Frederick J Ehlert

Title(s)Recall Faculty, Pharmaceutical Sciences
Address101 Theory, Suite 100
Irvine CA 92697-3958
Phone(949) 824-6208, 6928
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    1. Quantitating Ligand Bias Using the Competitive Model of Ligand Activity. Methods Mol Biol. 2019; 1957:235-247. Stahl EL, Ehlert FJ, Bohn LM. PMID: 30919358.
      View in: PubMed   Mentions:    Fields:    
    2. Analysis of Biased Agonism. Prog Mol Biol Transl Sci. 2018; 160:63-104. Ehlert FJ. PMID: 30470293.
      View in: PubMed   Mentions: 1     Fields:    Translation:HumansAnimals
    3. PDE8 Is Expressed in Human Airway Smooth Muscle and Selectively Regulates cAMP Signaling by ß2-Adrenergic Receptors and Adenylyl Cyclase 6. Am J Respir Cell Mol Biol. 2018 04; 58(4):530-541. Johnstone TB, Smith KH, Koziol-White CJ, Li F, Kazarian AG, Corpuz ML, Shumyatcher M, Ehlert FJ, Himes BE, Panettieri RA, Ostrom RS. PMID: 29262264.
      View in: PubMed   Mentions: 4     Fields:    Translation:HumansCells
    4. Estimation of the receptor-state affinity constants of ligands in functional studies using wild type and constitutively active mutant receptors: Implications for estimation of agonist bias. J Pharmacol Toxicol Methods. 2017 Jan - Feb; 83:94-106. Ehlert FJ, Stein RS. PMID: 27725245.
      View in: PubMed   Mentions: 1     Fields:    Translation:HumansCells
    5. Cooperativity Has Empirical and Ultimate Levels of Explanation. Trends Pharmacol Sci. 2016 08; 37(8):620-623. Ehlert FJ. PMID: 27364140.
      View in: PubMed   Mentions:    Fields:    Translation:Cells
    6. Functional studies cast light on receptor states. Trends Pharmacol Sci. 2015 Sep; 36(9):596-604. Ehlert FJ. PMID: 26123416.
      View in: PubMed   Mentions: 7     Fields:    Translation:HumansAnimalsCells
    7. Intrinsic relative activities of ? opioid agonists in activating Ga proteins and internalizing receptor: Differences between human and mouse receptors. Eur J Pharmacol. 2015 Aug 15; 761:235-44. DiMattio KM, Ehlert FJ, Liu-Chen LY. PMID: 26057692.
      View in: PubMed   Mentions: 8     Fields:    Translation:HumansAnimalsCells
    8. A novel method for analyzing extremely biased agonism at G protein-coupled receptors. Mol Pharmacol. 2015 May; 87(5):866-77. Stahl EL, Zhou L, Ehlert FJ, Bohn LM. PMID: 25680753.
      View in: PubMed   Mentions: 20     Fields:    Translation:AnimalsCells
    9. A kinetic model of GPCRs: analysis of G protein activity, occupancy, coupling and receptor-state affinity constants. J Recept Signal Transduct Res. 2015; 35(4):269-83. Stein RS, Ehlert FJ. PMID: 25353707.
      View in: PubMed   Mentions: 5     Fields:    Translation:HumansAnimalsCells
    10. International Union of Basic and Clinical Pharmacology. XC. multisite pharmacology: recommendations for the nomenclature of receptor allosterism and allosteric ligands. Pharmacol Rev. 2014 Oct; 66(4):918-47. Christopoulos A, Changeux JP, Catterall WA, Fabbro D, Burris TP, Cidlowski JA, Olsen RW, Peters JA, Neubig RR, Pin JP, Sexton PM, Kenakin TP, Ehlert FJ, Spedding M, Langmead CJ. PMID: 25026896.
      View in: PubMed   Mentions: 36     Fields:    Translation:HumansCells
    11. Estimation of ligand affinity constants for receptor states in functional studies involving the allosteric modulation of G protein-coupled receptors: implications for ligand bias. J Pharmacol Toxicol Methods. 2014 May-Jun; 69(3):253-79. Ehlert FJ, Griffin MT. PMID: 24434717.
