• 800.644.5687  
• Request a Quote  |
• Ordering  |
• Explore our Panels

• Document Resource Library
• Publication List

Publications & References List

DiscoveRx has been been featured in many publications

References below are grouped by technology platform and signaling pathway.

PathHunter

Zhao, X et al. (Sept 2008). A homogeneous enzyme fragment complementation-based {beta}-Arrestin translocation assay for high-throughput screening of G-Protein-Coupled receptors. J Biomol Screen. 13(8):737-747. (SSTR2)

Oka, S et al. (May 2010). Lysophosphatidylinositol induces rapid phosphorylation of p38 mitogen-activated protein kinase and activating transcription factor 2 in HEK293 cells expressing GPR55 and IM-9 lymphoblastoid cells. J Biochem. 147: 671-678. (GPR55)

Tan ES, Naylor JC, Groban ES, Bunzow JR, Jacobson MP, Grandy DK, Scanlan TS (2009).The Molecular Basis of Species-Specific Ligand Activation of Trace Amine-Associated Receptor 1 (TAAR1). ACS Chemical Biology, 4(3): 209-220.

PathHunter B-Arrestin

Lambertus, HC et al. C5a-Stimulated Recruitment of b-Arrestin2 to the non-signaling 7-transmembrane decoy receptor C5L2. J Biomol Screen. 14, 1067-1075 (2009)

Rosethorne, EM, et al. Agonist-Biased Signaling at the Histamine H4 Receptor: JN7777120 Recruits b-Arrestin Without Activating G-Proteins. Mol Pharmacol. 79, 749-757 (2011)

Van der Lee, MMC et al. (Aug 2009). Pharmacological Characterization of Receptor Redistribution and β-Arrestin Recruitment Assays for the Cannabinoid Receptor 1. J Biomol Screen. 14: 811-823. (CNR1)

Yin, H, et al. (May 2009). Lipid G protein-coupled receptor ligand identification using β-Arrestin PathHunter™ Assay. J Biol Chem. 284(18):12328-12338. (ProLink Cloning Vector and HEK 293 EA-Arrestin Parental Cell Line)

McGuinness, D, et al. (Jan 2009). Characterizing Cannabinoid CB2 Receptor Ligands using DiscoveRx PathHunter™ β-Arrestin Assay. J. Biomol Screen. 14(1):49-58. (CNR2)

Van der Lee, MMC et al. (Dec 2008). β-Arrestin recruitment assay for the identification of agonists of the sphingosine 1-phosphate receptor EDG1. J Biomol Screen. 13(10): 986-998. (EDG1)

Gao, Z-G and Jacobson, KA (April 2008). Translocation of arrestin induced by human A3 adenosine receptor ligands in an engineered cell line: comparison with G proteindependent pathways. Pharma Res. 57:303-311. (ADORA3)

Ma, L et al. (Sept. 2009). Selective activation of the M1 muscarinic acetylcholine receptor achieved by allosteric potentiation. PNAS. 106(37): 15950-15955. (CHRM1)

de Kruijf, P et al. (May 2009). Nonpeptidergic Allosteric Antagonists Differentially Bind to the CXCR2 chemokine Receptor. JPET 329(2):783-790. (CXCR2)

Fredman, G et al. (Oct 2010) Resolvin E1 regulates Adenosine Diphosphate activation of human platelets. Arterioscler Thromb Vasc Biol. 30: 2005-2013. (P2Y12)

Poulin, B et al. (May 2010). The M3-muscarinic receptor regulates learning and memory in a receptor phosphorylation/arrestin-dependent manner. PNAS 107: 9440-9445. (CHRM3)

Chu, A et al. (Jan 2010) Identification and characterization of a small molecule antagonist of human VPAC2 Receptor. Mol Pharmacol. 77: 95-101. (VPAC2)

Krishnamoorthy, S et al. (Dec 2009) Resolvin D1 binds human phagocytes with evidence for proresolving receptors. PNAS 107: 1660-1665. (GPR32)

Barbara, G et al. (Oct 2009) T-Type calcium channel inhibition underlies the analgesic effects of the endogenous lipoamino acids. J Neurosci 29: 13106-13114.

