, Florida, 33912, United States|Reliable Clinical Research, Hialeah, Florida, 33012, United States|Meridien Research, Lakeland, Florida, 33805, United States|Innovative Clinical Research, Inc, Lauderhill, Florida, 33319, United States|Research Centers of America, Oakland Park, Florida, 33334, United States|Medical Research Group of Central Florida, Orange City, Florida, 32763, United States|David A. Medina, MD, Orlando, Florida, 32819, United States|Institute for Advanced Medical Research, Atlanta, Georgia, 30341, United States|iResearch Atlanta, LLC, Decatur, Georgia, 30030, United States|Northwest Behavioral Research Center, Marietta, Georgia, 30060, United States|Attalla Consultants, LLC, Smyrna, Georgia, 30082, United States|Alexian Brothers Center for Psychiatric Research, Hoffman Estates, Illinois, 60169, United States|Capstone Clinical Research, Libertyville, Illinois, 60048, United States|AMR - Baber Research, Inc., Naperville, Illinois, 60563, United States|University of Kansas School of Medicine Clinical Trial Unit, Wichita, Kansas, 67214, United States|Lake Charles Clinical Trials, Lake Charles, Louisiana, 70629, United States|Louisiana Clinical Research, Shreveport, Louisiana, 71101, United States|ActivMed Practices & Research, Inc., Methuen, Massachusetts, 01844, United States|Coastal Research Associates, South Weymouth, Massachusetts, 02190, United States|University of Massachusetts Medical School, Worcester, Massachusetts, 01655, United States|Precise Research Centers, Flowood, Mississippi, 39232, United States|Psychiatric Care and Research Center, O'Fallon, Missouri, 63368, United States|St. Charles Psychiatric Associates, Saint Charles, Missouri, 63304, United States|Premier Psychiatric Research Institute, LLC, Lincoln, Nebraska, 68526, United States|Healthy Perspectives - Innovative Mental Health Services. PLLC, Nashua, New Hampshire, 03060, United States|Bio Behavioral Health, Toms River, New Jersey, 08755, United States|Albuquerque Neuroscience, Inc, Albuquerque, New Mexico, 87109, United States|SPRI Clinical Trials, LLC, Brooklyn, New York, 11235, United States|Manhattan Behavioral Medicine, New York, New York, 10022, United States|Finger Lakes Clinical Research, Rochester, New York, 14618, United States|Richmond Behavioral Associates, Staten Island, New York, 10312, United States|Patient Priority Clinical Sites, Cincinnati, Ohio, 45215, United States|The Ohio State University Department of Psychiatry, Columbus, Ohio, 43210, United States|Midwest Clinical Research Center LLC, Dayton, Ohio, 45417, United States|Professional Psychiatric Services, Mason, Ohio, 45040, United States|Red River Medical Research Center, LLC, Oklahoma City, Oklahoma, 73112, United States|Sooner Clinical Research, Inc, Oklahoma City, Oklahoma, 73112, United States|Paradigm Research Professionals, Oklahoma City, Oklahoma, 73118, United States|Summit Research Network LLC, Portland, Oregon, 97210, United States|Lehigh Center for Clinical Research, Allentown, Pennsylvania, 18104, United States|Dr. Cherian Verghese, Norristown, Pennsylvania, 19403, United States|Carolina Clinical Trials, Inc., Charleston, South Carolina, 29407, United States|Coastal Carolina Research Center, Mount Pleasant, South Carolina, 29464, United States|Research Strategies of Memphis, LLC, Memphis, Tennessee, 38119, United States|Donald J. Garcia, Jr., MD, PA, Austin, Texas, 78737, United States|Community Clinical Research, Austin, Texas, 78754, United States|Houston Clinical Trials, Bellaire, Texas, 77401, United States|North Texas Clinical Trials, Fort Worth, Texas, 76104, United States|Earle Research, Houston, Texas, 77058, United States|Red Oak Psychiatry Associates, PA, Houston, Texas, 77090, United States|Clinical Trials of Texas, San Antonio, Texas, 78229, United States|Grayline Clinical Drug Trials, Wichita Falls, Texas, 76309, United States|Psychiatric and Behavioral Solutions, Salt Lake City, Utah, 84105, United States|Psychiatric Alliance of the Blue Ridge, Inc, Charlottesville, Virginia, 22903, United States Less <<