      View in: PubMed   Mentions: 4     Fields:    Translation:HumansCells
    12. Effects of asparagine mutagenesis of conserved aspartic acids in helix 2 (D2.50) and 3 (D3.32) of M1-M4 muscarinic receptors on the irreversible binding of nitrogen mustard analogs of acetylcholine and McN-A-343. Biochemistry. 2013 Jul 23; 52(29):4914-28. Suga H, Ehlert FJ. PMID: 23826889.
      View in: PubMed   Mentions: 1     Fields:    Translation:HumansAnimalsCells
    13. What ligand-gated ion channels can tell us about the allosteric regulation of G protein-coupled receptors. Prog Mol Biol Transl Sci. 2013; 115:291-347. Ehlert FJ. PMID: 23415097.
      View in: PubMed   Mentions: 1     Fields:    Translation:HumansAnimalsCells
    14. Muscarinic agonists and antagonists: effects on gastrointestinal function. Handb Exp Pharmacol. 2012; (208):343-74. Ehlert FJ, Pak KJ, Griffin MT. PMID: 22222706.
      View in: PubMed   Mentions: 7     Fields:    Translation:HumansAnimalsCells
    15. Quantifying agonist activity at G protein-coupled receptors. J Vis Exp. 2011 Dec 26; (58):e3179. Ehlert FJ, Suga H, Griffin MT. PMID: 22231636.
      View in: PubMed   Mentions: 3     Fields:    Translation:AnimalsCells
    16. Characterization of muscarinic receptors in the human bladder mucosa: direct quantification of subtypes using 4-DAMP mustard. Urology. 2011 Sep; 78(3):721.e7-721.e12. Yoshida A, Seki M, Nasrin S, Otsuka A, Ozono S, Takeda M, Masuyama K, Araki I, Ehlert FJ, Yamada S. PMID: 21777958.
      View in: PubMed   Mentions:    Fields:    Translation:HumansCells
    17. Analysis of agonism and inverse agonism in functional assays with constitutive activity: estimation of orthosteric ligand affinity constants for active and inactive receptor states. J Pharmacol Exp Ther. 2011 Aug; 338(2):671-86. Ehlert FJ, Suga H, Griffin MT. PMID: 21576379.
      View in: PubMed   Mentions: 9     Fields:    Translation:HumansCells
    18. Analysis of functional responses at G protein-coupled receptors: estimation of relative affinity constants for the inactive receptor state. J Pharmacol Exp Ther. 2011 Aug; 338(2):658-70. Ehlert FJ, Griffin MT, Suga H. PMID: 21576380.
      View in: PubMed   Mentions: 7     Fields:    Translation:HumansAnimalsCells
    19. Mutagenesis of nucleophilic residues near the orthosteric binding pocket of M1 and M2 muscarinic receptors: effect on the binding of nitrogen mustard analogs of acetylcholine and McN-A-343. Mol Pharmacol. 2010 Oct; 78(4):745-55. Suga H, Sawyer GW, Ehlert FJ. PMID: 20643905.
      View in: PubMed   Mentions: 1     Fields:    Translation:HumansAnimalsCells
    20. Investigating the interaction of McN-A-343 with the M2 muscarinic receptor using its nitrogen mustard derivative. Biochem Pharmacol. 2010 Apr 01; 79(7):1025-35. Suga H, Ehlert FJ. PMID: 19913516.
      View in: PubMed   Mentions: 3     Fields:    Translation:AnimalsCells
    21. A conserved motif in the membrane proximal C-terminal tail of human muscarinic m1 acetylcholine receptors affects plasma membrane expression. J Pharmacol Exp Ther. 2010 Jan; 332(1):76-86. Sawyer GW, Ehlert FJ, Shults CA. PMID: 19841475.
      View in: PubMed   Mentions: 11     Fields:    Translation:HumansAnimalsCells
    22. The guinea pig ileum lacks the direct, high-potency, M(2)-muscarinic, contractile mechanism characteristic of the mouse ileum. Naunyn Schmiedebergs Arch Pharmacol. 2009 Oct; 380(4):327-35. Griffin MT, Matsui M, Ostrom RS, Ehlert FJ. PMID: 19582435.
