This is a rodent model, used to evaluate the potential for a compound to cross the blood-brain barrier (BBB) and enter the central nervous system. In an anesthetized rat or mouse, we replace the systemic circulation by buffer, infused into the brain via a carotid cannula connected to an external pump. After a brief (30-second) perfusion, the brain is removed rapidly for quantification (by LC-MS/MS) of the amount of test article in the tissue.
Use of this Model:
Compare distribution into the brain can be compared for a series of test articles to rank-order the compounds for brain permeation potential.
Get some perspective on your compound by placing it into the context of our internal database of brain perfusion data for a structurally diverse set of compounds.
Assess the involvement of drug efflux transporters such as P-glycoprotein (P-gp) pose a formidable biochemical component of the BBB, helping to exclude compounds from the brain, through the use of chemical inhibitors or knockout models.
Verify brain penetration predicted by a combination of in vitro permeability (MDR1-MDCK cell monolayers), plasma protein binding, and brain tissue binding.
Roughly predict brain penetration in humans for your compound, based on reasonably good correlation between in situ rodent brain perfusion data and human clinical data.