Cinar, R and Szűcs (Oct 2009) CB1 receptor-independent actions of SR141716 on G-protein signaling: Coapplication with the μ-Opioid agonist Tyr-D-Ala-Gly-(NMe)Phe-Glyol unmasks novel, pertussis toxin insensitive Opioid signaling in μ-Opioid receptor-chinese hamster ovary cells. J Pharmacol Exp Ther 330: 567-574. (CNR1/CB1)

Zabel, BA et al. (Sept 2009) Elucidation of CXCR7-mediated signaling events and inhibition of CXCR4-mediated tumor cell transendothelial migration by CXCR7 ligands. J Immunol 183: 3204-3211. (CXCR7)

Wisler, JM et al. (Oct 2007). A unique mechanism of β-blocker action: Carvedilol stimulates β-Arrestin signaling. PNAS 104(42):16657-16662

Rajagopal, S et al. (May 2010). Teaching old receptors new tricks: biasing seventransmembrane receptors. Nat Rev Drug Discovery 9: 373-386.

Drake, MT et al. (Feb 2008). β-Arrestin-biased agonism at the β2-adrenergic receptor. J Biol Chem. 283(9):5669-5676. (ADRB2)

Violin, JD and Leftowitz, RJ (Aug 2007). β-Arrestin-biased ligands at seventransmembrane receptors. Trends in Pharmacol Sci 28(8):416-422.

DeWire, SM et al. (Jan 2007). β-Arrestins and cell signaling. Annu. Rev. Physiol. 69:483–510.

Casarosa, P and Kollak, I. (May 2010). Molecular interactions between the human muscarinic M3 and b2 receptors: Evidence for heterodimerization. Am J Respir Crit Care Med 181: A6368.

HitHunter cAMP

East SP, et al. An orally bioavailable positive allosteric modulator of the mGlu4 receptor with efficacy in an animal model of motor dysfunction. Bioorg. Med. Chem. Lett. 15;20(16):4901-5 (2010)

Zhang J-H (1999). A Simple Statistical Parameter for Use in Evaluation and Validation of High Throughput Screening Assays. Journal of Biomolecular Screening, 4 (2): 67-73.

Golla R & Seethala R (2002). A Homogeneous Enzyme Fragment Complementation Cyclic AMP Screen for GPCR Agonists. Journal of Biomolecular Screening, 7 (6): 515-525.

Daniela G, Vernier M, Pfeifer MJ, Dasen B, Tenaillon L, and Bouhelal R (2003). High Throughput Screening Technologies for Direct Cyclic AMP Measurement. ASSAY and Drug Development Technologies, 1(2): 291-303.

Williams C (2004). CAMP Detection Methods in HTS: Selecting the Best from the Rest. Nature Reviews Drug Discovery, 3 (2): 125-135.

Dunlop J and Eglen R (2004). Identifying Orphan G Protein Coupled Receptors in Drug Discovery. Drug Discovery Today: Technologies, 1(1): 61-68.

Weber M, Ferrer M, Zheng W, Inglese J, Strulovici B and Kunapuli P (2004). A 1,536-Well cAMP Assay for Gs- and Gi-Coupled Receptors Using Enzyme Fragmentation Complementation. ASSAY and Drug Development Technologies, 2(1): 39-49.

Deo SK (2004). Exploring bioanalytical applications of assisted protein reassembly. Anal Bioanal Chem. 379:383–390.

Carter AA and Hill SJ (2005). Characterization of Isoprenaline- and Salmeterol-Stimulated Interactions between 2-Adrenoceptors and -Arrestin 2 Using Galactosidase Complementation in C2C12 Cells. Journal of Pharmacology and Experimental Therapeutics, 315 (2): 839-848.

Eglen RM (2005). Functional G Protein-Coupled Receptor Assays for Primary and Secondary Screening. Combinatorial Chemistry & High Throughput Screening 8 (4): 311-318.

Eglen RM (2005). An Overview of High Throughput Screening at G Protein Coupled Receptors. Frontiers in Drug Design & Discovery, 1(1): 97-111.

Xue, L, Gyles SL, Wettey FR, Gazi L, Townsend E, Hunter MG, and Pettipher R (2005). Prostaglandin D2 Causes Preferential Induction of Proinflammatory Th2 Cytokine Production through an Action on Chemoattractant Receptor-Like Molecule Expressed on Th2 Cells. The Journal of Immunology, 175: 6531-536.

