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Medicinal uses, phytochemistry and pharmacology of the genus Uncaria
Conclusion Preliminary investigations on pharmacological properties of the Uncaria species have enlightened their efficacious remedy for hypertension, asthma, cancer, diabetes, rheumatism and neurodegenerative diseases. To ensure the safety and effectiveness in clinical application, research on bioactive compounds, pharmacological mechanisms and toxicity of the genus Uncaria as well as the stereo-chemistry and structure-activity relationships of indole alkaloids seem very important. Graphical abstract
Source: Journal of Ethnopharmacology - July 26, 2015 Category: Drugs & Pharmacology Source Type: research

Involvement of NMDA receptor subtypes in cortical spreading depression in rats assessed by fMRI.
Abstract Cortical spreading depression (CSD) is a phenomenon implicated in migraine with aura and associated with other neurological disorders (e.g. stroke, brain trauma). Current evidence points to the essential role of NMDA receptors in CSD mechanisms. However, the roles of multiple subunits of NMDA receptors expressed in neurons, glia and blood vessels in vivo, are little explored. Using BOLD fMRI of urethane anesthetized rats as an integrative CSD readout, we tested the involvement of different NMDA receptor subtypes in CSD induction and propagation. Rats were treated with a non-selective NMDA blocker (MK-801...
Source: Neuropharmacology - February 14, 2015 Category: Drugs & Pharmacology Authors: Shatillo A, Salo RA, Giniatullin R, Gröhn OH Tags: Neuropharmacology Source Type: research

Potential mechanisms of prospective antimigraine drugs: A focus on vascular (side) effects
Publication date: March 2011 Source:Pharmacology & Therapeutics, Volume 129, Issue 3 Author(s): Kayi Y. Chan , Steve Vermeersch , Jan de Hoon , Carlos M. Villalón , Antoinette MaassenVanDenBrink Currently available drugs for the acute treatment of migraine, i.e. ergot alkaloids and triptans, are cranial vasoconstrictors. Although cranial vasoconstriction is likely to mediate—at least a part of—their therapeutic effects, this property also causes vascular side-effects. Indeed, the ergot alkaloids and the triptans have been reported to induce myocardial ischemia and stroke, albeit in extremely rare cases, and ...
Source: Pharmacology and Therapeutics - November 6, 2014 Category: Drugs & Pharmacology Source Type: research

Neurochemicals involved in medullary control of common carotid blood flow.
Abstract The common carotid artery (CCA) supplies intra- and extra-cranial vascular beds. An area in the medulla controlling CCA blood flow is defined as the dorsal facial area (DFA) by Kuo et al. in 1987. In the DFA, presynaptic nitrergic and/or glutamatergic fibers innervate preganglionic nitrergic and/or cholinergic neurons which give rise to the preganglionic fibers of the parasympathetic 7th and 9th cranial nerves. Released glutamate from presynaptic nitrergic and/or glutamatergic fibers can activate N-methyl-D-aspartate (NMDA) and α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) receptors on preg...
Source: Current Neuropharmacology - September 1, 2013 Category: Drugs & Pharmacology Authors: Gong CL, Leung YM, Wang MR, Lin NN, Lee TJ, Kuo JS Tags: Curr Neuropharmacol Source Type: research

Safety, pharmacokinetics and pharmacodynamics of multiple oral doses of apixaban, a factor Xa inhibitor, in healthy subjects
This study examined the safety, pharmacokinetics and pharmacodynamics of multiple‐dose apixaban. MethodsThis double‐blind, randomized, placebo‐controlled, parallel‐group, multiple‐dose escalation study was conducted in six sequential dose panels – apixaban 2.5, 5, 10 and 25 mg twice daily (BID) and 10 and 25 mg once daily (QD) – with 8 healthy subjects per panel. Within each panel, subjects were randomized (3:1) to oral apixaban or placebo for 7 days. Subjects underwent safety assessments and were monitored for adverse events (AEs). Blood samples were taken to measure apixaban plasma concentration, internatio...
Source: British Journal of Clinical Pharmacology - March 4, 2013 Category: Drugs & Pharmacology Authors: Charles Frost, Sunil Nepal, Jessie Wang, Alan Schuster, Wonkyung Byon, Rebecca A. Boyd, Zhigang Yu, Andrew Shenker, Yu Chen Barrett, Rogelio Mosqueda‐Garcia, Frank LaCreta Tags: PK‐PD Relationships Source Type: research

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