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Items: 1 to 50 of 75

1.

Synthesis and Pharmacological Characterization of 2-(2,6-Dichlorophenyl)-1-((1S,3R)-5-(3-hydroxy-3-methylbutyl)-3-(hydroxymethyl)-1-methyl-3,4-dihydroisoquinolin-2(1H)-yl)ethan-1-one (LY3154207), a Potent, Subtype Selective, and Orally Available Positive Allosteric Modulator of the Human Dopamine D1 Receptor.

Hao J, Beck JP, Schaus JM, Krushinski JH, Chen Q, Beadle CD, Vidal P, Reinhard MR, Dressman BA, Massey SM, Boulet SL, Cohen MP, Watson BM, Tupper D, Gardinier KM, Myers J, Johansson AM, Richardson J, Richards DS, Hembre EJ, Remick DM, Coates DA, Bhardwaj RM, Diseroad BA, Bender D, Stephenson G, Wolfangel CD, Diaz N, Getman BG, Wang XS, Heinz BA, Cramer JW, Zhou X, Maren DL, Falcone JF, Wright RA, Mitchell SN, Carter G, Yang CR, Bruns RF, Svensson KA.

J Med Chem. 2019 Oct 10;62(19):8711-8732. doi: 10.1021/acs.jmedchem.9b01234. Epub 2019 Sep 30.

PMID:
31532644
2.

Positive allosteric modulators of the dopamine D1 receptor: A new mechanism for the treatment of neuropsychiatric disorders.

Svensson KA, Hao J, Bruns RF.

Adv Pharmacol. 2019;86:273-305. doi: 10.1016/bs.apha.2019.06.001. Epub 2019 Jul 13.

PMID:
31378255
3.

Intracellular Binding Site for a Positive Allosteric Modulator of the Dopamine D1 Receptor.

Wang X, Heinz BA, Qian YW, Carter JH, Gadski RA, Beavers LS, Little SP, Yang CR, Beck JP, Hao J, Schaus JM, Svensson KA, Bruns RF.

Mol Pharmacol. 2018 Oct;94(4):1232-1245. doi: 10.1124/mol.118.112649. Epub 2018 Aug 15.

PMID:
30111649
4.

Preclinical profile of a dopamine D1 potentiator suggests therapeutic utility in neurological and psychiatric disorders.

Bruns RF, Mitchell SN, Wafford KA, Harper AJ, Shanks EA, Carter G, O'Neill MJ, Murray TK, Eastwood BJ, Schaus JM, Beck JP, Hao J, Witkin JM, Li X, Chernet E, Katner JS, Wang H, Ryder JW, Masquelin ME, Thompson LK, Love PL, Maren DL, Falcone JF, Menezes MM, Zhang L, Yang CR, Svensson KA.

Neuropharmacology. 2018 Jan;128:351-365. doi: 10.1016/j.neuropharm.2017.10.032. Epub 2017 Oct 26.

5.

An Allosteric Potentiator of the Dopamine D1 Receptor Increases Locomotor Activity in Human D1 Knock-In Mice without Causing Stereotypy or Tachyphylaxis.

Svensson KA, Heinz BA, Schaus JM, Beck JP, Hao J, Krushinski JH, Reinhard MR, Cohen MP, Hellman SL, Getman BG, Wang X, Menezes MM, Maren DL, Falcone JF, Anderson WH, Wright RA, Morin SM, Knopp KL, Adams BL, Rogovoy B, Okun I, Suter TM, Statnick MA, Gehlert DR, Nelson DL, Lucaites VL, Emkey R, DeLapp NW, Wiernicki TR, Cramer JW, Yang CR, Bruns RF.

J Pharmacol Exp Ther. 2017 Jan;360(1):117-128. Epub 2016 Nov 3.

6.

Reference values for the cervical length measurement in the second trimester of pregnancy using the transvaginal ultrasound in a large Brazilian population.

Peixoto AB, da Cunha Caldas TM, Alamy AH, Martins WP, Bruns RF, Araujo Júnior E.

Obstet Gynecol Sci. 2016 Jul;59(4):303-6. doi: 10.5468/ogs.2016.59.4.303. Epub 2016 Jul 13.

7.

Reproducibility of placental maturity grade classification using a dynamic ultrasonography.

Delle Donne RD, Araujo Júnior E, Rolo LC, Bruns RF.

J Matern Fetal Neonatal Med. 2017 Apr;30(8):987-989. doi: 10.1080/14767058.2016.1196661. Epub 2016 Jun 24.

PMID:
27245764
8.

Auditing fetal nasal bone images in the first trimester of pregnancy: results from a peer review program.

Palermo FG, Albuquerque Dde P, Martins WP, Araujo Júnior E, Bruns RF.