Wilson S, Wilkinson G, and Milligan G (2005). The CXCR1 and CXCR2 Receptors Form Constitutive Homo- and Heterodimers Selectively and with Equal Apparent Affinities. Journal of Biological Chemistry, 280(31) 28663-8674.

Thomsen W, Frazer J, and Unett D (2005). Functional Assays for Screening GPCR Targets. Current Opinion in Biotechnology 16(6): 655-65.

Wettey FR, Xue L, Pettipher R (2006). Salbutamol Inhibits Trypsin-mediated Production of CXCL8 by Keratinocytes. Cytokine 36.1-2: 29-34.

Jassen AK, Yang H, Miller GM, Calder E, Madras BK (2006). Receptor Regulation of Gene Expression of Axon Guidance Molecules: Implications for Adaptation. Molecular Pharmacology, 70(1): 71-77.

Yao BB, MukherjeeS, FanY, Garrison TR, Daza AV, Grayson GK, Hooker BA, Dart MJ, Sullivan JP and Meyer MD (2006). In vitro pharmacological characterization of AM1241: a protean agonist at the cannabinoid CB2 receptor. British Journal of Pharmacology, 149: 145–154.

Wainscott DB, Little SP, Yin T, Tu Y, Rocco VP, He JX, Nelson DL (2007). Pharmacologic Characterization of the Cloned Human Trace Amine-Associated Receptor1 (TAAR1) and Evidence for Species Differences with the Rat TAAR1. Journal of Pharmacology and Experimental Therapeutics, 320 (1): 475-85.

Nawoschik SP, Olsen M, Smith DL, Khawaja X (2007). Stable Expression of Adenylyl Cyclase 2 Leads to the Functional Rescue of Human 5-HT6 Receptor in a CHODUKX Cell Line. Journal of Pharmacological and Toxicological Methods, 55 (3): 323-31.

Selkirk JV, Nottebaum LM, Lee J, Yang W, Foster AC, Lechner SM (2007). Identification of Differential Melanocortin 4 Receptor Agonist Profiles at Natively Expressed Receptors in Rat Cortical Astrocytes and Recombinantly Expressed Receptors in Human Embryonic Kidney Cells. Neuropharmacology 52 (2): 459-66.

Bingham B, Jones PG, Uveges AJ, Kotnis S, Lu P, Smith VA, Sun SC, Resnick L, Chlenov M, He Y, Strassle BW, Cummons TA, Piesla MJ, Harrison JE, Whiteside GT, Kennedy JD (2007). Species-specific pharmacological Effects of the Cannabinoid Receptor 2 (CB2) Selective Ligand AM1241 and Its Resolved Enantiomers. British Journal of Pharmacology, 151(7): 1061-1070.

Ajit SK, Ramineni S, Edris W, Hunt RA, Hum WT, Hepler JR, Young KH (2007) . RGSZ1 Interacts with Protein Kinase C Interacting Protein PKCI-1 and Modulates Mu Opioid Receptor Signaling. Cellular Signalling, 19(4): 723-730.

McLoughlin DJ, Bertelli F, and Williams C (2007). The A, B, Cs of G-protein-coupled Receptor Pharmacology in Assay Development for HTS. Expert Opinion on Drug Discovery 2(5): 603-19.

Weber M, Muthusubramaniam L, Murray J, Hudak E, Kornienko O, Johnson EN, Strulovici B, and Kunapuli P (2007). Ultra-High-Throughput Screening for Antagonists of A Gi-Coupled Receptor in A 2.2-uL 3,456-Well Plate Format CyclicAMP Assay. ASSAY and Drug Development Technologies, 5 (1): 117-26.

Mettler SE, Ghayouri S, Christensen GP, Forte JG (2007). Modulatory Role of Phosphoinositide 3-kinase in Gastric Acid Secretion. Am J Physiol Gastrointest Liver Physiol. 293(3):G532-43.

Bora RS, Malik R, Arya R, Gupta D, Singh V, Aggarwal N, Dastidar S, Ray A, Saini KS (2007). A Reporter Gene Assay for Screening of PDE4 Subtype Selective Inhibitors. Biochemical and Biophysical Research Communications 356 (1): 153-58.

Yang JJ, Yoon S, Myung G, Gwak W, Kim G, Chung S. Lee S. Lee C. Kim and. Lee H (2007). Bile Acid-induced TGR5-dependent C-Jun-N Terminal Kinase Activation Leads to Enhanced Caspase 8 Activation in Hepatocytes. Biochemical and Biophysical Research Communications, 361(1): 156-61.