NCT03002077 Depressive Disorder, Major PHASE3 COMPLETED 2018-12-06 University of Alabama at Birmi... More >>ngham, Birmingham, Alabama, 35294, United States|Harmonex, Inc., Dothan, Alabama, 36303, United States|NoesisPharma, Phoenix, Arizona, 85032, United States|Woodland International Research Group, Little Rock, Arkansas, 72211, United States|Woodland Research Northwest, Rogers, Arkansas, 72758, United States|California Pharmaceutical Research Institute, Inc, Anaheim, California, 92804, United States|Southern California Research LLC., Beverly Hills, California, 90036, United States|ATP Clinical Research Inc., Costa Mesa, California, 92626, United States|ProScience Research Group, Culver City, California, 90230, United States|Collaborative Neuroscience Network, LLC, Garden Grove, California, 92845, United States|Behavioral Research Specialists, LLC, Glendale, California, 91206, United States|Sun Valley Research Center, Imperial, California, 92251, United States|Irvine Center for Clinical Research, Inc, Irvine, California, 92614, United States|Synergy Clinical Research Center of Escondido, Lemon Grove, California, 91945, United States|Synergy San Diego, Lemon Grove, California, 91945, United States|Pharmacology Research Institute, Los Alamitos, California, 90720, United States|Pacific Research Partners; LLC., Oakland, California, 94607, United States|Excell Research, Oceanside, California, 92056, United States|NRC Research Institute, Orange, California, 92868, United States|Asclepes Research Centers, Panorama City, California, 91402, United States|Anderson Clinical Research, Redlands, California, 92374, United States|CITrials, Riverside, California, 92506, United States|Artemis Institute for Clinical Research, San Diego, California, 92103, United States|PCSD Feighner Research, San Diego, California, 92108, United States|Artemis Institute for Clinical Research, San Marcos, California, 92078, United States|Thomas M. Shiovitz, M.D., Inc., DBA California Neuroscience Research Medical Group, Inc.,, Sherman Oaks, California, 91403, United States|Viking Clinical Research, Temecula, California, 92591, United States|Pacific Clinical Research Medical, Upland, California, 91786, United States|MCB Clinical Research Center, Colorado Springs, Colorado, 80910, United States|Comprehensive Psychiatric Care, Norwich, Connecticut, 06360, United States|Meridien Research, Bradenton, Florida, 34201, United States|Gulfcoast Clinical Research Center, Fort Myers, Florida, 33912, United States|Sarkis Clinical Trials, Gainesville, Florida, 32607, United States|MD Clinical, Hallandale Beach, Florida, 33009, United States|Reliable Clinical Research, Hialeah, Florida, 33012, United States|Clinical Neuroscience Solutions, Inc, Jacksonville, Florida, 32256, United States|Meridien Research, Lakeland, Florida, 33805, United States|Innovative Clinical Research, Inc, Lauderhill, Florida, 33319, United States|Innova Clinical Trials Inc., Miami, Florida, 33145, United States|International Research Associates, LLC, Miami, Florida, 33183, United States|Research Centers of America, Oakland Park, Florida, 33334, United States|Medical Research Group of Central Florida, Orange City, Florida, 32763, United States|Clinical Neuroscience Solutions, Inc, Orlando, Florida, 32801, United States|Combined Research Orlando Phase I-IV, Orlando, Florida, 32807, United States|Millenia Psychiatry & Research, Inc, Orlando, Florida, 32839, United States|Olympian Clinical Research, Tampa, Florida, 33609, United States|University of South Florida, Psychiatry and Behavioral Neurosciences, Tampa, Florida, 33613, United States|Institute for Advanced Medical Research, Atlanta, Georgia, 30005, United States|Atlanta Center for Medical Research, Atlanta, Georgia, 30331, United States|iResearch Atlanta, LLC, Decatur, Georgia, 30030, United States|Northwest Behavioral Research Center, Marietta, Georgia, 30060, United States|Iris Research, Smyrna, Georgia, 30080, United States|Great Lakes Clinical Trials, Chicago, Illinois, 60640, United States|Alexian Brothers Center for Psychiatric Research, Hoffman Estates, Illinois, 60169, United States|Capstone Clinical Research, Libertyville, Illinois, 60048, United States|AMR - Baber Research, Inc., Naperville, Illinois, 60563, United States|Psychiatric Associates, Overland Park, Kansas, 66211, United States|Heartland Research Associates, Wichita, Kansas, 67207, United States|Lake Charles Clinical Trials, Lake Charles, Louisiana, 70629, United States|Louisiana Clinical Research, Shreveport, Louisiana, 71101, United States|J Gary Booker, MD APMC, Shreveport, Louisiana, 71104, United States|Sheppard Pratt Health System, Baltimore, Maryland, 21204, United States|Pharmasite Research, Inc, Baltimore, Maryland, 21208, United States|CBH Health, Gaithersburg, Maryland, 20850, United States|Boston Clinical Trials, Boston, Massachusetts, 02131, United States|ActivMed Practices & Research, Inc., Methuen, Massachusetts, 01844, United States|Coastal Research Associates, South Weymouth, Massachusetts, 02190, United States|Adams Clinical Trials, Watertown, Massachusetts, 02472, United States|University of Massachusetts Medical School, Worcester, Massachusetts, 01655, United