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Showing 1 to 12 of 1926 entries
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Preclinical and translational evaluation of coagulation factor IXa as a novel therapeutic target.

Pharmacology research & perspectives

Ankrom W, Wood HB, Xu J, Geissler W, Bateman T, Chatterjee MS, Feng KI, Metzger JM, Strapps WR, Tadin-Strapps M, Seiffert D, Andre P.
PMID: 26977298
Pharmacol Res Perspect. 2016 Jan 15;4(1):e00207. doi: 10.1002/prp2.207. eCollection 2016 Feb.

The benefits of novel oral anticoagulants are hampered by bleeding. Since coagulation factor IX (fIX) lies upstream of fX in the coagulation cascade, and intermediate levels have been associated with reduced incidence of thrombotic events, we evaluated the viability...

Antidepressant activity of fingolimod in mice.

Pharmacology research & perspectives

di Nuzzo L, Orlando R, Tognoli C, Di Pietro P, Bertini G, Miele J, Bucci D, Motolese M, Scaccianoce S, Caruso A, Mauro G, De Lucia C, Battaglia G, Bruno V, Fabene PF, Nicoletti F.
PMID: 26171219
Pharmacol Res Perspect. 2015 Jun;3(3):e00135. doi: 10.1002/prp2.135. Epub 2015 May 24.

Recent findings indicate that fingolimod, the first oral drug approved for the treatment of multiple sclerosis (MS), acts as a direct inhibitor of histone deacetylases (HDACs) and enhances the production of brain-derived neurotrophic factor (BDNF) in the CNS. Both...

The putative P-gp inhibitor telmisartan does not affect the transcellular permeability and cellular uptake of the calcium channel antagonist verapamil in the P-glycoprotein expressing cell line MDCK II MDR1.

Pharmacology research & perspectives

Saaby L, Tfelt-Hansen P, Brodin B.
PMID: 26171231
Pharmacol Res Perspect. 2015 Aug;3(4):e00151. doi: 10.1002/prp2.151. Epub 2015 Jun 11.

Verapamil is used in high doses for the treatment of cluster headache. Verapamil has been described as a P-glycoprotein (P-gp, ABCB1) substrate. We wished to evaluate in vitro whether co administration of a P-gp inhibitor with verapamil could be...

Increased efficacy of VX-809 in different cellular systems results from an early stabilization effect of F508del-CFTR.

Pharmacology research & perspectives

Farinha CM, Sousa M, Canato S, Schmidt A, Uliyakina I, Amaral MD.
PMID: 26171232
Pharmacol Res Perspect. 2015 Aug;3(4):e00152. doi: 10.1002/prp2.152. Epub 2015 Jun 11.

Cystic fibrosis (CF), the most common recessive autosomal disease among Caucasians, is caused by mutations in the gene encoding the CF transmembrane conductance regulator (CFTR) protein. The most common mutation, F508del, leads to CFTR impaired plasma membrane trafficking. Therapies...

Efficacy of tomato concentrates in mouse models of dyslipidemia and cancer.

Pharmacology research & perspectives

Chattopadhyay A, Grijalva V, Hough G, Su F, Mukherjee P, Farias-Eisner R, Anantharamaiah GM, Faull KF, Hwang LH, Navab M, Fogelman AM, Reddy ST.
PMID: 26171234
Pharmacol Res Perspect. 2015 Aug;3(4):e00154. doi: 10.1002/prp2.154. Epub 2015 Jun 24.

We previously reported that adding freeze-dried tomato powder from transgenic plants expressing the apolipoprotein A-I mimetic peptide 6F at 2.2% by weight to a Western diet (WD) ameliorated dyslipidemia and atherosclerosis in mice. The same dose in a human...

Diclofenac, a nonsteroidal anti-inflammatory drug, is an antagonist of human TRPM3 isoforms.

Pharmacology research & perspectives

Suzuki H, Sasaki E, Nakagawa A, Muraki Y, Hatano N, Muraki K.
PMID: 27433342
Pharmacol Res Perspect. 2016 Apr 07;4(3):e00232. doi: 10.1002/prp2.232. eCollection 2016 Jun.