Sullivan NR, Leventhal L, Harrison J, Smith VA, Cummons TA, Spangler TB, Sun S-C, Lu P, Uveges AJ, Strassle BW, Piesla MJ, Ramdass R, Barry A, Schantz J, Adams W, Whiteside GT, Adedoyin A, and Jones PG (2007). Pharmacological Characterization of the Muscarinic Agonist (3R,4R)-3-(3-Hexylsulfanyl -pyrazin-2-yloxy)-1-aza-bicyclo [2.2.1] heptane (WAY-132983) in in Vitro and in Vivo Models of Chronic Pain. Journal of Pharmacology and Experimental Therapeutics 322.3 (2007): 1294-304.

Summerhill S, Stroud T, Nagendra R, Perroshuguet C, and Trevethick M (2008). A Cell-based Assay to Assess the Persistence of Action of Agonists Acting at Recombinant Human β2 Adrenoceptors. Journal of Pharmacological and Toxicological Methods 58 (3):189-97.

Chin CL, Tovcimak AE, Hradil VP, Seifert TR, Hollingsworth PR, Chandran P, Zhu CZ, Gauvin D, Pai M, Wetter J, Hsieh GC, Honore P, Frost JM, Dart MJ, Meyer MD, Yao BB, Cox BF, Fox GB (2008). Differential Effects of Cannabinoid Receptor Agonists on Regional Brain Activity Using Pharmacological MRI. British Journal of Pharmacology 153 (2): 367-79.

Sandrock T, Terry A, Martin JC, Erdogan E, Meikle WA (2008) Detection of Thyroid-Stimulating Immunoglobulins by Use of Enzyme-Fragment Complementation.Clinical Chemistry, 54(8): 1401-402.

Arya R, Aslam S, Gupta S, Bora RS, Vijayakrishnan L, Gulati P, Naithani S, Mukherjee S, Dastidar S, Bhattacharya A, Saini KS (2008). Purification of Recombinant Human Phosphodiesterase 7A Expressed in Dictyostelium Discoideum. Protein Expression and Purification, 61(2): 149-54.

Snead AN, Miyakawa M, Tan ES, Scanlan TS (2008). Trace Amine-associated Receptor 1 (TAAR1) Is Activated by Amiodarone Metabolites. Bioorganic & Medicinal Chemistry Letters, 18 (22): 5920-922.

Lee T, Schwandner R, Swaminath G, Weiszmann J, Cardozo M, Greenberg J, Jaeckel P, Ge H, Wang Y, Jiao X, Liu J, Kayser F, Tian H, Li Y (2008). Identification and Functional Characterization of Allosteric Agonists for the G Protein-Coupled Receptor FFA2. Molecular Pharmacology, 74 (6): 1599-609.

Shemesh R, Toporik A, Levine Z, Hecht I, Rotman G, Wool A, Dahary D, Gofer E, Kliger Y, Soffer MA, Rosenberg A, Eshel D, Cohen Y (2008). Discovery and Validation of Novel Peptide Agonists for G-protein-coupled Receptors. Journal of Biological Chemistry, 283(50): 34643-4649.

Trani G, Baddeley SM, Briggs MA, Chuang TT, Deeks NJ, Johnson CN, Khazragi AA, Mead TL, Medhurst AD, Milner PH, Quinn LP, Ray AM, Rivers DA, Stean TO, Stemp G, Trail BK, Witty DR (2008). Tricyclic Azepine Derivatives as Selective Brain Penetrant 5-HT6 Receptor Antagonists. Bioorganic & Medicinal Chemistry Letters,18 (20): 5698-700.

Zeller J, Poulsen KT, Sutton JE, Abdiche YN, Collier S, Chopra R, Garcia CA, Pons J, Rosenthal A, Shelton DL (2008). CGRP Function blocking Antibodies Inhibit Neurogenic Vasodilatation without Affecting Heart Rate or Arterial Blood Pressure in the Rat. British Journal of Pharmacology, 155(7): 1093-103.

Monaghan TK, Mackenzie CJ, Plevin R, Lutz EM (2008). PACAP-38 induces neuronal differentiation of human SH-SY5Y neuroblastoma cells via cAMP-mediated activation of ERK and p38 MAP kinases. J Neurochem, 104(1):74-88.

