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Review
. 2019 Mar 18;10(5):647-659.
doi: 10.1039/c8md00595h. eCollection 2019 May 1.

Selective modulation of the cannabinoid type 1 (CB1) receptor as an emerging platform for the treatment of neuropathic pain

Samuel D Banister  1 , Kaavya Krishna Kumar  2 , Vineet Kumar  1 , Brian K Kobilka  2 , Sanjay V Malhotra  1
Affiliations
Review

Selective modulation of the cannabinoid type 1 (CB1) receptor as an emerging platform for the treatment of neuropathic pain

Samuel D Banister et al. Medchemcomm. .

Abstract

Neuropathic pain is caused by a lesion or dysfunction in the nervous system, and it may arise from illness, be drug-induced or caused by toxin exposure. Since the discovery of two G-protein-coupled cannabinoid receptors (CB1 and CB2) nearly three decades ago, there has been a rapid expansion in our understanding of cannabinoid pharmacology. This is currently one of the most active fields of neuropharmacology, and interest has emerged in developing cannabinoids and other small molecule modulators of CB1 and CB2 as therapeutics for neuropathic pain. This short review article provides an overview of the chemotypes currently under investigation for the development of novel neuropathic pain treatments targeting CB1 receptors.

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Figures

Fig. 1
Fig. 1. Selected endogenous cannabinoids.
Fig. 2
Fig. 2. Selected phytocannabinoids and analogs.
Fig. 3
Fig. 3. Structures and activities of selected ligands reported during the discovery of CRA13.
Fig. 4
Fig. 4. Peripherally-restricted CB1 agonists under development by AstraZeneca.
Fig. 5
Fig. 5. Effect of the terminal carboline amine substituent on CB1 agonist activity and PSA.
Fig. 6
Fig. 6. Effect of the central carboline amine substituent on CB1 agonist activity and PSA.
Fig. 7
Fig. 7. Peripherally-restricted indole-3-heterocycle CB1 agonists.
Fig. 8
Fig. 8. Peripherally restricted CB1 agonists with efficacy in rodent models of neuropathic pain.
Fig. 9
Fig. 9. Selected endogenous and exogenous allosteric modulators of CB1.
Fig. 10
Fig. 10. Selected PAM modulator of CB1.
Fig. 11
Fig. 11. CB1 ligands for the treatment of Huntington disease.
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