The effects of diclofenac (Dic), an acetic acid derivative-type nonsteroidal anti-inflammatory drug, were examined on the function of transient receptor potential (TRP) melastatin (TRPM) 3 (TRPM3) in human embryonic kidney 293 cell-line (HEK293) cells with recombinant human TRPM3 isoforms...

A phase 1 study comparing the proposed biosimilar BS-503a with bevacizumab in healthy male volunteers.

Pharmacology research & perspectives

Tajima N, Martinez A, Kobayashi F, He L, Dewland P.
PMID: 28357118
Pharmacol Res Perspect. 2017 Feb 20;5(2):e00286. doi: 10.1002/prp2.286. eCollection 2017 Apr.

This is a randomized, double-blind, single-dose, parallel group phase 1 study to assess pharmacokinetic similarity, safety, and tolerability of BS-503a, a proposed bevacizumab biosimilar. A total of 114 male healthy subjects were randomized (1:1) to receive a single 3...

Metabolic effects of a mitochondrial-targeted coenzyme Q analog in high fat fed obese mice.

Pharmacology research & perspectives

Fink BD, Guo DF, Kulkarni CA, Rahmouni K, Kerns RJ, Sivitz WI.
PMID: 28357127
Pharmacol Res Perspect. 2017 Mar 10;5(2):e00301. doi: 10.1002/prp2.301. eCollection 2017 Apr.

We recently reported that mitoquinone (mitoQ, 500 

Evacetrapib: in vitro and clinical disposition, metabolism, excretion, and assessment of drug interaction potential with strong CYP3A and CYP2C8 inhibitors.

Pharmacology research & perspectives

Cannady EA, Wang MD, Friedrich S, Rehmel JL, Yi P, Small DS, Zhang W, Suico JG.
PMID: 26516590
Pharmacol Res Perspect. 2015 Oct;3(5):e00179. doi: 10.1002/prp2.179. Epub 2015 Oct 12.

Evacetrapib is an investigational cholesteryl ester transfer protein inhibitor (CETPi) for reduction of risk of major adverse cardiovascular events in patients with high-risk vascular disease. Understanding evacetrapib disposition, metabolism, and the potential for drug-drug interactions (DDI) may help guide...

Microparticle of drug and nanoparticle: a biosynthetic route.

Pharmacology research & perspectives

Sarkar S, Dasgupta AK.
PMID: 26516592
Pharmacol Res Perspect. 2015 Oct;3(5):e00188. doi: 10.1002/prp2.188. Epub 2015 Oct 02.

Microparticles (MPs) have great potentiality in material science- based applications. Their use in biology is however limited to clinics and has rarely been exploited in the pharmaceutical context. Unlike nanoparticles (NPs), they are amenable to routine detection by flow...

Acute cocaine exposure elicits rises in calcium in arousal-related laterodorsal tegmental neurons.

Pharmacology research & perspectives

Lambert MØ, Ipsen TH, Kohlmeier KA.
PMID: 28596834
Pharmacol Res Perspect. 2016 Dec 23;5(1):e00282. doi: 10.1002/prp2.282. eCollection 2017 Feb.

Cocaine has strong reinforcing properties, which underlie its high addiction potential. Reinforcement of use of addictive drugs is associated with rises in dopamine (DA) in mesoaccumbal circuitry. Excitatory afferent input to mesoaccumbal circuitry sources from the laterodorsal tegmental nucleus...

Structure-specific effects of lipidated oxytocin analogs on intracellular calcium levels, parental behavior, and oxytocin concentrations in the plasma and cerebrospinal fluid in mice.

Pharmacology research & perspectives

Cherepanov SM, Yokoyama S, Mizuno A, Ichinose W, Lopatina O, Shabalova AA, Salmina AB, Yamamoto Y, Okamoto H, Shuto S, Higashida H.
PMID: 28596839
Pharmacol Res Perspect. 2017 Jan 17;5(1):e00290. doi: 10.1002/prp2.290. eCollection 2017 Feb.

Oxytocin (OT) is a neuroendocrine nonapeptide that plays an important role in social memory and behavior. Nasal administration of OT has been shown to improve trust in healthy humans and social interaction in autistic subjects in some clinical trials....

Showing 1 to 12 of 1926 entries