Liu F, Grauer S, Kelley C, Navarra R, Graf R, Zhang G, Atkinson PJ, Popiolek M, Wantuch C, Khawaja X, Smith D, Olsen M, Kouranova E, Lai M, Pruthi F, Pulicicchio C, Day M, Gilbert A, Pausch MH, Brandon NJ, Beyer CE, Comery TA, Logue S, Rosenzweig-Lipson S, and K. L. Marquis KL (2008). ADX47273 [S-(4-Fluoro-phenyl)- -methanone]: A Novel Metabotropic Glutamate Receptor 5-Selective Positive Allosteric Modulator with Preclinical Antipsychotic-Like and Procognitive Activities. Journal of Pharmacology and Experimental Therapeutics, 327(3): 827-39.

Murray D L, Johnson EN, Wang P, Gauthier J, Bing N, Vanderwall D, Xu Z, Jensen, Cox RF, Kostura M and Sorensen SD (2009). Functional antagonism of IL-1α induced gene expression profiles define the cAMP/PKA pathway as a unique regulator of IL-1α signaling network. Journal of Receptors and Signal Transduction, 29 (5): 246-256

Bradley J and McLoughlin D (2009). Use of the DiscoveRx HitHunter cAMP II Assay for Direct Measurement of cAMP in Gs and Gi GPCRs. Methods in Molecular Biology, 552: 171- 179.

Abbas AI, Hedlund PB, Huang X-P, Tran TB, Meltzer HY and Roth BL (2009). Amisulpride is a potent 5-HT7 antagonist: relevance for antidepressant actions in vivo. Psychopharmacology, 205 (1): 119-128.

Fan P, Jiang Z, Diamond I and Yao L (2009). Up-Regulation of AGS3 during Morphine Withdrawal Promotes cAMP Superactivation via Adenylyl Cyclase 5 and 7 in Rat Nucleus Accumbens/Striatal Neurons. Molecular Pharmacology, 76 (3): 526-533

Zhu CZ, Mikusa JP, Fan Y, Hollingsworth PR, Pai M, Chandran P, Daza AV, Yao BB, Dart MJ, Meyer MD, Decker MW, Hsieh GC and Honore P (2009). Peripheral and central sites of action for the non-selective cannabinoid agonist WIN 55,212-2 in a rat model of post-operative pain. British Journal of Pharmacology, 157: 645–655

Shemesh, R., Hermesh, C., Toporik, A., Levine, Z., Novik, A., Wool, A., Kliger, Y., Rosenberg, A., Bathgate, R. A. D. and Cohen Y (2009), Activation of Relaxin-Related Receptors by Short, Linear Peptides Derived from a Collagen-Containing Precursor. Annals of the New York Academy of Sciences, 1160: 78–86.

Mancini I, Brusa R, Quadrato G, Foglia C, Scandroglio P, Silverman L, Tulshian D, Reggiani A and Beltramo M (2009). Constitutive activity of cannabinoid-2 (CB2) receptors plays an essential role in the protean agonism of (+) AM1241 and L768242. British Journal of Pharmacology, 158: 382–391.

Sieben A, Prenner L, Sorkalla T, Wolf A, Jakobs D, Runkel F, Haberlein H (2009). α-Hederin, but not hederacoside C and hederagenin from hedera helix, affects the binding behavior, dynamics, and regulation of β2-adrenergic receptors. Biochemistry 48 (15): 3477-3482.

Hu LA, Tang PM, Eslahi NK, Zhou T, Barbosa J, Liu Q (2009). Identification of surrogate agonists and antagonists for orphan G-protein-coupled receptor GPR139. J Biomol Screen. 14(7):789-97.

Roncarati R, Scali C, Comery TA, Grauer SM, Aschmi S, Bothmann H, Jow B, Kowal D, Gianfriddo M, Kelley C, Zanelli U, Ghiron C, Haydar S, Dunlop J, and Terstappen GC (2009). Procognitive and Neuroprotective Activity of a Novel α7 Nicotinic Acetylcholine Receptor Agonist for Treatment of Neurodegenerative and Cognitive Disorders . J Pharmacol. Exp. Ther. 329:459-468.