      View in: PubMed   Mentions: 2     Fields:    Translation:Animals
    23. Estimation of relative microscopic affinity constants of agonists for the active state of the receptor in functional studies on M2 and M3 muscarinic receptors. Mol Pharmacol. 2009 Feb; 75(2):381-96. Tran JA, Chang A, Matsui M, Ehlert FJ. PMID: 18996972.
      View in: PubMed   Mentions: 16     Fields:    Translation:HumansAnimalsCells
    24. Selectivity of agonists for the active state of M1 to M4 muscarinic receptor subtypes. J Pharmacol Exp Ther. 2009 Jan; 328(1):331-42. Figueroa KW, Griffin MT, Ehlert FJ. PMID: 18824613.
      View in: PubMed   Mentions: 29     Fields:    Translation:HumansAnimalsCells
    25. Use of acetylcholine mustard to study allosteric interactions at the M(2) muscarinic receptor. J Pharmacol Exp Ther. 2008 Nov; 327(2):518-28. Suga H, Figueroa KW, Ehlert FJ. PMID: 18682569.
      View in: PubMed   Mentions: 4     Fields:    Translation:HumansAnimalsCells
    26. 5th International Symposium on receptor mechanisms, signal transduction and drug effects. Naunyn Schmiedebergs Arch Pharmacol. 2008 Jun; 377(4-6):267-8. Yamada S, Ehlert FJ, Hollenberg MD. PMID: 18357439.
      View in: PubMed   Mentions:    Fields:    Translation:HumansCells
    27. Two-state models and the analysis of the allosteric effect of gallamine at the M2 muscarinic receptor. J Pharmacol Exp Ther. 2008 Jun; 325(3):1039-60. Ehlert FJ, Griffin MT. PMID: 18305010.
      View in: PubMed   Mentions: 11     Fields:    Translation:HumansAnimalsCells
    28. On the analysis of ligand-directed signaling at G protein-coupled receptors. Naunyn Schmiedebergs Arch Pharmacol. 2008 Jun; 377(4-6):549-77. Ehlert FJ. PMID: 18253722.
      View in: PubMed   Mentions: 28     Fields:    Translation:HumansAnimalsCells
    29. Cysteine pairs in the third intracellular loop of the muscarinic m1 acetylcholine receptor play a role in agonist-induced internalization. J Pharmacol Exp Ther. 2008 Jan; 324(1):196-205. Sawyer GW, Ehlert FJ, Shults CA. PMID: 17540859.
      View in: PubMed   Mentions: 1     Fields:    Translation:HumansAnimalsCells
    30. Neuronally released acetylcholine acts on the M2 muscarinic receptor to oppose the relaxant effect of isoproterenol on cholinergic contractions in mouse urinary bladder. J Pharmacol Exp Ther. 2007 Aug; 322(2):631-7. Ehlert FJ, Ahn S, Pak KJ, Park GJ, Sangnil MS, Tran JA, Matsui M. PMID: 17473176.
      View in: PubMed   Mentions: 10     Fields:    Translation:AnimalsCells
    31. Estimation of agonist activity at G protein-coupled receptors: analysis of M2 muscarinic receptor signaling through Gi/o,Gs, and G15. J Pharmacol Exp Ther. 2007 Jun; 321(3):1193-207. Griffin MT, Figueroa KW, Liller S, Ehlert FJ. PMID: 17392404.
      View in: PubMed   Mentions: 35     Fields:    Translation:HumansAnimalsCells
    32. Differential coupling of muscarinic M1, M2, and M3 receptors to phosphoinositide hydrolysis in urinary bladder and longitudinal muscle of the ileum of the mouse. J Pharmacol Exp Ther. 2006 Aug; 318(2):649-56. Tran JA, Matsui M, Ehlert FJ. PMID: 16675640.
      View in: PubMed   Mentions: 4     Fields:    Translation:AnimalsCells
    33. Determination of the rate of muscarinic M1 receptor plasma membrane delivery using a regulated secretion/aggregation system. J Pharmacol Toxicol Methods. 2006 May-Jun; 53(3):219-33. Sawyer GW, Ehlert FJ, Hart JP. PMID: 16213169.
      View in: PubMed   Mentions: 4     Fields:    Translation:HumansAnimalsCells
    34. Analysis of allosterism in functional assays. J Pharmacol Exp Ther. 2005 Nov; 315(2):740-54. Ehlert FJ. PMID: 16046613.
