EntomoPharm has developed an invertebrate ex vivo system, based on a natural biological brain barrier from the locust grasshopper (Locusta Migratoria or Schistocerca Gregaria), that can be used to screen and rank small-molecule compounds to identify drug leads with improved BBB properties. The model can replace standard in
vitro screen models with an additional opportunity for identification of P-glycoprotein (P-gp) substrates in the early screen cascade. All this whilst meeting the drug discovery demands for reliability, time and cost efficiency.
In the ex vivo Locust BBB model compound permeability is studied at constant brain exposure of 1-10 µM and is independent of degrading enzymes, elimination and plasma protein binding. The model opens possibility for testing dose/time response over an intact
barrier system. Data quality is high and the study outcome is always judged towards the response of an internal positive control.
Key model advantages:
1.The locust blood brain barrier is a natural biological brain barrier that retains its biological integrity and control functions during the test procedure similar to vertebrate in
vivo BBB models.
2. The ex vivo Locust BBB permeability model is the only existing ex vivo model of BBB
permeability that is based on an intact bio-membrane.
3. The Locust brain barrier contains a P-gp efflux mechanism that can be inhibited
by verapamil and the ex vivo BBB locust permeability model is a valuable tool for the
identification of P-gp substrates and inhibitors. The P-gp inhibitor, verapamil, can be included in the test protocol for identification of active P-gp mediated transport.
4. Only a small amount of compound material is needed for the ex vivo BBB permeability model and re-synthesis of compound is rarely necessary.
For more information please click on the link below to open a one-pager about the model:
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