6 results match your criteria trpv1 favourable

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Capsaicin may have important potential for promoting vascular and metabolic health.

Open Heart 2015;2(1):e000262. Epub 2015 Jun 17.

Mid America Heart Institute, St. Luke's Hospital , Kansas City, Missouri , USA.

Capsaicin, the phytochemical responsible for the spiciness of peppers, has the potential to modulate metabolism via activation of transient receptor potential vanilloid 1 (TRPV1) receptors, which are found not only on nociceptive sensory neurons, but also in a range of other tissues. TRPV1 activation induces calcium influx, and in certain tissues this is associated with increased activation or expression of key proteins such as endothelial nitric oxide synthase (eNOS), uncoupling protein 2 (UCP2), KLF2, PPARdelta, PPARgamma, and LXRα. The calcium influx triggered by TRPV1 activation in endothelial cells mimics the impact of shear stress in this regard, activating and increasing the expression of eNOS-but also increasing expression of cox-2, thrombomodulin, and nrf2-responsive antioxidant enzymes, while decreasing expression of proinflammatory proteins. Read More

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Cardiovascular effects of current and future anti-obesity drugs.

Curr Vasc Pharmacol 2014 May;12(3):493-504

Department of Biomedicine- Pharmacology, Aarhus University, Wilhelm Meyers Alle 4, 8000 Aarhus C, Denmark.

The prevalence of obesity increases and is associated with increases in co-morbidities e.g. type 2 diabetes, hyperlipidemia, hypertension, obstructive sleep apnea, heart disease, stroke, asthma, several forms of cancer, depression, and may result in reduction of expected remaining lifespan. Read More

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Antinociceptive curcuminoid, KMS4034, effects on inflammatory and neuropathic pain likely via modulating TRPV1 in mice.

Br J Anaesth 2013 Oct 29;111(4):667-72. Epub 2013 May 29.

Department of Dental Anesthesiology and Dental Research Institute, School of Dentistry, Seoul National University, Seoul, Republic of Korea.

Background: Curcumin, the active ingredient of turmeric (Curcuma longa), has a wide range of beneficial effects including anti-inflammation and analgesia. However, poor bioavailability of curcumin hinders its clinical application. To overcome this limitation, we modified the structure of curcumin and synthesized new derivatives with favourable pharmacokinetic profiles. Read More

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October 2013

Synthesis and biological evaluation of [¹¹C]SB366791: a new PET-radioligand for in vivo imaging of the TRPV1 receptor.

Nucl Med Biol 2013 Jan 7;40(1):141-7. Epub 2012 Nov 7.

Laboratory for Radiopharmacy, KU Leuven, Leuven, Belgium.

Introduction: The transient receptor potential vanilloid subfamily member 1 (TRPV1) receptor, a non-selective cation channel, is known for its key role in pain nociception and neurogenic inflammation. TRPV1 expression has been demonstrated in diverse tissues and an essential role for TRPV1 in various disorders has been suggested. A TRPV1-specific PET-radioligand can serve as a useful tool for further in vivo research in animals and directly in humans. Read More

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January 2013

N-Tetrahydroquinolinyl, N-quinolinyl and N-isoquinolinyl biaryl carboxamides as antagonists of TRPV1.

Bioorg Med Chem Lett 2006 Sep 27;16(17):4533-6. Epub 2006 Jun 27.

Neurology and GI Center of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Harlow, Essex, UK.

Starting from the high throughput screening hit (3), novel N-tetrahydroquinolinyl, N-quinolinyl and N-isoquinolinyl carboxamides have been identified as potent antagonists of the ion channel TRPV1. The N-quinolinylnicotinamide (46) showed excellent potency at human, guinea pig and rat TRPV1, a favourable in vitro DMPK profile and activity in an in vivo model of inflammatory pain. Read More

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September 2006

Efferent-like roles of afferent neurons in the gut: Blood flow regulation and tissue protection.

Peter Holzer

Auton Neurosci 2006 Apr 20;125(1-2):70-5. Epub 2006 Mar 20.

Department of Experimental and Clinical Pharmacology, Medical University of Graz, Universitätsplatz 4, A-8010 Graz, Austria.

The maintenance of gastrointestinal mucosal integrity depends on the rapid alarm of protective mechanisms in the face of pending injury. To this end, the gastric mucosa is innervated by intrinsic sensory neurons and two populations of extrinsic sensory neurons: vagal and spinal afferents. Extrinsic afferent neurons constitute an emergency system that is called into operation when the gastrointestinal mucosa is endangered by noxious chemicals. Read More

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