Search Results - "PETTIBONE, Douglas J"

International Union of Pharmacology. XLV. Classification of the Kinin Receptor Family: from Molecular Mechanisms to Pathophysiological Consequences by Leeb-Lundberg, LMFredrik, Marceau, Francois, Muller-Esterl, Werner, Pettibone, Douglas J, Zuraw, Bruce L

“…Kinins are proinflammatory peptides that mediate numerous vascular and pain responses to tissue injury. Two pharmacologically distinct kinin receptor subtypes…”
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A novel selective positive allosteric modulator of metabotropic glutamate receptor subtype 5 has in vivo activity and antipsychotic-like effects in rat behavioral models by Kinney, Gene G, O'Brien, Julie A, Lemaire, Wei, Burno, Maryann, Bickel, Denise J, Clements, Michelle K, Chen, Tsing-Bau, Wisnoski, David D, Lindsley, Craig W, Tiller, Philip R, Smith, Sheri, Jacobson, Marlene A, Sur, Cyrille, Duggan, Mark E, Pettibone, Douglas J, Conn, P Jeffrey, Williams, Jr, David L

“…We found that 3-cyano-N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamide (CDPPB) is a potent and selective positive allosteric modulator of the metabotropic glutamate…”
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N-Desmethylclozapine, an Allosteric Agonist at Muscarinic 1 Receptor, Potentiates N-Methyl-D-Aspartate Receptor Activity by Sur, Cyrille, Mallorga, Pierre J., Wittmann, Marion, Jacobson, Marlene A., Pascarella, Danette, Williams, Jacinta B., Brandish, Philip E., Pettibone, Douglas J., Scolnick, Edward M., Conn, P. Jeffrey

“…The molecular and neuronal substrates conferring on clozapine its unique and superior efficacy in the treatment of schizophrenia remain elusive. The…”
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A family of highly selective allosteric modulators of the metabotropic glutamate receptor subtype 5 by O'Brien, Julie A, Lemaire, Wei, Chen, Tsing-Bau, Chang, Raymond S L, Jacobson, Marlene A, Ha, Sookhee N, Lindsley, Craig W, Schaffhauser, Hervé J, Sur, Cyrille, Pettibone, Douglas J, Conn, P Jeffrey, Williams, Jr, David L

“…We have identified a family of highly selective allosteric modulators of the group I metabotropic glutamate receptor subtype 5 (mGluR5). This family of closely…”
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A novel selective allosteric modulator potentiates the activity of native metabotropic glutamate receptor subtype 5 in rat forebrain by O'Brien, Julie A, Lemaire, Wei, Wittmann, Marion, Jacobson, Marlene A, Ha, Sookhee N, Wisnoski, David D, Lindsley, Craig W, Schaffhauser, Hervé J, Rowe, Blake, Sur, Cyrille, Duggan, Mark E, Pettibone, Douglas J, Conn, P Jeffrey, Williams, Jr, David L

“…We found that N-[4-chloro-2-[(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl]phenyl]-2-hydroxybenzamide (CPPHA), is a potent and selective positive allosteric…”
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The effects of deleting the mouse neurotensin receptor NTR1 on central and peripheral responses to neurotensin by Pettibone, Douglas J, Hess, J Fred, Hey, Patricia J, Jacobson, Marlene A, Leviten, Michael, Lis, Edward V, Mallorga, Pierre J, Pascarella, Danette M, Snyder, Melissa A, Williams, Jacinta B, Zeng, Zhizhen

“…Mice deficient in the neurotensin (NT)-1 receptor (NTR1) were developed to characterize the NT receptor subtypes that mediate various in vivo responses to NT…”
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Design, Synthesis, and In Vivo Efficacy of Glycine Transporter-1 (GlyT1) Inhibitors Derived from a Series of [4-Phenyl-1-(propylsulfonyl)piperidin-4-yl]methyl Benzamides by Lindsley, Craig W., Zhao, Zhijian, Leister, William H., O'Brien, Julie, Lemaire, Wei, Williams Jr, David L., Chen, Tsing-Bau, Chang, Raymond S. L., Burno, Maryann, Jacobson, Marlene A., Sur, Cyrille, Kinney, Gene G., Pettibone, Douglas J., Tiller, Philip R., Smith, Sheri, Tsou, Nancy N., Duggan, Mark E., Conn, P. Jeffrey, Hartman, George D.

