Chemistry:LBP-1 (drug)
From HandWiki
Short description: Chemical compound
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| Formula | C23H29ClN6O3 |
| Molar mass | 472.97 g·mol−1 |
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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 cannabinoid receptor agonist, 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]
See also
References
- ↑ "Design, synthesis, and structure-activity relationships of indole-3-heterocycles as agonists of the CB1 receptor". Bioorganic & Medicinal Chemistry Letters 21 (1): 506–9. January 2011. doi:10.1016/j.bmcl.2010.10.093. PMID 21075630.
- ↑ "Discovery of potent and orally bioavailable heterocycle-based cannabinoid CB1 receptor agonists". Bioorganic & Medicinal Chemistry Letters 21 (6): 1748–53. March 2011. doi:10.1016/j.bmcl.2011.01.082. PMID 21316962.
- ↑ "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. April 2011. doi:10.1016/j.bmcl.2011.02.023. PMID 21411321.
- ↑ "Low brain penetrant CB1 receptor agonists for the treatment of neuropathic pain". Bioorganic & Medicinal Chemistry Letters 22 (8): 2932–7. April 2012. doi:10.1016/j.bmcl.2012.02.048. PMID 22421020.
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