Prasannaa G, Fortnerf J, Xiangb C, Zhang E, Carreiroa S, Scott Anderson S, Sartnurakc S, Wuc G, Gukasyanc H, Niesmana M, Naird S, Ruid E, Lafontained J, Almadene CD, Wellse P and Kraussa A (2009). Ocular pharmacokinetics and hypotensive activity of PF-04475270, an EP4 prostaglandin agonist in preclinical models. Experimental Eye Research, 89 (5): 608-617.

Heinrich JN, Butera JA, Carrick T, Kramer A, Kowal D, Lock T, Marquis KL, Pausch MH, Popiolek M, Sun S-C, Tseng E, Uveges AJ, Mayer SC (2009). Pharmacological comparison of muscarinic ligands: Historical versus more recent muscarinic M1-preferring receptor agonists. European Journal of Pharmacology, 605 ( 1-3): 53-56.

Dschietzig T, Bartsch C, Baumann G, and Stangl K (2009). RXFP1-inactive relaxin activates human glucocorticoid receptor: Further investigations into the relaxin-GR pathway. Regulatory Peptides, 154 (1-3): 77-84.

Griffith DA, Hadcock JR, Black SC, Iredale PA, Carpino PA, DaSilva-Jardine P, Day R, DiBrino J, Dow RL, Landis MS, O’Connor RE and Scott DO (2009). Discovery of 1-[9-(4-Chlorophenyl)-8-(2-chlorophenyl) -9H-purin-6-yl] -4-ethylaminopiperidine-4-carboxylic Acid Amide (CP-945,598), a Novel, Potent, and Selective Cannabinoid Type 1 Receptor Antagonist. J. Med. Chem. 52 (2): 369–378.

Dastidar SG, Ray A, Shirumalla R, Rajagopal D, Chaudhary S, Nanda K, Sharma P, Seth MK, Balachandran S, Gupta N, Palle V (2009). Pharmacology of a Novel, Orally Active PDE4 Inhibitor. Pharmacology 83: 275-286.

Simon S, Young TJ, Nickolls SA (2009). The effect of assay formats on the estimation of melanocortin agonist affinity and efficacy using the operation model of agonism. European Journal of Pharmacology, 615 (1-3): 33-39.

Sanger GJ, Westaway SM, Barnes AA,. Macpherson DT, Muir AI, Jarvie EM, Bolton VN (2009). GSK962040: a small molecule, selective motilin receptor agonist, effective as a stimulant of human and rabbit gastrointestinal motility. Neurogastroenterology & Motility, 21 (6):657–e31.

Bazhina AV, Kahnerta S, Kimpflera S, Schadendorfc D and Umanskya V (2010). Distinct metabolism of cyclic adenosine monophosphate in regulatory and helper CD4+ T cells. Molecular Immunology, 47 (4): 678-684

King-Keller S, Li M, Smith A, Zheng S, Kaur G, Yang X, Wang B, Docampo R (2010). Chemical validation of phosphodiesterase C as a chemotherapeutic target in Trypanosoma cruzi, the etiological agent of Chagas' disease. Antimicrob. Agents Chemother. 54(9):3738-3745.

Hampton SL and Kinnaird AI (2010). Genetic interventions in mammalian cells; applications and uses in high-throughput screening and drug discovery. Cell Biology and Toxicology, 26 (1): 43-55.

Yang M, Chisholma JW, Soelaimana S and Shryocka JC (2010). Sulfonylureas uncouple glucose-dependence for GPR40-mediated enhancement of insulin secretion from INS-1E cells. Molecular and Cellular Endocrinology, 315 (1-2):308-313

Eapen MS, Sodhi R, Balakrishnan G, Dastidar S, Ray A and Vijayakrishnan L (2010). Evaluation of Nonradioactive Cell-Free cAMP Assays for Measuring in vitro Phosphodiesterase Activity. Pharmacology, 85(5):280-285.

Wanga Y, Jiaoa X, Kaysera F, Liua J, Wanga Z, Wanskaa M, Greenbergb J, Weiszmannb J, Hongfei Geb, Tian H, Wong S, Schwandnerd R, Leeb T and Lib Y (2010). The first synthetic agonists of FFA2: Discovery and SAR of phenylacetamides as allosteric modulators. Bioorganic & Medicinal Chemistry Letters, 20 (2): 493-498.

