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The First Novel Fluorescent Cannabinoid Ligand, Tocrifluor T1117, Available Exclusively From Tocris Bioscience


2/25/2009 2:02:45 PM

Tocris Bioscience (www.tocris.com) is pleased to announce the launch of Tocrifluor T1117. Co developed by Tocris and the University of Glasgow, Tocrifluor T1117 is the CB1 antagonist AM 251 labelled with a rhodamine derivative, and is the first fluorescent cannabinoid ligand commercially available.

New research published by Daly et al (2008) has now shown that Tocrifluor T1117 is a novel and potentially very powerful tool for identifying the cellular location of cannabinoid receptors, including GPR551.

Dr. Craig Daly, Research Fellow at the University of Glasgow, said, "The role of cannabinoids in the cardiovascular system is both complicated and fascinating. We have found that T1117 has fluorescent properties ideally suited for analysing its binding in unfixed, thick biological specimens (i.e. blood vessels). T1117 is very stable under confocal laser excitation, has a good fluorescent yield, does not appear to be toxic and binds to similar (but not identical) sites as those recognised by other vasoactive fluorescent ligands for adrenergic receptors. T1117 should be a very useful tool for fluorescence based receptor studies."

The CB1 receptor, also known as the central cannabinoid receptor, is a member of the cannabinoid receptor group of G-protein-coupled receptors that also includes CB2. CB1 receptors are found mainly in the terminals of central and peripheral neurons where they usually mediate inhibition of neurotransmitter release. They can also be present on some non-neuronal cells, including immune cells.

GPR55 was identified and cloned for the first time in 1999. Later it was identified as a putative cannabinoid receptor because of a similar amino acid sequence in the binding region. Consistent with this, GPR55 is activated by endogenous, plant and synthetic cannabinoids and this profile as a distinct non-CB1/CB2 receptor has led to suggestions that GPR55 be categorised as the CB3 receptor.

Duncan Crawford, Tocris’ Chief Scientific Officer, said, “Novel products have always been an essential component of Tocris’ range. We anticipate that the ability of Tocrifluor T1117 to pinpoint these receptors will be of great benefit to life scientists.”

1Daly et al (2008) Vascular and Smooth Muscle Phys.Soc. Symposium 2008.

Full product information on Tocrifluor T1117 can be viewed at: Tocrifluor T1117.

Additional T1117 images can be viewed at: http://www.cardiovascular.org/T1117.htm.

About Tocris Bioscience

Tocris Bioscience (www.tocris.com) is a leading supplier of high performance chemicals, peptides and antibodies, with customers in all of the world’s major pharmaceutical companies, universities and research institutes. The Company is committed to making new life science discoveries possible by providing the highest performing and most innovative range of research reagents.

Tocris Bioscience products are used by scientists carrying out non-clinical research in fields such as cancer, stroke, Alzheimer's disease and obesity. The Company's catalogue of over 3000 reagents represents a unique collection of novel, exclusive and licensed research tools. A major source of key signal transduction reagents and arguably the world leader in the supply of neuroscience reagents, the Company won the Queen's Award for Enterprise (International Business) in 2002.

Tocris Bioscience is the trading name for the companies in the Tocris Cookson Group. Tocris Cookson Ltd is privately held and headquartered in Bristol, UK. Its US subsidiary, Tocris Cookson Inc, is located in St. Louis, Missouri, USA. There are approximately 50 employees in the Group worldwide, operating out of two sites in the UK and one in the US.

For more information about Tocris Bioscience visit www.tocris.com.


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