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Recent Publications The following publications are examples of research advances made using compounds available from Tocris Bioscience. January 2008
ICI 182,780 & Tamoxifen
December 2007The antiestrogens ICI 182,780 and Tamoxifen have been shown to have high binding affinities for the membrane estrogen receptor GPR30. Thomas et al (2007) Endocrinol. 146 624. Kisspeptin The GPR54 receptor ligand activates GnRH neurons via both direct and transsynaptic mechanisms. Peilecka-Fortuna et al (2007) Endocrinol. (in press). Acifran The hypolipidaemic agent is an agonist of high and low affinity niacin receptors, GRP109a and GPR109b. Jung et al (2007) Mol.Pharmacol. 50 1445.
Anandamide
November 2007Anandamide has been shown to inhibit the function of α4β2 nicotinic acetylcholine receptors in a CB1 receptor-independent manner. Spivak et al (2007) Mol.Pharmacol. 72 1024. Amiloride The Na+ channel blocker Amiloride inhibits TRPP3-mediated Ca2+-activated currents in two-microelectrode voltage clamp experiments. Dai et al (2007) Mol.Pharmacol. 72 1576. LY 294002 LY 294002 blocks RANTES-induced chemotaxis and reduces levels of Akt phosphorylation via inhibition of PI3Kγ pathway. Ferrandi et al (2007) J.Pharmacol.Exp.Ther. 322 923.
Rottlerin
September 2007Rottlerin has been shown to be neuroprotective in cell cultures and preclinical animal models of Parkinson’s disease. Zhang et al (2007) J.Pharmacol.Exp.Ther. 322 913. Melanotan-II Peripheral melanotan-II treatment leads to weight loss that affects both the visceral and subcutaneous fat compartments. Strader et al (2007) J.Pharmacol.Exp.Ther. 322 1153. Demethylasterriquinone B1 GAPDH has been revealed as a cellular target of the insulin mimic demethylasterriquinone B1. Kim et al (2007) J.Med.Chem.50 3423.
ACPA
August 2007The CB1 agonist ACPA has been shown to modulate neurotransmitter release in the end-plate of the frog neuromuscular junction. Sanchez-Pastor et al (2007) J.Pharmacol.Exp.Ther. 321 439. AM 630 and AM 251 The cannabinoid antagonists AM 630 and AM 251, supplied by Tocris, were used to investigate the role of 2-arachidonoyl glycerol in central antinociception. Guindon et al (2007) Br.J.Pharmacol. 150 693. (-)-Blebbistatin (-)-Blebbistatin potently inhibits arterial smooth muscle tonic contractions by inhibition of smooth muscle myosin II. Eddinger et al (2007) J.Pharmacol.Exp.Ther.320 865.
MRS 1706
July 2007MRS 1706, supplied by Tocris, has been shown to display inverse agonist properties at adenosine A2B receptors. Li et al (2007) J.Pharmacol.Exp.Ther. 320 637. 2-APB The IP3 receptor modulator has been shown to block specific gap channel subtypes (Cx26, Cx30, Cx36, Cx40 and Cx45). Bai et al (2006) J.Pharmacol.Exp.Ther. 319 1452. HU 210 HU 210, supplied by Tocris, induces spatial memory deficits and suppresses hippocampal firing rates in rats. Robinson et al (2007) Br.J.Pharmacol. 151 688.
GS 39783
June 2007The GABAB positive allosteric modulator has been investigated for its role in the rewarding properties of nicotine. Mombereau et al (2007) J.Pharmacol.Exp.Ther. 321 172. Zonisamide The mechanism of action of this antiepileptic drug has been further elucidated, revealing its effects in hippocampal neurons via large-conductance Ca2+-activated K+ (BKCa) channels. Huang et al (2007) J.Pharmacol.Exp.Ther. 321 98. L-655,708 This GABAA α5-subunit containing receptor ligand has been shown to display inverse agonist properties and has been investigated for its role in learning and memory. Atack et al (2006) Neuropharmacology 511023. CGP 7930 The GABAB positive allosteric modulator, supplied by Tocris, has been administered in vivo to explore ethanol self-administration in rats. Liang et al (2006) Neuropharmacology 50 632.
CCT 018159
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Biological characterisation of the novel Hsp90 inhibitor and clarification of its antitumour activity. Sharp et al (2007) Cancer Res. 67 2206. JTE 013 The S1P2-selective antagonist, supplied by Tocris, has been administered in vivo to explore auditory functioning in mice. Kono et al (2007) J.Biol.Chem. 282 10690. MRS 2578 The selective P2Y6 receptor antagonist has been used to elucidate the role of UDP in microglial phagocytosis. Koizumi et al (2007) Nature 446 1091. L-152,804 This NPY Y5 receptor antagonist has been investigated for its role in ethanol reinforcement and obesity. Schroeder et al (2005) Alcohol 36 179. Ishihara et al (2006) Proc.Natl.Acad.Sci.USA. 103 7154. Mashiko et al (2007) Mol.Pharmacol. 71 602. |
Tocris Bioscience Launches New Unique & Affordable Screening Library (more). Upcoming ConferencesENDO Annual Meeting |
