Advanced search
Publication Cover
Current Eye Research Volume 30, 2005 - Issue 9
Submit an article Journal homepage
147
Views
57
CrossRef citations to date
0
Altmetric
Research Article

The Cross-Species A3 Adenosine-Receptor Antagonist MRS 1292 Inhibits Adenosine-Triggered Human Nonpigmented Ciliary Epithelial Cell Fluid Release and Reduces Mouse Intraocular Pressure

Hui Yang Department of Physiology, University of Pennsylvania, Philadelphia, Pennsylvania, USA
,
Marcel Y. Avila Department of Physiology, University of Pennsylvania, Philadelphia, Pennsylvania, USA
,
Kim Peterson-Yantorno Department of Physiology, University of Pennsylvania, Philadelphia, Pennsylvania, USA
,
Miguel Coca-Prados Department of Ophthalmology and Visual Science, Yale University, New Haven, Connecticut, USA
,
Richard A. Stone Department of Ophthalmology, University of Pennsylvania, Philadelphia, Pennsylvania, USA
,
Kenneth A. Jacobson Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland, USA
&
Mortimer M. Civan Department of Physiology and Department of Medicine, University of Pennsylvania, Philadelphia, Pennsylvania, USA
 show all
Pages 747-754 | Received 29 Jul 2004, Accepted 18 Jan 2005, Published online: 02 Jul 2009

Citations (57)

Keep up to date with the latest research on this topic with citation updates for this article.

Subscribe to citation updates

Read on this site (3)

Stefania Gessi, Stefania Merighi, Debora Fazzi, Angela Stefanelli, Katia Varani & Pier Andrea Borea. (2011) Adenosine receptor targeting in health and disease. Expert Opinion on Investigational Drugs 20:12, pages 1591-1609.
Read now
Neil J Press, Stefania Gessi, Pier A Borea & Riccardo Polosa. (2007) Therapeutic potential of adenosine receptor antagonists and agonists. Expert Opinion on Therapeutic Patents 17:8, pages 979-991.
Read now
KennethA. Jacobson, Stefano Costanzi, Soo-Kyung Kim, Eunjoo Roh, BhalchandraV. Joshi, Susanna Tchilibon, HengT. Duong & Zhan-Guo Gao. (2006) Action of Nucleosides and Nucleotides at 7 Transmembrane-Spanning Receptors. Nucleosides, Nucleotides & Nucleic Acids 25:12, pages 1425-1436.
Read now

Articles from other publishers (54)