      View in: PubMed   Mentions: 31     Fields:    
    35. The M2 muscarinic receptor mediates contraction through indirect mechanisms in mouse urinary bladder. J Pharmacol Exp Ther. 2005 Apr; 313(1):368-78. Ehlert FJ, Griffin MT, Abe DM, Vo TH, Taketo MM, Manabe T, Matsui M. PMID: 15608083.
      View in: PubMed   Mentions: 24     Fields:    Translation:AnimalsCells
    36. Functional analysis of muscarinic acetylcholine receptors using knockout mice. Life Sci. 2004 Nov 05; 75(25):2971-81. Matsui M, Yamada S, Oki T, Manabe T, Taketo MM, Ehlert FJ. PMID: 15474550.
      View in: PubMed   Mentions: 16     Fields:    Translation:Animals
    37. Comparison of the antimuscarinic action of p-fluorohexahydrosiladifenidol in ileal and tracheal smooth muscle. J Pharmacol Exp Ther. 2005 Feb; 312(2):592-600. Ehlert FJ, Hsu JC, Leung K, Lee AG, Shehnaz D, Griffin MT. PMID: 15456838.
      View in: PubMed   Mentions:    Fields:    Translation:AnimalsCells
    38. Contractile role of M2 and M3 muscarinic receptors in gastrointestinal, airway and urinary bladder smooth muscle. Life Sci. 2003 Dec 05; 74(2-3):355-66. Ehlert FJ. PMID: 14607264.
      View in: PubMed   Mentions: 24     Fields:    Translation:HumansAnimalsCells
    39. Muscarinic agonist-mediated heterologous desensitization in isolated ileum requires activation of both muscarinic M2 and M3 receptors. J Pharmacol Exp Ther. 2004 Jan; 308(1):339-49. Griffin MT, Matsui M, Shehnaz D, Ansari KZ, Taketo MM, Manabe T, Ehlert FJ. PMID: 14563784.
      View in: PubMed   Mentions: 5     Fields:    Translation:Animals
    40. Comparison of the pharmacological antagonism of M2 and M3 muscarinic receptors expressed in isolation and in combination. Biochem Pharmacol. 2003 Apr 15; 65(8):1227-41. Griffin MT, Hsu JC, Shehnaz D, Ehlert FJ. PMID: 12694864.
      View in: PubMed   Mentions: 8     Fields:    Translation:HumansAnimalsCells
    41. Increased relaxant action of forskolin and isoproterenol against muscarinic agonist-induced contractions in smooth muscle from M2 receptor knockout mice. J Pharmacol Exp Ther. 2003 Apr; 305(1):106-13. Matsui M, Griffin MT, Shehnaz D, Taketo MM, Ehlert FJ. PMID: 12649358.
      View in: PubMed   Mentions: 16     Fields:    Translation:Animals
    42. Pharmacological analysis of the contractile role of M2 and M3 muscarinic receptors in smooth muscle. Receptors Channels. 2003; 9(4):261-77. Ehlert FJ. PMID: 12893538.
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    43. Identification and molecular characterization of two closely related G protein-coupled receptors activated by prokineticins/endocrine gland vascular endothelial growth factor. J Biol Chem. 2002 May 31; 277(22):19276-80. Lin DC, Bullock CM, Ehlert FJ, Chen JL, Tian H, Zhou QY. PMID: 11886876.
      View in: PubMed   Mentions: 89     Fields:    Translation:HumansAnimalsCells
    44. Acetylcholine-induced desensitization of muscarinic contractile response in Guinea pig ileum is inhibited by pertussis toxin treatment. J Pharmacol Exp Ther. 2001 Dec; 299(3):1126-32. Ehlert FJ, Ansari KZ, Shehnaz D, Sawyer GW, Griffin MT. PMID: 11714903.
      View in: PubMed   Mentions:    Fields:    Translation:AnimalsCells
    45. A simple method for estimation of agonist activity at receptor subtypes: comparison of native and cloned M3 muscarinic receptors in guinea pig ileum and transfected cells. J Pharmacol Exp Ther. 1999 May; 289(2):981-92. Ehlert FJ, Griffin MT, Sawyer GW, Bailon R. PMID: 10215678.
      View in: PubMed   Mentions: 24     Fields:    Translation:AnimalsCells
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