Zobrazeno 1 - 10
of 7 199
pro vyhledávání: ''
Autor:
Richard Hargreaves, Jeffrey M. Schkeryantz, Carlos Lopez, Kevin C. Dines, Julie V. Selkirk, Andrea Bortolato, Iliana Ruiz, Yingzhuo Grace Yan, Nathan Ching, Deepak Dalvie, Shameek Biswas
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 379:386-399
Ozanimod, a sphingosine 1-phosphate (S1P) receptor modulator that binds with high affinity selectively to S1P receptor subtypes 1 (S1P1) and 5 (S1P5), is approved for the treatment of relapsing multiple sclerosis (MS) in multiple countries. Ozanimod
Autor:
Hayley M. Schrock, Thomas E. Prisinzano, Kevin B. Freeman, Kenneth J. Sufka, Bruce E. Blough, C. Austin Zamarripa, Tanya Pareek
Publikováno v:
Psychopharmacology (Berl)
RATIONALE: Triazole 1.1 is a novel kappa-opioid receptor (KOR) agonist reported to produce antinociception without KOR-typical adverse effects. When combined with the mu-opioid receptor (MOR) agonist, oxycodone, triazole 1.1 blocks oxycodone-induced
Publikováno v:
Immunopharmacology and Immunotoxicology. 43:594-598
Angiogenesis and inflammation exhibit a mutually reinforcing relationship in many human diseases. Vascular endothelial growth factor (VEGF) is one of the most important proangiogenic mediators. Conbercept is a novel VEGF inhibitor.Type II collagen-in
Autor:
Robert K Leśniak, Steven Andrew Baker, Curt R. Fischer, Nay L. Saw, Kathleen S. Montine, Thomas J. Montine, Adam M. Wawro, Mehrdad Shamloo, Chandresh R. Gajera
Publikováno v:
Journal of Neurochemistry. 158:1074-1082
Imbalance in the metabolic pathway linking excitatory and inhibitory neurotransmission has been implicated in multiple psychiatric and neurologic disorders. Recently, we described enantiomer-specific effects of 2-methylglutamate, which is not decarbo
Autor:
Michael Derks, Christoph Wandel, Sian Lennon-Chrimes, Axel Paehler, Piotr Szczesny, Heidemarie Kletzl, Lisa Squassante, Andreas Guenther
Publikováno v:
Expert Opinion on Investigational Drugs. 30:893-901
Balovaptan is a potent, selective vasopressin 1a receptor antagonist. The early-phase pharmacokinetics (PK) of balovaptan are reported.Two Phase 1 studies (overallAbsolute balovaptan bioavailability was high (103-116%). Steady-state (Day 14) balovapt
Autor:
Michael L. Mohler, Ramesh Narayanan, Duane D. Miller, Dong Jin Hwang, Yali He, Thirumagal Thiyagarajan, Suriyan Ponnusamy
Publikováno v:
J Med Chem
A series of propanamide derivatives were designed, synthesized, and pharmacologically characterized as selective androgen receptor degraders (SARDs) and pan-antagonists that exert a broad-scope androgen receptor (AR) antagonism. Incorporating differe
Publikováno v:
Brain Research Bulletin. 172:120-128
A modulatory role has been reported for the isoflavone, genistein, on voltage-gated Na+ channels in the trigeminal ganglion in vitro. However, the acute effects of genistein in vivo, particularly on nociceptive transmission in the trigeminal system,
Autor:
Nwakile Calistus Dozie, Ogechukwu Calista Dozie-Nwakile, Onyemelukwe Ngozi Felicia, Uchendu Ikenna Kingsley, Okonkwo Francis Catherine
Publikováno v:
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry. 20:219-227
Background: Pneumonia is an acute or chronic inflammatory disorder of the lungs, affecting the mucosal areas of the lung. It can be caused by bacteria, viruses or fungi. In some cases, it may be caused by physical or chemical irritants. Kolaviron, a
Autor:
Temitope Janet Olatoyan-Layonu, Abraham Ifedayo Abe, Oluwaseyi A. Adeyeba, Oluropo B. Awosan, OA Olowe, Mokaila K Olapade, Oluwaseyi K Wakeel
Publikováno v:
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry. 20:206-218
Objective: This study investigated the anti-nociceptive and anti-inflammatory activities of the aqueous extract of Ficus capensis (AEFC) by bio-guided fractionation. Methods: The anti-nociceptive and anti-inflammatory effects of AEFC (250, 500, 1000
Publikováno v:
Chemical Research in Toxicology. 34:1348-1354
Linezolid, the principal oxazolidinone antibiotic for therapy of Gram-positive infections, is limited by its myelosuppression and monoamine oxidase (MAO) inhibition, with the latter manifested as serotonergic neurotoxicity. The oral oxazolidinone con