“…An iterative analogue library synthesis approach rapidly delivered (S)‐13 h, a potent, reversible, and selective GlyT1 inhibitor. (S)‐13 h selectively…”
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Discovery of a Potent, Non-peptide Bradykinin B1 Receptor Antagonist by Su, Dai-Shi, Markowitz, M. Kristine, DiPardo, Robert M, Murphy, Kathy L, Harrell, C. Meacham, O'Malley, Stacy S, Ransom, Richard W, Chang, Raymond S. L, Ha, Sookhee, Hess, Fred J, Pettibone, Douglas J, Mason, Glenn S, Boyce, Susan, Freidinger, Roger M, Bock, Mark G

“…Bradykinin (BK) plays an important role in the pathophysiological processes accompanying pain and inflammation. Selective bradykinin B1 receptor antagonists…”
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Development of a scintillation proximity assay for analysis of Na +/Cl −-dependent neurotransmitter transporter activity by Williams, Jacinta B, Mallorga, Pierre J, Lemaire, Wei, Williams, David L, Na, Sang, Patel, Smita, Conn, Jeffrey P, Pettibone, Douglas J, Austin, Christopher, Sur, Cyrille

“…Human placental choriocarcinoma (JAR) cells endogenously expressing glycine transporter type 1a (GlyT1a) have been cultured in 96-well scintillating…”
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Generation and characterization of a human bradykinin receptor B1 transgenic rat as a pharmacodynamic model by Hess, J Fred, Ransom, Richard W, Zeng, Zhizhen, Chang, Raymond S L, Hey, Patricia J, Warren, Lee, Harrell, Charles M, Murphy, Kathryn L, Chen, Tsing-Bau, Miller, Patricia J, Lis, Edward, Reiss, Duane, Gibson, Raymond E, Markowitz, M Kristine, DiPardo, Robert M, Su, Dai-Shi, Bock, Mark G, Gould, Robert J, Pettibone, Douglas J

“…Antagonists of the B1 bradykinin receptor (B1R) offer the promise of novel therapeutic agents for the treatment of inflammatory and neuropathic pain. However,…”
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Development of Orally Active Oxytocin Antagonists:  Studies on 1-(1-{4-[1-(2-Methyl-1-oxidopyridin-3-ylmethyl)piperidin-4-yloxy]-2- methoxybenzoyl}piperidin-4-yl)-1,4-dihydrobenz[d][1,3]oxazin-2-one (L-372,662) and Related Pyridines by Bell, Ian M, Erb, Jill M, Freidinger, Roger M, Gallicchio, Steven N, Guare, James P, Guidotti, Maribeth T, Halpin, Rita A, Hobbs, Doug W, Homnick, Carl F, Kuo, Michelle S, Lis, Edward V, Mathre, David J, Michelson, Stuart R, Pawluczyk, Joseph M, Pettibone, Douglas J, Reiss, Duane R, Vickers, Stanley, Williams, Peter D, Woyden, Carla J

“…The previously reported oxytocin antagonist L-371,257 (2) has been modified at its acetylpiperidine terminus to incorporate various pyridine N-oxide groups…”
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Bradykinin B1 receptor antagonists : An α-hydroxy amide with an improved metabolism profile by KUDUK, Scott D, CHANG, Ronald K, BOCK, Mark G, DIPARDO, Robert M, DI MARCO, Christina N, MURPHY, Kathy L, RANSOM, Richard W, REISS, Duane R, TANG, Cuyue, PRUEKSARITANONT, Thomayant, PETTIBONE, Douglas J

“…A series of carbo- and heterocyclic alpha-hydroxy amide-derived bradykinin B1 antagonists was prepared and evaluated. A 4,4-difluorocyclohexyl alpha-hydroxy…”
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Development of Orally Bioavailable and CNS Penetrant Biphenylaminocyclopropane Carboxamide Bradykinin B1 Receptor Antagonists by Kuduk, Scott D., Di Marco, Christina N., Chang, Ronald K., Wood, Michael R., Schirripa, Kathy M., Kim, June J., Wai, Jenny M. C., DiPardo, Robert M., Murphy, Kathy L., Ransom, Richard W., Harrell, C. Meacham, Reiss, Duane R., Holahan, Marie A., Cook, Jacquelynn, Hess, J. Fred, Sain, Nova, Urban, Mark O., Tang, Cuyue, Prueksaritanont, Thomayant, Pettibone, Douglas J., Bock, Mark G.

