ArticleJournal of medicinal chemistry2020
Application of Fluorine- and Nitrogen-Walk Approaches: Defining the Structural and Functional Diversity of 2-Phenylindole Class of Cannabinoid 1 Receptor Positive Allosteric Modulators.
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Article in Journal of medicinal chemistry, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 25 papers.
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25 citing papers in PubMed, 59 citations in OpenAlex.
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- Functional dynamics of G protein-coupled receptors reveal new routes for drug discovery.Nature reviews. Drug discovery · 2025Review
- Discovery and mechanism verification of first-in-class hydrophobic tagging-based degraders of HBV core protein.Acta pharmaceutica Sinica. B · 2025Article
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- Discovery of 6α-Thiazolylcarboxamidonaltrexamine Derivative (NTZ) as a Potent and Central Nervous System Penetrant Opioid Receptor Modulator with Drug-like Properties for Potential Treatment of Opioid Use Disorder.ACS pharmacology & translational science · 2024Article
- Determination of the Cannabinoid CB1 Receptor's Positive Allosteric Modulator Binding Site through Mutagenesis Studies.Pharmaceuticals (Basel, Switzerland) · 2024Article
- New Insights into Bitopic Orthosteric/Allosteric Ligands of Cannabinoid Receptor Type 2.International journal of molecular sciences · 2023Article
- In Vitro Characterization of 6-Methyl-3-(2-nitro-1-(thiophen-2-yl)ethyl)-2-phenyl-1ACS pharmacology & translational science · 2022Article
- Design, Synthesis, and Biological Activity of New CB2 Receptor Ligands: from Orthosteric and Allosteric Modulators to Dualsteric/Bitopic Ligands.Journal of medicinal chemistry · 2022Article
- The type 1 cannabinoid receptor positive allosteric modulators GAT591 and GAT593 reduce spike-and-wave discharges in Genetic Absence Epilepsy Rats from Strasbourg.IBRO neuroscience reports · 2022Article
- The endocannabinoid system impacts seizures in a mouse model of Dravet syndrome.Neuropharmacology · 2022Article
- Pharmacological evaluation of enantiomerically separated positive allosteric modulators of cannabinoid 1 receptor, GAT591 and GAT593.Frontiers in pharmacology · 2022Article
- Modulation of type 1 cannabinoid receptor activity by cannabinoid by-products fromFrontiers in pharmacology · 2022Article
- Design, synthesis and biological evaluation of novel orthosteric-allosteric ligands of the cannabinoid receptor type 2 (CBFrontiers in chemistry · 2022Article
- CB1 Cannabinoid Receptor Signaling and Biased Signaling.Molecules (Basel, Switzerland) · 2021Review
- Exploring naltrexamine derivatives featuring azaindole moiety via nitrogen-walk approach to investigate their in vitro pharmacological profiles at the mu opioid receptor.Bioorganic & medicinal chemistry letters · 2021Article
- Assessment of select synthetic cannabinoid receptor agonist bias and selectivity between the type 1 and type 2 cannabinoid receptor.Scientific reports · 2021Article
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Authors and funding
22 authors at 7 institutions in 3 countries.
Sumanta GaraiDepartment of Pharmaceutical Sciences, School of Pharmacy, Bouvé College of Health Sciences , Northeastern University , Boston , Massachusetts 02115 , United States.
Pushkar M KulkarniDepartment of Pharmaceutical Sciences, School of Pharmacy, Bouvé College of Health Sciences , Northeastern University , Boston , Massachusetts 02115 , United States.
Peter C SchafferDepartment of Pharmaceutical Sciences, School of Pharmacy, Bouvé College of Health Sciences , Northeastern University , Boston , Massachusetts 02115 , United States.
Luciana M LeoCenter for Substance Abuse Research, Lewis Katz School of Medicine , Temple University , Philadelphia , Pennsylvania 19140 , United States.
Asher L BrandtCollege of Pharmacy and Nutrition , University of Saskatchewan , 104 Clinic Pl , Saskatoon , SK S7N2Z4 , Canada.
Ayat ZagzoogCollege of Pharmacy and Nutrition , University of Saskatchewan , 104 Clinic Pl , Saskatoon , SK S7N2Z4 , Canada.
Tallan BlackCollege of Pharmacy and Nutrition , University of Saskatchewan , 104 Clinic Pl , Saskatoon , SK S7N2Z4 , Canada.
Xiaoyan LinProgram in Neuroscience, Psychological and Brain Sciences, and Gill Center for Biomolecular Science , Indiana University , Bloomington , Indiana 47405 , United States.
Dow P HurstCenter for Drug Discovery , University of North Carolina Greensboro , Greensboro , North Carolina 27402 , United States.
David R JaneroDepartment of Pharmaceutical Sciences, Bouvé College of Health Sciences, Department of Chemistry and Chemical Biology, College of Science, and Health Sciences Entrepreneurs , Northeastern University , Boston , Massachusetts 02115 , United States.