States|Precise Research Centers, Flowood, Mississippi, 39232, United States|Psychiatric Care and Research Center, O'Fallon, Missouri, 63368, United States|St. Charles Psychiatric Associates - Midwest Research Group, Saint Charles, Missouri, 63304, United States|Millennium Psychiatric Associates, Saint Louis, Missouri, 63141, United States|Premier Psychiatric Research Institute, LLC, Lincoln, Nebraska, 68526, United States|Altea Research, Las Vegas, Nevada, 89102, United States|Healthy Perspectives - Innovative Mental Health Services. PLLC, Nashua, New Hampshire, 03060, United States|Hassman Research Institute, LLC, Berlin, New Jersey, 08009, United States|Center for Emotional Fitness, Cherry Hill, New Jersey, 08002, United States|Pharmaceutical Research Associates Inc, Marlton, New Jersey, 08053, United States|Global Medical Institute, LLC, Princeton, New Jersey, 08540, United States|Bio Behavioral Health, Toms River, New Jersey, 08755, United States|Albuquerque Neuroscience, Inc, Albuquerque, New Mexico, 87109, United States|SPRI Clinical Trials, Inc, Brooklyn, New York, 11235, United States|Bioscience Research, Mount Kisco, New York, 10549, United States|Manhattan Behavioral Medicine, New York, New York, 10022, United States|Eastside Comprehensive Medical Center, LLC, New York, New York, 10128, United States|The Medical Research Network, LLC, New York, New York, 10128, United States|Fieve Clinical Research, New York, New York, 10168, United States|Finger Lakes Clinical Research, Rochester, New York, 14618, United States|Richmond Behavioral Associates, Staten Island, New York, 10312, United States|Carolina Clinical Trials, Inc., Charleston, North Carolina, 29407, United States|New Hope Clinical Research Inc., Charlotte, North Carolina, 28211, United States|Richard H. Weisler, MD, PA, Raleigh, North Carolina, 27609, United States|Neuro-Behavioral Clinical Research, Inc, Canton, Ohio, 44718, United States|Patient Priority Clinical Site, LLC, Cincinnati, Ohio, 45215, United States|The Ohio State University Department of Psychiatry, Columbus, Ohio, 43210, United States|Midwest Clinical Research Center LLC, Dayton, Ohio, 45417, United States|Charak Clinical Research Center, Garfield Heights, Ohio, 44125, United States|Lindner Center of Hope, Mason, Ohio, 45040, United States|Professional Psychiatric Services, Mason, Ohio, 45040, United States|IPS Research, Oklahoma City, Oklahoma, 73103, United States|Red River Medical Research Center, LLC, Oklahoma City, Oklahoma, 73112, United States|Sooner Clinical Research, Inc, Oklahoma City, Oklahoma, 73112, United States|Paradigm Research Professionals, Oklahoma City, Oklahoma, 73118, United States|Summit Research Network, Portland, Oregon, 97210, United States|Lehigh Center for Clinical Research, Allentown, Pennsylvania, 18104, United States|Suburban Research Associates, Media, Pennsylvania, 19063, United States|Keystone Clinical Studies, LLC, Norristown, Pennsylvania, 20006, United States|Coastal Carolina Research Center, Inc., Mount Pleasant, South Carolina, 29464, United States|Clinical Neuroscience Solutions, Inc, Memphis, Tennessee, 38119, United States|Research Strategies of Memphis, LLC, Memphis, Tennessee, 38119, United States|Donald J. Garcia, Jr., MD, PA, Austin, Texas, 78737, United States|Community Clinical Research, Inc., Austin, Texas, 78754, United States|BioBehavioral Research of Austin, Austin, Texas, 78759, United States|Houston Clinical Trials, LLC, Bellaire, Texas, 77401, United States|Relaro Medical Trials, Dallas, Texas, 75243, United States|El Campo Clinical Trials, El Campo, Texas, 77347, United States|North Texas Clinical Trials, Fort Worth, Texas, 76104, United States|Earle Research, Houston, Texas, 77058, United States|Red Oak Psychiatry Associates, PA, Houston, Texas, 77090, United States|Clinical Trials of Texas, San Antonio, Texas, 78229, United States|Family Psychiatry of The Wood, The Woodlands, Texas, 77381, United States|Grayline Clinical Drug Trials, Wichita Falls, Texas, 76309, United States|Psychiatric and Behavioral Solutions, Salt Lake City, Utah, 84105, United States|Pharmaceutical Research Associates, Inc, Salt Lake City, Utah, 84106, United States|Psychiatric Alliance of the Blue Ridge, Inc., Charlottesville, Virginia, 22903, United States|NorthWest Clinical Research Center, Bellevue, Washington, 98007, United States|Pacific Institute of Medical Sciences, Bothell, Washington, 98011, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.42mL

0.48mL

0.24mL

12.09mL

2.42mL

1.21mL

24.19mL

4.84mL

2.42mL

References

 

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