Filippo Prencipe, Tatiana Da Ros, Eleonora Cescon, Ilenia Grieco, Margherita Persico, Giampiero Spalluto & Stephanie Federico. 2023.
Zhan-Guo Gao, John A. Auchampach & Kenneth A. Jacobson. (2022) Species dependence of A3 adenosine receptor pharmacology and function. Purinergic Signalling.
Crossref
Yunhee Kim, Jaewook Yang, Jee Young Kim, Jang Mi Lee, Woo Chan Son & Byoung-Gon Moon. (2022) HL3501, a Novel Selective A3 Adenosine Receptor Antagonist, Lowers Intraocular Pressure (IOP) in Animal Glaucoma Models. Translational Vision Science & Technology 11:2, pages 30.
Crossref
Eleonora Spinozzi, Cecilia Baldassarri, Laura Acquaticci, Fabio Del Bello, Mario Grifantini, Loredana Cappellacci & Petrelli Riccardo. (2021) Adenosine receptors as promising targets for the management of ocular diseases. Medicinal Chemistry Research 30:2, pages 353-370.
Crossref
Dilip K. Tosh, Veronica Salmaso, Harsha Rao, Amelia Bitant, Courtney L. Fisher, David I. Lieberman, Helmut Vorbrüggen, Marc L. Reitman, Oksana Gavrilova, Zhan-Guo Gao, John A. Auchampach & Kenneth A. Jacobson. (2020) Truncated (N)-Methanocarba Nucleosides as Partial Agonists at Mouse and Human A 3 Adenosine Receptors: Affinity Enhancement by N 6 -(2-Phenylethyl) Substitution . Journal of Medicinal Chemistry 63:8, pages 4334-4348.
Crossref
Wiwin Is Effendi, Tatsuya Nagano, Kazuyuki Kobayashi & Yoshihiro Nishimura. (2020) Focusing on Adenosine Receptors as a Potential Targeted Therapy in Human Diseases. Cells 9:3, pages 785.
Crossref
Xue Yang, Jacobus P. D. van Veldhoven, Jelle Offringa, Boaz J. Kuiper, Eelke B. Lenselink, Laura H. Heitman, Daan van der Es & Adriaan P. IJzerman. (2019) Development of Covalent Ligands for G Protein-Coupled Receptors: A Case for the Human Adenosine A 3 Receptor . Journal of Medicinal Chemistry 62:7, pages 3539-3552.
Crossref
Jae-Young Lee, Ju-Hwan Park, Ki-Taek Kim, Jinha Yu, Pramod K. Sahu, Naewon Kang, Hyeon-Jong Shin, Min-Hwan Kim, Ji-Su Kim, In-Soo Yoon, Lak Shin Jeong & Dae-Duk Kim. (2017) Determination and validation of LJ-2698, a potent human A3 adenosine receptor antagonist, in rat plasma by liquid chromatography-tandem mass spectrometry and its application in pharmacokinetic study. Archives of Pharmacal Research 40:8, pages 952-961.
Crossref
Antonella Ciancetta & Kenneth Jacobson. (2017) Structural Probing and Molecular Modeling of the A3 Adenosine Receptor: A Focus on Agonist Binding. Molecules 22:3, pages 449.
Crossref
Soo-Kyung Kim & William A. Goddard III. 2017. Pharmaceutical Sciences. Pharmaceutical Sciences 656 682 .
Kenneth A. JacobsonMortimer M. Civan. (2016) Ocular Purine Receptors as Drug Targets in the Eye. Journal of Ocular Pharmacology and Therapeutics 32:8, pages 534-547.
Crossref
Rebecca K. Donegan & Raquel L. Lieberman. (2015) Discovery of Molecular Therapeutics for Glaucoma: Challenges, Successes, and Promising Directions. Journal of Medicinal Chemistry 59:3, pages 788-809.
Crossref
Soo-Kyung Kim & William A. Goddard III. 2016. Applied Case Studies and Solutions in Molecular Docking-Based Drug Design. Applied Case Studies and Solutions in Molecular Docking-Based Drug Design 158 185 .
Amarendra Panda, Suresh Satpati, Anshuman Dixit & Shantanu Pal. (2016) Novel homologated-apio adenosine derivatives as A 3 adenosine receptor agonists: design, synthesis and molecular docking studies . RSC Advances 6:14, pages 11233-11239.
Crossref
Joana Galvao, Filipe Elvas, Tiago Martins, M. Francesca Cordeiro, António Francisco Ambrósio & Ana Raquel Santiago. (2015) Adenosine A 3 receptor activation is neuroprotective against retinal neurodegeneration. Experimental Eye Research 140, pages 65-74.
Crossref
