2. Academic Validation
  3. Low brain penetrant CB1 receptor agonists for the treatment of neuropathic pain

Low brain penetrant CB1 receptor agonists for the treatment of neuropathic pain

  • Bioorg Med Chem Lett. 2012 Apr 15;22(8):2932-7. doi: 10.1016/j.bmcl.2012.02.048.
Julia M Adam 1,  John K Clark,  Keneth Davies,  Kathryn Everett,  Ruth Fields,  Stuart Francis,  Fiona Jeremiah,  Takao Kiyoi,  Maurice Maidment,  Angus Morrison,  Paul Ratcliffe,  Alan Prosser,  Jurgen Schulz,  Grant Wishart,  James Baker,  Susan Boyce,  Robert Campbell,  Jean E Cottney,  Maureen Deehan,  Iain Martin
Affiliations

Affiliation

  • 1 Department of Chemistry, Merck Research Laboratories, MSD, Newhouse, Lanarkshire, UK. julia1adam@gmail.com
PMID: 22421020 DOI: 10.1016/j.bmcl.2012.02.048
Abstract

Novel, low brain penetrant, orally bioavailable CB1 receptor agonists were designed starting from a mature lead series of potent brain penetrant CB1 receptor agonists. Increasing the calculated polar surface area was found to be a good strategy for reducing brain penetration whilst retaining drug-like properties. This in silico approach led to the discovery of LBP1, an orally bioavailable, low brain penetrant CB1 receptor agonist with robust activity in rodent models of neuropathic pain and a good preclinical therapeutic profile, which was selected for clinical development.

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