Mary E AboodCenter for Substance Abuse Research, Lewis Katz School of Medicine , Temple University , Philadelphia , Pennsylvania 19140 , United States.ORCID 0000-0002-1744-2820
Anaelle ZimmowitchProgram in Neuroscience, Psychological and Brain Sciences, and Gill Center for Biomolecular Science , Indiana University , Bloomington , Indiana 47405 , United States.
Alex StraikerProgram in Neuroscience, Psychological and Brain Sciences, and Gill Center for Biomolecular Science , Indiana University , Bloomington , Indiana 47405 , United States.
Roger G PertweeSchool of Medicine, Medical Sciences and Nutrition, Institute of Medical Sciences , University of Aberdeen , Aberdeen AB25 2ZD , Scotland, U.K.
Melanie KellyDepartment of Pharmacology, Faculty of Medicine , Dalhousie University , 5850 College St , Halifax , NS , B3H4R2 , Canada.
Anna-Maria SzczesniakDepartment of Pharmacology, Faculty of Medicine , Dalhousie University , 5850 College St , Halifax , NS , B3H4R2 , Canada.
Eileen M Denovan-WrightDepartment of Pharmacology, Faculty of Medicine , Dalhousie University , 5850 College St , Halifax , NS , B3H4R2 , Canada.
Ken MackieProgram in Neuroscience, Psychological and Brain Sciences, and Gill Center for Biomolecular Science , Indiana University , Bloomington , Indiana 47405 , United States.
Andrea G HohmannProgram in Neuroscience, Psychological and Brain Sciences, and Gill Center for Biomolecular Science , Indiana University , Bloomington , Indiana 47405 , United States.
Patricia H ReggioCenter for Drug Discovery , University of North Carolina Greensboro , Greensboro , North Carolina 27402 , United States.
Robert B LaprairieCollege of Pharmacy and Nutrition , University of Saskatchewan , 104 Clinic Pl , Saskatoon , SK S7N2Z4 , Canada.
Ganesh A ThakurDepartment of Pharmaceutical Sciences, School of Pharmacy, Bouvé College of Health Sciences , Northeastern University , Boston , Massachusetts 02115 , United States.ORCID 0000-0002-7468-8819
Indiana University Bloomington · USNortheastern University · USDalhousie University · CAUniversity of Saskatchewan · CATemple University · USUniversity of North Carolina at Greensboro · USUniversity of Aberdeen · GB
Funding
Pilot Projects Core (PPC)P30DA013429 · NIDA · TEMPLE UNIV OF THE COMMONWEALTH · PI SCOTT M. RAWLS · 2000 to 2026
$34.6MProject 3 - In vivo pharmacology of cannabinoid receptor probesP01DA009158 · NIDA · UNIVERSITY OF CONNECTICUT STORRS · PI Alexandros Makriyannis · 1994 to 2026
$26.0MMolecular Determinants of Cannabinoid ActivityR01DA003934 · NIDA · UNIVERSITY OF NORTH CAROLINA GREENSBORO · PI REGGIO, PATRICIA HODAPP · 1985 to 2019
$5.6MCB2 Cannabinoid Mechanisms for Suppressing Opioid Tolerance and DependenceR01DA047858 · NIDA · TRUSTEES OF INDIANA UNIVERSITY · PI HOHMANN, ANDREA GRACE, MACKIE, KENNETH · 2019 to 2023
$2.6MRole of CB2 in Analgesic MechanismsR01DA041229 · NIDA · TRUSTEES OF INDIANA UNIVERSITY · PI HOHMANN, ANDREA GRACE, MACKIE, KENNETH · 2016 to 2020
$1.8MMolecular Determinants of GPR55 ActivityR01DA045698 · NIDA · UNIVERSITY OF NORTH CAROLINA GREENSBORO · PI CROATT, MITCHELL PETER · 2018 to 2022
$1.7MNIDA NIH HHS P01 DA009158NIDA NIH HHS P30 DA013429NIDA NIH HHS R01 DA003934NIDA NIH HHS R01 DA041229NIDA NIH HHS R01 DA045698NIDA NIH HHS R01 DA047858
Abstract
Cannabinoid 1 receptor (CB1R) allosteric ligands hold a far-reaching therapeutic promise. We report the application of fluoro- and nitrogen-walk approaches to enhance the drug-like properties of GAT211, a prototype CB1R allosteric agonist-positive allosteric modulator (ago-PAM). Several analogs exhibited improved functional potency (cAMP, β-arrestin 2), metabolic stability, and aqueous solubility. Two key analogs, GAT591 (
Indexed as
Allosteric RegulationAnimalsAnti-Inflammatory Agents, Non-SteroidalBiotransformationFluorineFreund's AdjuvantHEK293 CellsHumansIndolesInflammationMaleMiceMice, Inbred C57BLNeuronsNitrogenReceptor, Cannabinoid, CB13-(2-nitro-1-phenylethyl)-2-phenyl-1H-indoleAnti-Inflammatory Agents, Non-SteroidalFluorineFreund's AdjuvantIndolesNitrogenReceptor, Cannabinoid, CB1
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the Socratic graph.