Pier Andrea Borea, Katia Varani, Fabrizio Vincenzi, Pier Giovanni Baraldi, Mojgan Aghazadeh Tabrizi, Stefania Merighi & Stefania Gessi. (2015) The A 3 Adenosine Receptor: History and Perspectives . Pharmacological Reviews 67:1, pages 74-102.
Crossref
Kenneth A. Jacobson, Zhan-Guo Gao, Silvia Paoletta, Evgeny Kiselev, Saibal Chakraborty, P. Suresh Jayasekara, Ramachandran Balasubramanian & Dilip K. Tosh. (2015) John Daly Lecture: Structure-guided Drug Design for Adenosine and P2Y Receptors. Computational and Structural Biotechnology Journal 13, pages 286-298.
Crossref
Kenneth A. Jacobson. (2013) Structure-Based Approaches to Ligands for G-Protein-Coupled Adenosine and P2Y Receptors, from Small Molecules to Nanoconjugates. Journal of Medicinal Chemistry 56:10, pages 3749-3767.
Crossref
Siew Lee Cheong, Stephanie Federico, Gopalakrishnan Venkatesan, Alexander Laurence Mandel, Yi‐Ming Shao, Stefano Moro, Giampiero Spalluto & Giorgia Pastorin. (2011) The A 3 adenosine receptor as multifaceted therapeutic target: pharmacology, medicinal chemistry, and in silico approaches . Medicinal Research Reviews 33:2, pages 235-335.
Crossref
Pier Giovanni Baraldi, Delia Preti, Pier Andrea Borea & Katia Varani. (2012) Medicinal Chemistry of A 3 Adenosine Receptor Modulators: Pharmacological Activities and Therapeutic Implications . Journal of Medicinal Chemistry 55:12, pages 5676-5703.
Crossref
Pier Giovanni Baraldi, Giulia Saponaro, Romeo Romagnoli, Mojgan Aghazadeh Tabrizi, Stefania Baraldi, Allan R. Moorman, Sandro Cosconati, Salvatore Di Maro, Luciana Marinelli, Stefania Gessi, Stefania Merighi, Katia Varani, Pier Andrea Borea & Delia Preti. (2012) Water-Soluble Pyrazolo[4,3- e ][1,2,4]triazolo[1,5- c ]pyrimidines as Human A 3 Adenosine Receptor Antagonists . Journal of Medicinal Chemistry 55:11, pages 5380-5390.
Crossref
Dilip K. Tosh, Francesca Deflorian, Khai Phan, Zhan-Guo Gao, Tina C. Wan, Elizabeth Gizewski, John A. Auchampach & Kenneth A. Jacobson. (2012) Structure-Guided Design of A 3 Adenosine Receptor-Selective Nucleosides: Combination of 2-Arylethynyl and Bicyclo[3.1.0]hexane Substitutions . Journal of Medicinal Chemistry 55:10, pages 4847-4860.
Crossref
Feng Luan, André Melo, Fernanda Borges & M. Natália D.S. Cordeiro. (2011) Affinity prediction on A3 adenosine receptor antagonists: The chemometric approach. Bioorganic & Medicinal Chemistry 19:22, pages 6853-6859.
Crossref
Soo-Kyung Kim, Lindsay Riley, Ravinder Abrol, Kenneth A. Jacobson & William A. GoddardIIIIII. (2011) Predicted structures of agonist and antagonist bound complexes of adenosine A 3 receptor . Proteins: Structure, Function, and Bioinformatics 79:6, pages 1878-1897.
Crossref
Christa E. Müller & Kenneth A. Jacobson. (2011) Recent developments in adenosine receptor ligands and their potential as novel drugs. Biochimica et Biophysica Acta (BBA) - Biomembranes 1808:5, pages 1290-1308.
Crossref
Daniela Poli, Daniela Catarzi, Vittoria Colotta, Flavia Varano, Guido Filacchioni, Simona Daniele, Letizia Trincavelli, Claudia Martini, Silvia Paoletta & Stefano Moro. (2011) The Identification of the 2-Phenylphthalazin-1(2 H )-one Scaffold as a New Decorable Core Skeleton for the Design of Potent and Selective Human A 3 Adenosine Receptor Antagonists . Journal of Medicinal Chemistry 54:7, pages 2102-2113.
Crossref
Stefania Gessi, Stefania Merighi, Katia Varani & Pier Andrea Borea. 2011. Pharmacology of Purine and Pyrimidine Receptors. Pharmacology of Purine and Pyrimidine Receptors 41 75 .
Isaac Avni, Hanna J. Garzozi, Irina S. Barequet, Fanni Segev, David Varssano, Gil Sartani, Noa Chetrit, Erez Bakshi, David Zadok, Oren Tomkins, Gilad Litvin, Kenneth A. Jacobson, Sari Fishman, Zivit Harpaz, Motti Farbstein, Sara Bar Yehuda, Michael H. Silverman, William D. Kerns, David R. Bristol, Ilan Cohn & Pnina Fishman. (2010) Treatment of Dry Eye Syndrome with Orally Administered CF101. Ophthalmology 117:7, pages 1287-1293.