J Matern Fetal Neonatal Med. 2016 Sep;29(17):2874-7. doi: 10.3109/14767058.2015.1107899. Epub 2015 Nov 23.

PMID:
26465391
9.

Fetal thymus: visualization rate and volume by integrating 2D- and 3D-ultrasound during 2nd trimester echocardiography.

Tonni G, Rosignoli L, Cariati E, Martins WP, Miyague AH, Bruns RF, Araujo Júnior E.

J Matern Fetal Neonatal Med. 2016;29(14):2223-8. doi: 10.3109/14767058.2015.1081892. Epub 2015 Sep 11.

PMID:
26365654
10.

Applicability of pocket ultrasound during the first trimester of pregnancy.

Bruns RF, Menegatti CM, Martins WP, Araujo Júnior E.

Med Ultrason. 2015 Sep;17(3):284-8. doi: 10.11152/mu.2013.2066.173.rfb.

11.

Reference intervals of fetal cisterna magna volume by two-dimensional method using the multiplanar mode of three-dimensional ultrasonography.

Nardozza LM, Passos AP, Araujo Júnior E, Bruns RF, Moron AF.

Radiol Bras. 2014 Jul-Aug;47(4):201-5. doi: 10.1590/0100-3984.2013.1852.

12.

Reference ranges of fetal cisterna magna length and area measurements by 3-dimensional ultrasonography using the multiplanar mode.

Passos AP, Araujo Júnior E, Bruns RF, Nardozza LM, Moron AF.

J Child Neurol. 2015 Feb;30(2):209-15. doi: 10.1177/0883073814535496. Epub 2014 May 19.

PMID:
24846899
13.

Reference range of fetal cisterna magna volume by three-dimensional ultrasonography using the VOCAL method.

Araujo Júnior E, Passos AP, Bruns RF, Nardozza LM, Moron AF.

J Matern Fetal Neonatal Med. 2014 Jul;27(10):1023-8. doi: 10.3109/14767058.2013.847419. Epub 2013 Oct 22.

PMID:
24063432
14.

Laparoscopic treatment of intrauterine fallopian tube incarceration.

Kondo W, Bruns RF, Nicola MC, Ribeiro R, Trippia CH, Zomer MT.

Case Rep Obstet Gynecol. 2013;2013:205957. doi: 10.1155/2013/205957. Epub 2013 Apr 30.

15.

Diastrophic dysplasia: prenatal diagnosis and review of the literature.

Honório JC, Bruns RF, Gründtner LF, Raskin S, Ferrari LP, Araujo Júnior E, Nardozza LM.

Sao Paulo Med J. 2013;131(2):127-32. Review.

16.

Rules for identifying potentially reactive or promiscuous compounds.

Bruns RF, Watson IA.

J Med Chem. 2012 Nov 26;55(22):9763-72. doi: 10.1021/jm301008n. Epub 2012 Oct 25.

PMID:
23061697
17.

Prenatal diagnosis of Nager syndrome in the third trimester of pregnancy and anatomopathological correlation.

Rios LT, Araujo Júnior E, Nardozza LM, Bruns RF, Moron AF, da Glória Martins M.

J Med Ultrason (2001). 2012 Oct;39(4):287-9. doi: 10.1007/s10396-012-0374-7. Epub 2012 May 25.

PMID:
27279120
18.

[Obstetric ultrasound in Brazil: a plea for standardization].

Bruns RF, Araujo Júnior E, Nardozza LM, Moron AF.

Rev Bras Ginecol Obstet. 2012 May;34(5):191-5. Portuguese. No abstract available.

PMID:
22584852
19.

Measurements and planes assessed during second-trimester scans in Brazil: an online survey.

Bruns RF, Araujo Júnior E, Nardozza LM, Martins WP, Moron AF.

J Matern Fetal Neonatal Med. 2012 Nov;25(11):2242-7. doi: 10.3109/14767058.2012.684173. Epub 2012 May 11.

PMID:
22545630
20.

Azetidinones as vasopressin V1a antagonists.

Guillon CD, Koppel GA, Brownstein MJ, Chaney MO, Ferris CF, Lu SF, Fabio KM, Miller MJ, Heindel ND, Hunden DC, Cooper RD, Kaldor SW, Skelton JJ, Dressman BA, Clay MP, Steinberg MI, Bruns RF, Simon NG.

Bioorg Med Chem. 2007 Mar 1;15(5):2054-80. Epub 2006 Dec 23.

21.

The role of nuchal translucency in the screening for congenital heart defects.

Bruns RF, Moron AF, Murta CG, Gonçalves LF, Zamith MM.