Cole DC, Gross JL, Comery TA, Aschmies S, Hirst WD, Kelley C, Kim JI, Ellingboe JW (2010). Benzimidazole- and indole-substituted 1,3′-bipyrrolidine benzamides as histamine H3 receptor antagonists. Bioorganic and Medicinal Chemistry Letters, 20 (3):1237-1240.

Bradley SR, Lameh J, Ohrmund L, Son T, Bajpai A, Nguyen D, Friberg M, Bonhaus DW (2010). AC-260584, an orally bioavailable M1 muscarinic receptor allosteric agonist, improves cognitive performance in an animal model. Neuropharmacology, 58 (2): 365-373.

Cheung AW, Brinkman J, Firooznia F, Flohr A, Grimsby J, Gubler ML, Guertin K, Hamid R, Marcopulos N, Norcross RD, Qi L, Ramsey G, Tan J, Wen Y and Sarabu R (2010). 4-Substituted-7-N-alkyl-N-acetyl 2-aminobenzothiazole amides: Drug-like and non-xanthine based A2B adenosine receptor antagonists. Bioorganic & Medicinal Chemistry Letters, 20 (14): 4140-4146.

Frost JM, Dart MJ, Tietje KR, Garrison TR, Grayson GK, Daza AV, El-Kouhen OF, Yao BB, Hsieh GC, Pai M, Zhu CZ, Chandran P, Michael D (2010). Meyer1.Indol-3-ylcycloalkyl Ketones: Effects of N1 Substituted Indole Side Chain Variations on CB2 Cannabinoid Receptor Activity. Journal of Medicinal Chemistry, 53 (1): 295-315.

Haque TS, Lee VG, Riexinger D, Lei M, Malmstrom S, Xin L, Han S, Krupinski J (2010). Identification of potent 11mer Glucagon-Like Peptide-1 Receptor agonist peptides with novel C-terminal amino acids: Homohomophenylalanine analogs. Peptides, 31 (5):950-955.

Dwyera JM, Platta BJ, Stacey J. Rizzoa SJS, Claudine M. Pulicicchioa CM, Wantucha C, Zhang M-Y, Cummonsa T, Leventhala L, Bendera CN, Zhang J, Kowal D, Lu S, S. Rajarao JR, Smith DL, Shilling AD, Wang J, Butera J, Resnick L, Rosenzweig-Lipson S, Schechter LE and Beyer CE (2010). Preclinical characterization of BRL 44408: antidepressant- and analgesic-like activity through selective α2A-adrenoceptor antagonism. The International Journal of Neuropsychopharmacology, 13:1193-1205

Lameh J, Bertozzi F, Kelly N, Jacobi PM, Nguyen D, Bajpai A, Gaubert G, Olsson R, and Gardell LR (2010). Neuropeptide ff receptors have opposing modulatory: Effects on nociception. J Pharmacol Exp Ther. 334:244-254.

Leonti M, Casu L, Raduner S, Cottiglia F, Floris C, Altmann K.-H, Gertsch J (2010). Falcarinol is a covalent cannabinoid CB1 receptor antagonist and induces pro-allergic effects in skin. Biochemical Pharmacology, 79 (12): 1815-1826.

Nygaard R, Valentin-Hansen L, Mokrosinski J, Frimurer TM and Schwartz TW (2010). Conserved Water-mediated Hydrogen Bond Network between TM-I, -II, -VI, and -VII in 7TM Receptor Activation. The Journal of Biological Chemistry, 285, 19625-19636.

Chen XP, Yang W, Fan Y, Luo JS, Hong K, Wang Z, Yan JF, Chen X, Lu JX, Benovic JL, Zhou NM (2010). Structural determinants in the second intracellular loop of the human cannabinoid CB(1) receptor mediate selective coupling to G(s) and G(i). Br J Pharmacol. [Epub ahead of print], PMID: 20735408.

East SP, Bamford S, Dietz MG, Eickmeier C, Flegg A, Ferger B, Gemkow MJ, Heilker R, Hengerer B, Kotey A, Loke P, Schänzle G, Schubert HD, Scott J, Whittaker M, Williams M, Zawadzki P, Gerlach K (2010). An orally bioavailable positive allosteric modulator of the mGlu4 receptor with efficacy in an animal model of motor dysfunction. Bioorg. Med. Chem. Lett. 15;20(16):4901-5.