Crossref
John A. Auchampach, Elizabeth T. Gizewski, Tina C. Wan, Sonia de Castro, Garth G. BrownJr.Jr. & Kenneth A. Jacobson. (2010) Synthesis and pharmacological characterization of [125I]MRS5127, a high affinity, selective agonist radioligand for the A3 adenosine receptor. Biochemical Pharmacology 79:7, pages 967-973.
Crossref
Dilip K. Tosh, Lena S. Yoo, Moshe Chinn, Kunlun Hong, S. Michael KilbeyIIII, Matthew O. Barrett, Ingrid P. Fricks, T. Kendall Harden, Zhan-Guo Gao & Kenneth A. Jacobson. (2010) Polyamidoamine (PAMAM) Dendrimer Conjugates of “Clickable” Agonists of the A 3 Adenosine Receptor and Coactivation of the P2Y 14 Receptor by a Tethered Nucleotide . Bioconjugate Chemistry 21:2, pages 372-384.
Crossref
Zhao Wang, Chi Wai Do, Marcel Y. Avila, Kim Peterson-Yantorno, Richard A. Stone, Zhan-Guo Gao, Bhalchandra Joshi, Pedro Besada, Lak Shin Jeong, Kenneth A. Jacobson & Mortimer M. Civan. (2010) Nucleoside-derived antagonists to A3 adenosine receptors lower mouse intraocular pressure and act across species. Experimental Eye Research 90:1, pages 146-154.
Crossref
Dilip K. Tosh, Moshe Chinn, Lena S. Yoo, Dong Wook Kang, Hans Luecke, Zhan-Guo Gao & Kenneth A. Jacobson. (2010) 2-Dialkynyl derivatives of (N)-methanocarba nucleosides: ‘Clickable’ A3 adenosine receptor-selective agonists. Bioorganic & Medicinal Chemistry 18:2, pages 508-517.
Crossref
Pier Giovanni Baraldi, Romeo Romagnoli, Giulia Saponaro, Stefania Baraldi, Mojgan Aghazadeh Tabrizi & Delia Preti. 2010. A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics. A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics 121 147 .
Kenneth A. Jacobson, Zhan-Guo Gao, Dilip K. Tosh, Gangadhar J. Sanjayan & Sonia de Castro. 2010. A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics. A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics 93 120 .
Dilip K. Tosh, Moshe Chinn, Andrei A. Ivanov, Athena M. Klutz, Zhan-Guo Gao & Kenneth A. Jacobson. (2009) Functionalized Congeners of A 3 Adenosine Receptor-Selective Nucleosides Containing a Bicyclo[3.1.0]hexane Ring System . Journal of Medicinal Chemistry 52:23, pages 7580-7592.
Crossref
Shantanu Pal, Won Jun Choi, Seung Ah Choe, Cara L. Heller, Zhan-Guo Gao, Moshe Chinn, Kenneth A. Jacobson, Xiyan Hou, Sang Kook Lee, Hea Ok Kim & Lak Shin Jeong. (2009) Structure–activity relationships of truncated adenosine derivatives as highly potent and selective human A3 adenosine receptor antagonists. Bioorganic & Medicinal Chemistry 17:10, pages 3733-3738.
Crossref
Vittoria ColottaOmbretta LenziDaniela CatarziFlavia VaranoGuido FilacchioniClaudia MartiniLetizia TrincavelliOsele CiampiAnna Maria PuglieseChiara TrainiFelicita PedataErika MorizzoStefano Moro. (2009) Pyrido[2,3- e ]-1,2,4-triazolo[4,3- a ]pyrazin-1-one as a New Scaffold To Develop Potent and Selective Human A 3 Adenosine Receptor Antagonists. Synthesis, Pharmacological Evaluation, and Ligand−Receptor Modeling Studies . Journal of Medicinal Chemistry 52:8, pages 2407-2419.
Crossref
Ramiro G. Dip. (2009) Adenosine receptor modulation: Potential implications in veterinary medicine. The Veterinary Journal 179:1, pages 38-49.
Crossref
Vittoria Colotta, Francesca Capelli, Ombretta Lenzi, Daniela Catarzi, Flavia Varano, Daniela Poli, Fabrizio Vincenzi, Katia Varani, Pier Andrea Borea, Diego Dal Ben, Rosaria Volpini, Gloria Cristalli & Guido Filacchioni. (2009) Novel potent and highly selective human A3 adenosine receptor antagonists belonging to the 4-amido-2-arylpyrazolo[3,4-c]quinoline series: Molecular docking analysis and pharmacological studies. Bioorganic & Medicinal Chemistry 17:1, pages 401-410.