“…A series of biphenylaminocyclopropane carboxamide based bradykinin B1 receptor antagonists has been developed that possesses good pharmacokinetic properties…”
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Indazole derivatives as novel bradykinin B1 receptor antagonists by BODMER-NARKEVITCH, Vera, ANTHONY, Neville J, BOCK, Mark G, KUDUK, Scott D, COFRE, Victoria, JOLLY, Samson M, MURPHY, Kathy L, RANSOM, Richard W, REISS, Duane R, CUYUE TANG, PRUEKSARITANONT, Thomayant, PETTIBONE, Douglas J

“…A new class of indazole-derived bradykinin B(1) antagonists and their structure-activity relationships (SAR) is reported. A number of compounds were found to…”
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Pharmacology and expression analysis of glycine transporter GlyT1 with [ 3H]-(N-[3-(4′-fluorophenyl)-3-(4′phenylphenoxy)propyl])sarcosine by Mallorga, Pierre J, Williams, Jacinta B, Jacobson, Marlene, Marques, Rosemary, Chaudhary, Ashok, Conn, P.Jeffrey, Pettibone, Douglas J, Sur, Cyrille

“…In the central nervous system, re-uptake of the neurotransmitter glycine is mediated by two different glycine transporters, GlyT1 and GlyT2. GlyT2 is found in…”
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Orally active, nonpeptide oxytocin antagonists by Evans, Ben E, Leighton, James L, Rittle, Kenneth E, Gilbert, Kevin F, Lundell, George F, Gould, Norman P, Hobbs, Doug W, DiPardo, Robert M, Veber, Daniel F, Pettibone, Douglas J, Clineschmidt, Bradley V, Anderson, Paul S, Freidinger, Roger M

“…The first nonpeptide antagonists of the neurohypophyseal hormone, oxytocin (OT) are described. Derivatives of the spiroindenepiperidine ring system, these…”
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Effects of typical and atypical antipsychotics on human glycine transporters by Williams, Jacinta B., Mallorga, Pierre J., Jeffrey Conn, P., Pettibone, Douglas J., Sur, Cyrille

“…Augmentation strategy in the treatment of schizophrenia with the NMDA receptor co-agonist glycine has demonstrated significant improvement in patient symptoms…”
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2-Aminobenzophenones as a Novel Class of Bradykinin B1 Receptor Antagonists by Su, Dai-Shi, Lim, John L, Tinney, Elizabeth, Wan, Bang-Lin, Murphy, Kathy L, Reiss, Duane R, Harrell, C. Meacham, O’Malley, Stacy S, Ransom, Rick W, Chang, Raymond S. L, Pettibone, Douglas J, Yu, Jian, Tang, Cuyue, Prueksaritanont, Thomayant, Freidinger, Roger M, Bock, Mark G, Anthony, Neville J

“…Selective bradykinin (BK) B1 receptor antagonists could be novel therapeutic agents for the treatment of pain and inflammation. Elucidation of the structure…”
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Cyclopropylamino Acid Amide as a Pharmacophoric Replacement for 2,3-Diaminopyridine. Application to the Design of Novel Bradykinin B1 Receptor Antagonists by Wood, Michael R, Schirripa, Kathy M, Kim, June J, Wan, Bang-Lin, Murphy, Kathy L, Ransom, Richard W, Chang, Raymond S. L, Tang, Cuyue, Prueksaritanont, Thomayant, Detwiler, Theodore J, Hettrick, Lisa A, Landis, Elizabeth R, Leonard, Yvonne M, Krueger, Julie A, Lewis, Sidney D, Pettibone, Douglas J, Freidinger, Roger M, Bock, Mark G

“…Antagonism of the bradykinin B1 receptor represents a potential treatment for chronic pain and inflammation. Novel antagonists were designed that display…”
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Bradykinin B1 antagonists : Biphenyl SAR studies in the cyclopropanecarboxamide series by KUDUK, Scott D, DIPARDO, Robert M, BOCK, Mark G, CHANG, Ronald K, DI MARCO, Christina N, MURPHY, Kathy L, RANSOM, Richard W, REISS, Duane R, TANG, Cuyue, PRUEKSARITANONT, Thomayant, PETTIBONE, Douglas J

“…SAR study of the biphenyl region of cyclopropanecarboxamide derived bradykinin B(1) antagonists was examined. Incorporation of a pyridine in place of the…”
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