Arq Bras Cardiol. 2006 Sep;87(3):307-14. English, Portuguese.

22.

Structure-activity relationship of a series of diaminoalkyl substituted benzimidazole as neuropeptide Y Y1 receptor antagonists.

Zarrinmayeh H, Zimmerman DM, Cantrell BE, Schober DA, Bruns RF, Gackenheimer SL, Ornstein PL, Hipskind PA, Britton TC, Gehlert DR.

Bioorg Med Chem Lett. 1999 Mar 8;9(5):647-52.

PMID:
10201822
23.

Structure-activity relationships of a series of benzothiophene-derived NPY Y1 antagonists: optimization of the C-2 side chain.

Britton TC, Spinazze PG, Hipskind PA, Zimmerman DM, Zarrinmayeh H, Schober DA, Gehlert DR, Bruns RF.

Bioorg Med Chem Lett. 1999 Feb 8;9(3):475-80.

PMID:
10091705
24.

Structure-activity relationships of a series of 1-substituted-4-methylbenzimidazole neuropeptide Y-1 receptor antagonists.

Zimmerman DM, Cantrell BE, Smith EC, Nixon JA, Bruns RF, Gitter B, Hipskind PA, Ornstein PL, Zarrinmayeh H, Britton TC, Schober DA, Gehlert DR.

Bioorg Med Chem Lett. 1998 Mar 3;8(5):473-6.

PMID:
9871601
25.

Synthesis and evaluation of a series of novel 2-[(4-chlorophenoxy)methyl]benzimidazoles as selective neuropeptide Y Y1 receptor antagonists.

Zarrinmayeh H, Nunes AM, Ornstein PL, Zimmerman DM, Arnold MB, Schober DA, Gackenheimer SL, Bruns RF, Hipskind PA, Britton TC, Cantrell BE, Gehlert DR.

J Med Chem. 1998 Jul 16;41(15):2709-19.

PMID:
9667962
26.

The neuropeptide Y Y1 antagonist, 1229U91, a potent agonist for the human pancreatic polypeptide-preferring (NPY Y4) receptor.

Schober DA, Van Abbema AM, Smiley DL, Bruns RF, Gehlert DR.

Peptides. 1998;19(3):537-42.

PMID:
9533642
27.

Potent and selective 1,2,3-trisubstituted indole NPY Y-1 antagonists.

Hipskind PA, Lobb KL, Nixon JA, Britton TC, Bruns RF, Catlow J, Dieckman-McGinty DK, Gackenheimer SL, Gitter BD, Iyengar S, Schober DA, Simmons RM, Swanson S, Zarrinmayeh H, Zimmerman DM, Gehlert DR.

J Med Chem. 1997 Nov 7;40(23):3712-4. No abstract available.

PMID:
9371234
28.

PD 81,723, an allosteric enhancer of the A1 adenosine receptor, lowers the threshold for ischemic preconditioning in dogs.

Mizumura T, Auchampach JA, Linden J, Bruns RF, Gross GJ.

Circ Res. 1996 Sep;79(3):415-23.

PMID:
8781475
29.

Conformational induction versus conformational selection: evidence from allosteric enhancers.

Bruns RF.

Trends Pharmacol Sci. 1996 May;17(5):189; discussion 190-1. No abstract available.

PMID:
8669125
30.

3-Aryl-1,2-diacetamidopropane derivatives as novel and potent NK-1 receptor antagonists.

Hipskind PA, Howbert JJ, Bruns RF, Cho SS, Crowell TA, Foreman MM, Gehlert DR, Iyengar S, Johnson KW, Krushinski JH, Li DL, Lobb KL, Mason NR, Muehl BS, Nixon JA, Phebus LA, Regoli D, Simmons RM, Threlkeld PG, Waters DC, Gitter BD.

J Med Chem. 1996 Feb 2;39(3):736-48.

PMID:
8576917
31.

Pharmacological characterization of LY303870: a novel, potent and selective nonpeptide substance P (neurokinin-1) receptor antagonist.

Gitter BD, Bruns RF, Howbert JJ, Waters DC, Threlkeld PG, Cox LM, Nixon JA, Lobb KL, Mason NR, Stengel PW, et al.

J Pharmacol Exp Ther. 1995 Nov;275(2):737-44.

PMID:
7473161
32.

Cyclosporin A is a substance P (tachykinin NK1) receptor antagonist.

Gitter BD, Waters DC, Threlkeld PG, Lovelace AM, Matsumoto K, Bruns RF.

Eur J Pharmacol. 1995 May 26;289(3):439-46.

PMID:
7556412
33.

Allosteric enhancer PD 81,723 acts by novel mechanism to potentiate cardiac actions of adenosine.

