LBP-1 is a drug originally developed by Organon for the treatment of neuropathic pain,[1][2][3] It acts as a potent and selective cannabinoidreceptoragonist, with high potency at both the CB1 and CB2 receptors, but low penetration of the blood–brain barrier. This makes LBP-1 peripherally selective, and while it was effective in animal models of neuropathic pain and allodynia, it did not produce cannabinoid-appropriate responding suggestive of central effects, at any dose tested.[4]
^Morrison AJ, Adam JM, Baker JA, Campbell RA, Clark JK, Cottney JE, et al. (January 2011). "Design, synthesis, and structure-activity relationships of indole-3-heterocycles as agonists of the CB1 receptor". Bioorganic & Medicinal Chemistry Letters. 21 (1): 506–9. doi:10.1016/j.bmcl.2010.10.093. PMID21075630.
^Kiyoi T, Adam JM, Clark JK, Davies K, Easson AM, Edwards D, et al. (March 2011). "Discovery of potent and orally bioavailable heterocycle-based cannabinoid CB1 receptor agonists". Bioorganic & Medicinal Chemistry Letters. 21 (6): 1748–53. doi:10.1016/j.bmcl.2011.01.082. PMID21316962.
^Ratcliffe P, Adam JM, Baker J, Bursi R, Campbell R, Clark JK, et al. (April 2011). "Design, synthesis and structure-activity relationships of (indo-3-yl) heterocyclic derivatives as agonists of the CB1 receptor. Discovery of a clinical candidate". Bioorganic & Medicinal Chemistry Letters. 21 (8): 2541–6. doi:10.1016/j.bmcl.2011.02.023. PMID21411321.
^Adam JM, Clark JK, Davies K, Everett K, Fields R, Francis S, et al. (April 2012). "Low brain penetrant CB1 receptor agonists for the treatment of neuropathic pain". Bioorganic & Medicinal Chemistry Letters. 22 (8): 2932–7. doi:10.1016/j.bmcl.2012.02.048. PMID22421020.
