Tocris Bioscience Extends Novel Range of Fast, Light-Sensitive Caged Compounds Developed by Columbia University

Newswise — Tocris Bioscience and Columbia University today announced that they have expanded their license agreement to include RuBi-Glutamate and RuBi-4AP, two additional novel caged compounds with significant applications for basic science research.

Caged compounds are biologically-relevant molecules rendered inactive by a photolabile bond to a chemical group (the “cage”). Typically, the active molecule can be “uncaged” by breaking this bond with light, resulting in activation of the compound. Photorelease of caged bioactive molecules is a powerful tool for studying molecular mechanisms, as pre-determined amounts of such molecules can be delivered at precise, controllable time points.

RuBi-Glutamate, a ruthenium-bipyridine-trimethylphosphine caged glutamate, is excited by visible wavelengths and releases glutamate, the brain’s main neurotransmitter, after one- or two-photon excitation. It possesses a high quantum efficiency and can be used at low concentrations, partly avoiding blockade of GABAergic transmission seen with other caged glutamate compounds. RuBi-Glutamate also displays high spatial resolution and generates excitatory responses in individual dendritic spines with physiological kinetics. RuBi-Glutamate is one of the fastest caged glutamate compounds yet developed, releasing glutamate in tens of nanoseconds.

RuBi-4AP, a water soluble ruthenium-bipyridine-triphenylphosphine caged 4-aminopyridine (4-AP), is also excited by visible wavelengths and has two-photon uncaging capabilities under physiological conditions. RuBi-4AP releases 4-AP, a voltage-dependent potassium channel blocker. These channels control synaptic release and are crucial for the normal functioning of the nervous system.

“Compared to currently available ultraviolet (UV) light-sensitive caged compounds, RuBi-Glutamate and RuBi-4AP, along with the previously licensed RuBi-GABA, can all be uncaged using longer wavelengths of light, e.g. blue or even green light, resulting in less scattering and allowing the light source to penetrate deeper into living tissue. This could be key for their future use in vivo,” says Rafael Yuste, M.D., Ph.D., a professor in the Department of Biological Sciences at Columbia University and an investigator of the Howard Hughes Medical Institute and a co-inventor of the technology, along with colleague Roberto Etchenique, Ph.D., a professor in the Department of Inorganic Chemistry at the University of Buenos Aires.

Duncan Crawford, Tocris’ Chief Scientific Officer, says, “We know that there is a great deal of interest in caging technology from the global research community. By making these novel products available to scientists, we hope to facilitate new and exciting discoveries in the basic mechanisms underlying fundamental biological processes.”

“Understanding these processes may also expand investigation of these compounds for clinical applications,” suggests Beth Kauderer, the licensing officer at Columbia Technology Ventures who negotiated the agreement. “4AP is now approved for treating certain neurodegenerative syndromes; it is possible that caged 4AP compounds may be employed for more selective, safer therapies.”

About Columbia Technology VenturesA leading academic and research university, Columbia University continually seeks to advance the frontiers of knowledge and to foster a campus community deeply engaged in understanding and addressing the complex global issues of our time. Columbia University's technology transfer office, Columbia Technology Ventures, manages Columbia’s intellectual property portfolio and serves as the university’s gateway for companies and entrepreneurs seeking novel technology solutions. Columbia Technology Venture’s core mission is to facilitate the transfer of inventions from academic research to outside organizations for the benefit of society on a local, national and global basis. For more information on Columbia Technology Ventures, please visit

About Tocris BioscienceTocris Bioscience ( 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 3,000 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.