Kollias-Baker C, Ruble J, Dennis D, Bruns RF, Linden J, Belardinelli L.

Circ Res. 1994 Dec;75(6):961-71.

PMID:
7955150
34.

Selective potentiation by an A1 adenosine receptor enhancer of the negative dromotropic action of adenosine in the guinea pig heart.

Amoah-Apraku B, Xu J, Lu JY, Pelleg A, Bruns RF, Belardinelli L.

J Pharmacol Exp Ther. 1993 Aug;266(2):611-7.

PMID:
8355194
35.

Cardiac functional responses to adenosine by PD 81,723, an allosteric enhancer of the adenosine A1 receptor.

Mudumbi RV, Montamat SC, Bruns RF, Vestal RE.

Am J Physiol. 1993 Mar;264(3 Pt 2):H1017-22.

PMID:
8456969
36.

Beta-proline analogues as agonists at the strychnine-sensitive glycine receptor.

Johnson G, Drummond JT, Boxer PA, Bruns RF.

J Med Chem. 1992 Jan 24;35(2):233-41.

PMID:
1310117
37.

Functional activity of the adenosine binding enhancer, PD 81,723, in the in vitro hippocampal slice.

Janusz CA, Bruns RF, Berman RF.

Brain Res. 1991 Dec 20;567(2):181-7.

PMID:
1817724
38.

Species differences in affinities of non-peptide antagonists for substance P receptors.

Gitter BD, Waters DC, Bruns RF, Mason NR, Nixon JA, Howbert JJ.

Eur J Pharmacol. 1991 May 17;197(2-3):237-8. No abstract available.

PMID:
1717291
39.

Inhibition of protein kinase C by calphostin C is light-dependent.

Bruns RF, Miller FD, Merriman RL, Howbert JJ, Heath WF, Kobayashi E, Takahashi I, Tamaoki T, Nakano H.

Biochem Biophys Res Commun. 1991 Apr 15;176(1):288-93.

PMID:
1708246
40.

N6-substituted adenosine receptor agonists: potential antihypertensive agents.

Trivedi BK, Blankley CJ, Bristol JA, Hamilton HW, Patt WC, Kramer WJ, Johnson SA, Bruns RF, Cohen DM, Ryan MJ.

J Med Chem. 1991 Mar;34(3):1043-9.

PMID:
2002448
41.

Structure-activity relationships for enhancement of adenosine A1 receptor binding by 2-amino-3-benzoylthiophenes.

Bruns RF, Fergus JH, Coughenour LL, Courtland GG, Pugsley TA, Dodd JH, Tinney FJ.

Mol Pharmacol. 1990 Dec;38(6):950-8.

PMID:
2250667
42.
43.

Subclasses of angiotensin II binding sites and their functional significance.

Dudley DT, Panek RL, Major TC, Lu GH, Bruns RF, Klinkefus BA, Hodges JC, Weishaar RE.

Mol Pharmacol. 1990 Sep;38(3):370-7.

PMID:
2402226
44.

Adenosine receptors. Roles and pharmacology.

Bruns RF.

Ann N Y Acad Sci. 1990;603:211-25; discussion 225-6. Review. No abstract available.

PMID:
2291523
45.

Linear and proximal benzo-separated alkylated xanthines as adenosine-receptor antagonists.

Schneller SW, Ibay AC, Christ WJ, Bruns RF.

J Med Chem. 1989 Oct;32(10):2247-54.

PMID:
2795597
46.

Solubilities of adenosine antagonists determined by radioreceptor assay.

Bruns RF, Fergus JH.

J Pharm Pharmacol. 1989 Sep;41(9):590-4.

PMID:
2573701
47.

Evaluation and synthesis of aminohydroxyisoxazoles and pyrazoles as potential glycine agonists.

Drummond J, Johnson G, Nickell DG, Ortwine DF, Bruns RF, Welbaum B.

J Med Chem. 1989 Sep;32(9):2116-28.

PMID:
2549245
48.

C2,N6-disubstituted adenosines: synthesis and structure-activity relationships.

Trivedi BK, Bruns RF.

J Med Chem. 1989 Aug;32(8):1667-73.

PMID:
2754691
49.

Characteristics of an adenosine A1 binding site in human placental membranes.

Work C, Hutchison K, Prasad M, Bruns RF, Fox IH.

Arch Biochem Biophys. 1989 Jan;268(1):191-202.

50.

N6-bicycloalkyladenosines with unusually high potency and selectivity for the adenosine A1 receptor.

Trivedi BK, Bridges AJ, Patt WC, Priebe SR, Bruns RF.

J Med Chem. 1989 Jan;32(1):8-11. No abstract available.

PMID:
2909748

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