Search Results - "Ott, Thomas R"

Structural requirements of transmembrane domain 3 for activation by the M1 muscarinic receptor agonists AC-42, AC-260584, clozapine, and N-desmethylclozapine: evidence for three distinct modes of receptor activation by Spalding, Tracy A, Ma, Jian-Nong, Ott, Thomas R, Friberg, Mikael, Bajpai, Abhishek, Bradley, Stefania Risso, Davis, Robert E, Brann, Mark R, Burstein, Ethan S

“…Transmembrane domain 3 (TM3) plays a crucial role mediating muscarinic acetylcholine receptor activation by acetylcholine, carbachol, and other muscarinic…”
Get more information

A Transcriptionally Active Human Type II Gonadotropin-Releasing Hormone Receptor Gene Homolog Overlaps Two Genes in the Antisense Orientation on Chromosome 1q.12 by Morgan, Kevin, Conklin, Darrell, Pawson, Adam J, Sellar, Robin, Ott, Thomas R, Millar, Robert P

“…GnRH-II peptide hormone exhibits complete sequence conservation across vertebrate species, including man. Type-II GnRH receptor genes have been characterized…”
Get full text

Characterization of the Mas‐related gene family: structural and functional conservation of human and rhesus MrgX receptors by Burstein, Ethan S, Ott, Thomas R, Feddock, Michele, Ma, Jian‐Nong, Fuhs, Steve, Wong, Steven, Schiffer, Hans H, Brann, Mark R, Nash, Norman R

“…Recently, a large family of G‐protein‐coupled receptors called Mas‐related genes (Mrgs), which is selectively expressed in small‐diameter sensory neurons of…”
Get full text

Identification of CC Chemokine Receptor 7 Residues Important for Receptor Activation by Ott, Thomas R, Pahuja, Anil, Nickolls, Sarah A, Alleva, David G, Struthers, R Scott

“…The binding pocket of family A GPCRs that bind small biogenic amines is well characterized. In this study we identify residues on CC chemokine receptor 7…”
Get full text

Two Mutations in Extracellular Loop 2 of the Human GnRH Receptor Convert an Antagonist to an Agonist by Ott, Thomas R, Troskie, Brigitte E, Roeske, Roger W, Illing, Nicola, Flanagan, Colleen A, Millar, Robert P

“…GnRH regulates the reproductive system through cognate G protein-coupled receptors in vertebrates. Certain GnRH analogs that are antagonists at mammalian…”
Get full text

Synthesis and Evaluation of Dibenzothiazepines: A Novel Class of Selective Cannabinoid-1 Receptor Inverse Agonists by Pettersson, Hanna, Bülow, Anne, Ek, Fredrik, Jensen, Jacob, Ottesen, Lars K, Fejzic, Alma, Ma, Jian-Nong, Del Tredici, Andria L, Currier, Erika A, Gardell, Luis R, Tabatabaei, Ali, Craig, Darren, McFarland, Krista, Ott, Thomas R, Piu, Fabrice, Burstein, Ethan S, Olsson, Roger

“…A novel class of CB1 inverse agonists was discovered. To efficiently establish structure−activity relationships (SARs), new synthetic methodologies amenable…”
Get full text

The N-terminal domain of CCL21 reconstitutes high affinity binding, G protein activation, and chemotactic activity, to the C-terminal domain of CCL19 by Ott, Thomas R., Lio, Francisco M., Olshefski, Dennis, Liu, Xin-Jun, Ling, Nicholas, Struthers, R. Scott

“…CC chemokine receptor 7 (CCR7), which regulates the trafficking of leucocytes to the secondary lymphoid organs, has two endogenous chemokine ligands: CCL19 and…”
Get full text

A high-throughput chemotaxis assay for pharmacological characterization of chemokine receptors: Utilization of U937 monocytic cells by Ott, Thomas R., Pahuja, Anil, Lio, Francisco M., Mistry, Monica S., Gross, Molly, Hudson, Sarah C., Wade, Warren S., Simpson, Pedro B., Struthers, R. Scott, Alleva, David G.

“…Introduction: Higher-throughput chemotaxis assays have had limited use in chemokine receptor pharmacology studies mainly because of the unavailability of…”
Get full text

A Chicken Gonadotropin-releasing Hormone Receptor That Confers Agonist Activity to Mammalian Antagonists by Sun, Yuh-Man, Flanagan, Colleen A., Illing, Nicola, Ott, Thomas R., Sellar, Robin, Fromme, Bernhard J., Hapgood, Janet, Sharp, Peter, Sealfon, Stuart C., Millar, Robert P.

“…Mammalian receptors for gonadotropin-releasing hormone (GnRH) have over 85% sequence homology and similar ligand selectivity. Biological studies indicated that…”
Get full text

AC-260584, an orally bioavailable M1 muscarinic receptor allosteric agonist, improves cognitive performance in an animal model by Bradley, Stefania Risso, Lameh, Jelveh, Ohrmund, Linda, Son, Thomas, Bajpai, Abhishek, Nguyen, Derek, Friberg, Mikael, Burstein, Ethan S., Spalding, Tracy A., Ott, Thomas R., Schiffer, Hans H., Tabatabaei, Ali, McFarland, Krista, Davis, Robert E., Bonhaus, Douglas W.

