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Publikationer i urvalet

14 träffar

Bibliografisk träff 2022-12-23

Optical-Controlled Kinetic Switch: Fine-Tuning of the Residence Time of an Antagonist Binding to the Vasopressin V<sub>2</sub> Receptor in <i>In Vitro</i>, Ex Vivo, and In Vivo Models of ADPKD.

Gu X, Yuan H, Zhao W, Sun N, Yan W, Jiang C, He Y, Liu H, Cheng J, Guo D.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.2c01625

Bibliografisk träff 2012-04-03

Assessment of exposure of metabolites in preclinical species and humans at steady state from the single-dose radiolabeled absorption, distribution, metabolism, and excretion studies: a case study.

Prakash C, Li Z, Orlandi C, Klunk L.

Drug Metab Dispos · journal article · DOI 10.1124/dmd.112.044933

Bibliografisk träff 2007-09-19

Next-generation spirobenzazepines: identification of RWJ-676070 as a balanced vasopressin V1a/V2 receptor antagonist for human clinical studies.

Xiang MA, Rybczynski PJ, Patel M, Chen RH, McComsey DF, Zhang HC, Gunnet JW, Look R, Wang Y, Minor LK, Zhong HM, Villani FJ, Demarest KT, Damiano BP, Maryanoff BE.

Bioorg Med Chem Lett · comparative study; journal article · DOI 10.1016/j.bmcl.2007.09.059

Bibliografisk träff 2007-08-28

Identification and synthesis of major metabolites of Vasopressin V2-receptor agonist WAY-151932, and antagonist, Lixivaptan.

Molinari AJ, Trybulski EJ, Bagli J, Croce S, Considine J, Qi J, Ali K, Demaio W, Lihotz L, Cochran D.

Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2007.08.053

Bibliografisk träff 2005-11-01

(4-Substituted-phenyl)-(5H-10,11-dihydro-pyrrolo [2,1-c][1,4] benzodiazepin-10-yl)-methanone derivatives as vasopressin receptor modulators.

Venkatesan AM, Grosu GT, Failli AA, Chan PS, Coupet J, Saunders T, Mazandarani H, Ru X.

Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2005.08.007

Bibliografisk träff 2004-06-01

Potent nonpeptide vasopressin receptor antagonists based on oxazino- and thiazinobenzodiazepine templates.

Matthews JM, Hoekstra WJ, Dyatkin AB, Hecker LR, Hlasta DJ, Poulter BL, Andrade-Gordon P, de Garavilla L, Demarest KT, Ericson E, Gunnet JW, Hageman W, Look R, Moore JB, Reynolds CH, Maryanoff BE.

Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2004.03.083

Bibliografisk träff 2003-07-01

Structure-activity study of novel tricyclic benzazepine arginine vasopressin antagonists.

Sum FW, Dusza J, Santos ED, Grosu G, Reich M, Du X, Albright JD, Chan P, Coupet J, Ru X, Mazandarani H, Saunders T.

Bioorg Med Chem Lett · journal article · DOI 10.1016/s0960-894x(03)00388-3

Bibliografisk träff 2003-02-01

Synthesis and biological evaluation of novel indoloazepine derivatives as non-peptide vasopressin V2 receptor antagonists.

Matthews JM, Greco MN, Hecker LR, Hoekstra WJ, Andrade-Gordon P, de Garavilla L, Demarest KT, Ericson E, Gunnet JW, Hageman W, Look R, Moore JB, Maryanoff BE.

Bioorg Med Chem Lett · journal article · DOI 10.1016/s0960-894x(02)01059-4

Bibliografisk träff 2002-11-01

Bridged bicyclic vasopressin receptor antagonists with V(2)-selective or dual V(1a)/V(2) activity.

Dyatkin AB, Hoekstra WJ, Hlasta DJ, Andrade-Gordon P, de Garavilla L, Demarest KT, Gunnet JW, Hageman W, Look R, Maryanoff BE.

Bioorg Med Chem Lett · journal article · DOI 10.1016/s0960-894x(02)00649-2

Bibliografisk träff 2000-04-01

The synthesis and vasopressin (AVP) antagonist activity of a novel series of N-aroyl-2,4,5,6-tetrahydropyrazolo[3,4-d]thieno[3,2-b]azepines.

Albright JD, Delos Santos EG, Dusza JP, Chan PS, Coupet J, Ru X, Mazandarani H.

Bioorg Med Chem Lett · journal article · DOI 10.1016/s0960-894x(00)00084-6

Bibliografisk träff 2000-04-01

The design, synthesis and physical chemical properties of novel human vasopressin V2-receptor antagonists optimized for parenteral delivery.

Ashwell MA, Bagli JF, Caggiano TJ, Chan PS, Molinari AJ, Palka C, Park CH, Rogers JF, Sherman M, Trybulski EJ, Williams DK.

Bioorg Med Chem Lett · journal article · DOI 10.1016/s0960-894x(00)00095-0

Bibliografisk träff 1999-07-01

4,10-dihydro-5H-thieno[3,2-c][1]benzazepine derivatives and 9,10-dihydro-4H-thieno[2,3-c][1]benzazepine derivatives as orally active arginine vasopressin receptor antagonists.

Aranapakam V, Albright JD, Grosu GT, Chan PS, Coupet J, Saunders T, Ru X, Mazandarani H.

Bioorg Med Chem Lett · research support, non-u.s. gov't; journal article · DOI 10.1016/s0960-894x(99)00278-4

Bibliografisk träff 1999-07-01

5-fluoro-2-methyl-N-[5-(5H-pyrrolo[2,1-c][1,4]benzodiazepine-10(11H)-yl carbonyl)-2-pyridinyl]benzamide (CL-385004) and analogs as orally active arginine vasopressin receptor antagonists.

Aranapakam V, Albright JD, Grosu GT, Delos Santos EG, Chan PS, Coupet J, Ru X, Saunders T, Mazandarani H.

Bioorg Med Chem Lett · research support, non-u.s. gov't; journal article · DOI 10.1016/s0960-894x(99)00279-6

Bibliografisk träff 1998-07-01

5-Fluoro-2-methyl-N-[4-(5H-pyrrolo[2,1-c]-[1, 4]benzodiazepin-10(11H)-ylcarbonyl)-3-chlorophenyl]benzamide (VPA-985): an orally active arginine vasopressin antagonist with selectivity for V2 receptors.

Albright JD, Reich MF, Delos Santos EG, Dusza JP, Sum FW, Venkatesan AM, Coupet J, Chan PS, Ru X, Mazandarani H, Bailey T.

J Med Chem · clinical trial; randomized controlled trial; journal article · DOI 10.1021/jm980179c