Modulation of CBI cannabinoid receptor by allosteric ligands: Pharmacology and therapeutic opportunities

作者：Khurana Leepakshi; Mackie Ken; Piomelli Daniele; Kendall Debra A^*

来源：Neuropharmacology, 2017, 124: 3-12.

DOI：10.1016/j.neuropharm.2017.05.018

• CB1
• Allosteric modulator
• Biased signaling
• Therapeutic potential

Cannabinoid pharmacology has been intensely studied because of cannabis' pervasive medicinal and non-medicinal uses as well as for the therapeutic potential of cannabinoid-based drugs for the treatment of pain, anxiety, substance abuse, obesity, cancer and neurodegenerative disorders. The identification of allosteric modulators of the cannabinoid receptor 1 (CBI) has given a new direction to the development of cannabinoid-based therapeutics due to the many advantages offered by targeting allosteric site(s). Allosteric receptor modulators hold potential to develop subtype-specific and pathway-specific therapeutics. Here we briefly discuss the first-generation of allosteric modulators of CB1 receptor, their structure-activity relationships, signaling pathways and the allosteric binding site(s) on the CB1 receptor.
This article is part of the Special Issue entitled "A New Dawn in Cannabinoid Neurobiology".

• 出版日期2017-9-15