Get full text

AC-260584, an orally bioavailable M 1 muscarinic receptor allosteric agonist, improves cognitive performance in an animal model by Bradley, Stefania Risso, Lameh, Jelveh, Ohrmund, Linda, Son, Thomas, Bajpai, Abhishek, Nguyen, Derek, Friberg, Mikael, Burstein, Ethan S., Spalding, Tracy A., Ott, Thomas R., Schiffer, Hans H., Tabatabaei, Ali, McFarland, Krista, Davis, Robert E., Bonhaus, Douglas W.

“…The recent discovery of allosteric potentiators and agonists of the muscarinic M 1 receptor represents a significant advance in the muscarinic receptor…”
Get full text

Pharmacological and behavioral profile of N-(4-fluorophenylmethyl)-N-(1-methylpiperidin-4-yl)-N'-(4-(2-methylpropyloxy)phenylmethyl) carbamide (2R,3R)-dihydroxybutanedioate (2:1) (ACP-103), a novel 5-hydroxytryptamine(2A) receptor inverse agonist by Vanover, Kimberly E, Weiner, David M, Makhay, Malath, Veinbergs, Isaac, Gardell, Luis R, Lameh, Jelveh, Del Tredici, Andria L, Piu, Fabrice, Schiffer, Hans H, Ott, Thomas R, Burstein, Ethan S, Uldam, Allan K, Thygesen, Mikkel B, Schlienger, Nathalie, Andersson, Carl Magnus, Son, Thomas Y, Harvey, Scott C, Powell, Susan B, Geyer, Mark A, Tolf, Bo-Ragner, Brann, Mark R, Davis, Robert E

“…The in vitro and in vivo pharmacological properties of N-(4-fluorophenylmethyl)-N-(1-methylpiperidin-4-yl)-N'-(4-(2-methylpropyloxy)phenylmethyl)carbamide…”
Get more information

AC-260584, an orally bioavailable M sub(1) muscarinic receptor allosteric agonist, improves cognitive performance in an animal model by Bradley, Stefania Risso, Lameh, Jelveh, Ohrmund, Linda, Son, Thomas, Bajpai, Abhishek, Nguyen, Derek, Friberg, Mikael, Burstein, Ethan S, Spalding, Tracy A, Ott, Thomas R, Schiffer, Hans H, Tabatabaei, Ali, McFarland, Krista, Davis, Robert E, Bonhaus, Douglas W

“…The recent discovery of allosteric potentiators and agonists of the muscarinic M sub(1) receptor represents a significant advance in the muscarinic receptor…”
Get full text

A chicken gonadotropin-releasing hormone receptor that confers agonist activity to mammalian antagonists. Identification of D-Lys(6) in the ligand and extracellular loop two of the receptor as determinants by Sun, Y M, Flanagan, C A, Illing, N, Ott, T R, Sellar, R, Fromme, B J, Hapgood, J, Sharp, P, Sealfon, S C, Millar, R P

“…Mammalian receptors for gonadotropin-releasing hormone (GnRH) have over 85% sequence homology and similar ligand selectivity. Biological studies indicated that…”
Get full text

In Vitro pharmacology of N‐desmethylclozapine (ACP‐104) as compared to other atypical antipsychotic agents by Lameh, Jelveh, Bradley, Stefania Risso, Schiffer, Hans H., Ma, Jian‐Nong, Ott, Thomas R., Son, Thomas, Nguyen, Derek, Burstein, Ethan S., Bonhaus, Douglas W.

“…Effective treatment with antipsychotics depends on the balance between their activities at multiple receptors. Interaction with serotonin receptors contributes…”
Get full text

Identification of novel antagonists of CB1 cannabinoid receptors by Burstein, Ethan S, Ott, Thomas R, Bulow, Anne, Ek, Fredrick, Ma, Jian‐Nong, Pettersson, Hanna, Jensen, Jacob, Ottesen, Lars, Owens, Michelle L, Clemons, Bryan, Bertozzi, Fabio, Johnson, Robert W, Sweetnam, Timothy, Currier, Erika, Del Tredici, Andria L, Schiffer, Hans H, Piu, Fabrice, McFarland, Krista, Tabatabaei, Ali, Gardell, Luis R, Olsson, Roger, Bonhaus, Doug

“…Abstract only CB1 cannabinoid receptor antagonists have therapeutic utility in CNS as well as metabolic disorders. We identified multiple novel structural…”
Get full text

Two mutations in extracellular loop 2 of the human GnRH receptor convert an antagonist to an agonist by Ott, Thomas R, Troskie, Brigitte E, Roeske, Roger W, Illing, Nicola, Flanagan, Colleen A, Millar, Robert P

“…GnRH regulates the reproductive system through cognate G protein-coupled receptors in vertebrates. Certain GnRH analogs that are antagonists at mammalian…”
Get full text

AC-260584, an orally bioavailable M(1) muscarinic receptor allosteric agonist, improves cognitive performance in an animal model by Bradley, Stefania Risso, Lameh, Jelveh, Ohrmund, Linda, Son, Thomas, Bajpai, Abhishek, Nguyen, Derek, Friberg, Mikael, Burstein, Ethan S, Spalding, Tracy A, Ott, Thomas R, Schiffer, Hans H, Tabatabaei, Ali, McFarland, Krista, Davis, Robert E, Bonhaus, Douglas W

“…The recent discovery of allosteric potentiators and agonists of the muscarinic M(1) receptor represents a significant advance in the muscarinic receptor…”
Get full text