Crossref
Kenneth A. Jacobson, Athena M. Klutz, Dilip K. Tosh, Andrei A. Ivanov, Delia Preti & Pier Giovanni Baraldi. 2009. Adenosine Receptors in Health and Disease. Adenosine Receptors in Health and Disease 123 159 .
P.A. Borea, S. Gessi, S. Bar-Yehuda & P. Fishman. 2009. Adenosine Receptors in Health and Disease. Adenosine Receptors in Health and Disease 297 327 .
Kenneth A. Jacobson. 2009. Adenosine Receptors in Health and Disease. Adenosine Receptors in Health and Disease 1 24 .
Artem Melman, Ben Wang, Bhalchandra V. Joshi, Zhan-Guo Gao, Sonia de Castro, Cara L. Heller, Soo-Kyung Kim, Lak Shin Jeong & Kenneth A. Jacobson. (2008) Selective A3 adenosine receptor antagonists derived from nucleosides containing a bicyclo[3.1.0]hexane ring system. Bioorganic & Medicinal Chemistry 16:18, pages 8546-8556.
Crossref
Kenneth A. Jacobson, Bhalchandra V. Joshi, Ben Wang, Athena Klutz, Yoonkyung Kim, Andrei A. Ivanov, Artem Melman & Zhan‐Guo Gao. 2008. Modified Nucleosides. Modified Nucleosides 433 449 .
Lak Shin Jeong, Hyuk Woo Lee, Hea Ok Kim, Dilip K. Tosh, Shantanu Pal, Won Jun Choi, Zhan-Guo Gao, Amit R. Patel, Wanda Williams, Kenneth A. Jacobson & Hee-Doo Kim. (2008) Structure–activity relationships of 2-chloro-N6-substituted-4′-thioadenosine-5′-N,N-dialkyluronamides as human A3 adenosine receptor antagonists. Bioorganic & Medicinal Chemistry Letters 18:5, pages 1612-1616.
Crossref
Pier Giovanni Baraldi, Mojgan Aghazadeh Tabrizi, Stefania Gessi & Pier Andrea Borea. (2008) Adenosine Receptor Antagonists:  Translating Medicinal Chemistry and Pharmacology into Clinical Utility. Chemical Reviews 108:1, pages 238-263.
Crossref
Iok‐Hou Pang & Abbot F. Clark. 2008. The Eye's Aqueous Humor. The Eye's Aqueous Humor 427 469 .
Mortimer M. Civan. 2008. The Eye's Aqueous Humor. The Eye's Aqueous Humor 1 45 .
Chi-wai Do, Chi-wing Kong, Chu-yan Chan, Mortimer M. Civan & Chi-ho To. 2008. Ocular Transporters In Ophthalmic Diseases And Drug Delivery. Ocular Transporters In Ophthalmic Diseases And Drug Delivery 61 86 .
C. W. Do & M. M. Civan. (2006) Swelling‐activated chloride channels in aqueous humour formation: on the one side and the other. Acta Physiologica 187:1-2, pages 345-352.
Crossref
. (2006) Invited Lectures. Purinergic Signalling 2:1, pages 1-324.
Crossref
Kenneth A. Jacobson & Zhan-Guo Gao. (2006) Adenosine receptors as therapeutic targets. Nature Reviews Drug Discovery 5:3, pages 247-264.
Crossref
Zhan-Guo Gao, Bhalchandra V. Joshi, Athena M. Klutz, Soo-Kyung Kim, Hyuk Woo Lee, Hea Ok Kim, Lak Shin Jeong & Kenneth A. Jacobson. (2006) Conversion of A3 adenosine receptor agonists into selective antagonists by modification of the 5′-ribofuran-uronamide moiety. Bioorganic & Medicinal Chemistry Letters 16:3, pages 596-601.
Crossref
Pedro Besada, Liaman K. Mamedova, Krishnan K. Palaniappan, Zhan-Guo Gao, Bhalchandra V. Joshi, Lak Shin Jeong, Mortimer M. Civan & Kenneth A. Jacobson. (2006) Nucleoside Prodrugs of A3 Adenosine Receptor Agonists and Antagonists. Collection of Czechoslovak Chemical Communications 71:6, pages 912-928.
Crossref

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Order Reprints Request Corporate Permissions

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

Request Academic Permissions

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.

Related research

People also read lists articles that other readers of this article have read.

Recommended articles lists articles that we recommend and is powered by our AI driven recommendation engine.

Cited by lists all citing articles based on Crossref citations.
Articles with the Crossref icon will open in a new tab.