Thiophenes

Publication Title: 
Journal of thrombosis and haemostasis: JTH

BACKGROUND: Thromboprophylaxis with rivaroxaban (R) is superior to enoxaparin in patients undergoing major orthopedic surgery (MOS). However, rivaroxaban has never been directly compared with fondaparinux (F), which also shows superior efficacy over enoxaparin. The clinical impact of switching from fondaparinux to rivaroxaban thromboprophylaxis is unclear. OBJECTIVES: To evaluate the efficacy and safety of rivaroxaban or fondaparinux thromboprophylaxis in unselected patients undergoing MOS.

Author(s): 
Beyer-Westendorf, J.
L¸tzner, J.
Donath, L.
Radke, O. C.
Kuhlisch, E.
Hartmann, A.
Weiss, N.
Werth, S.
Publication Title: 
Journal of Medicinal Chemistry

Two recently reported hit compounds, COR627 and COR628, underpinned the development of a series of 2-(acylamino)thiophene derivatives. Some of these compounds displayed significant activity in vitro as positive allosteric modulators of the GABAB receptor by potentiating GTP?S stimulation induced by GABA at 2.5 and 25 ?M while failing to exhibit intrinsic agonist activity. Compounds were also found to be effective in vivo, potentiating baclofen-induced sedation/hypnosis in DBA mice when administered either intraperitoneally or intragastrically.

Author(s): 
Mugnaini, Claudia
Pedani, Valentina
Casu, Angelo
Lobina, Carla
Casti, Alberto
Maccioni, Paola
Porcu, Alessandra
Giunta, Daniela
Lamponi, Stefania
Solinas, Maurizio
Dragoni, Stefania
Valoti, Massimo
Colombo, Giancarlo
Castelli, Maria Paola
Gessa, Gian Luigi
Corelli, Federico
Publication Title: 
Brazilian Journal of Medical and Biological Research = Revista Brasileira De Pesquisas Médicas E Biológicas / Sociedade Brasileira De Biofísica ... [et Al.]

The N-acylhydrazone (NAH) analogues N-methyl 2-thienylidene 3,4-benzoylhydrazine (LASSBio-785) and N-benzyl 2-thienylidene 3,4-benzoylhydrazine (LASSBio-786) were prepared from 2-thienylidene 3,4-methylenedioxybenzoylhydrazine (LASSBio-294). The ability of LASSBio-785 and LASSBio-786 to decrease central nervous system activity was investigated in male Swiss mice. LASSBio-785 or LASSBio-786 (30?mg/kg, ip) reduced locomotor activity from 209 ± 26 (control) to 140 ± 18 (P < 0.05) or 146 ± 15 crossings/min (P < 0.05), respectively.

Author(s): 
Silva, G. a. P.
Kummerle, A. E.
Antunes, F.
Fraga, C. a. M.
Barreiro, E. J.
Zapata-Sudo, G.
Sudo, R. T.
Publication Title: 
Expert Review of Clinical Immunology

This article presents a brief review of the physiologic abnormalities seen in fibromyalgia, current theories of widespread pain, and treatment options, including emerging therapeutics, with a focus on the use of duloxetine to manage fibromyalgia symptoms. Major clinical trials that examine the efficacy and effectiveness of duloxetine to date are reviewed, and safety issues are discussed.

Author(s): 
Wright, Cheryl L.
Mist, Scott D.
Ross, Rebecca L.
Jones, Kim D.
Publication Title: 
The Journal of Pharmacology and Experimental Therapeutics

Prostaglandins (PGs) are a family of cellular messengers exerting diverse homeostatic and pathophysiologic effects. Recently, several studies reported significant increases of PGI(2) and PGF(2α) after the inhibition of microsomal PGE synthase-1 (mPGES-1) expression, which indicated that PGH(2) metabolism might be redistributed when the PGE(2) pathway is blocked.

Author(s): 
Yu, Rui
Xiao, Lei
Zhao, Guiqing
Christman, John W.
van Breemen, Richard B.
Publication Title: 
PharmacoEconomics

BACKGROUND: Little is known about the real-world treatment patterns and costs of patients with chronic low back pain (CLBP) who are treated with duloxetine compared with those receiving other non-surgical treatments. OBJECTIVE: Our objective was to compare the real-world treatment patterns and costs between patients with CLBP who initiated duloxetine and matched controls who initiated another non-surgical treatment. METHODS: The study sample was selected from a US privately insured claims database (2004-8).

Author(s): 
Ivanova, Jasmina I.
Birnbaum, Howard G.
Kantor, Evan
Schiller, Matt
Swindle, Ralph W.
Publication Title: 
BMJ (Clinical research ed.)

Diabetes is a worldwide epidemic, and associated neuropathy is its most costly and disabling complication. Given the rising prevalence of painful diabetic neuropathy, it is increasingly important that we understand the best ways to diagnose and treat this condition. Diagnostic tests in this field are evolving rapidly. These include the use of skin biopsies to measure small unmyelinated fibers, as well as even newer techniques that can measure both small unmyelinated fibers and large myelinated fibers in the same biopsy.

Author(s): 
Peltier, Amanda
Goutman, Stephen A.
Callaghan, Brian C.
Publication Title: 
Oncology (Williston Park, N.Y.)

Xerostomia is a permanent and devastating sequela of head and neck irradiation, and its consequences are numerous. Pharmaceutical therapy attempts to preserve or salvage salivary gland function through systemic administration of various protective compounds, most commonly amifostine (Ethyol) or pilocarpine. When these agents are ineffective or the side effects too bothersome, patients often resort to palliative care, for example, with tap water, saline, bicarbonate solutions, mouthwashes, or saliva substitutes.

Author(s): 
Kahn, Shannon T.
Johnstone, Peter A. S.
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