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Latest advances in cannabinoid receptor agonists.
Expert Opin Ther Pat 2009; 19(12):1647-73EO

Abstract

BACKGROUND

Since the discovery of cannabinoid receptors and their endogenous ligands in early 1990s, the endocannabinoid system has been shown to play a vital role in several pathophysiological processes. It has been targeted for the treatment of several diseases including neurodegenerative diseases (Parkinson's disease, Alzheimer's disease, Huntington's disease and MS), cancer, obesity, inflammatory bowel disease, neuropathic and inflammatory pain. The last decade has witnessed remarkable advances in the development of cannabinergic ligands displaying high selectivity and potency towards two subtypes of cannabinoid receptors, namely CB1 and CB2.

OBJECTIVE

In this review, we highlight the latest advances made in the development of cannabinoid agonists and summarize recently disclosed, novel chemical scaffolds as CB-selective agonists in patents that appeared during January 2008 - June 2009.

METHODS

Data presented here are obtained through the search of PubMed for research articles and reviews, and the website of European patents (http://ep.espacenet.com), SciFinder Scholar and US patents (www.uspto.gov).

CONCLUSIONS

Our analysis reveals prolific patenting activity mainly in the CB2 selective agonist area. Limiting the BBB penetrability, thereby, leading to peripherally restricted CB1/CB2 agonists and enhancing CB2-selectivity emerge as likely prerequisites for avoidance of adverse central CB1 mediated side effects.

Authors+Show Affiliations

Northeastern University, Center for Drug Discovery, 116 Mugar Hall, Boston, MA 02115, USA. g.thakur@neu.edu

Pub Type(s)

Journal Article
Review

Language

eng

PubMed ID

19939187

Citation

Thakur, Ganesh A., et al. "Latest Advances in Cannabinoid Receptor Agonists." Expert Opinion On Therapeutic Patents, vol. 19, no. 12, 2009, pp. 1647-73.
Thakur GA, Tichkule R, Bajaj S, et al. Latest advances in cannabinoid receptor agonists. Expert Opin Ther Pat. 2009;19(12):1647-73.
Thakur, G. A., Tichkule, R., Bajaj, S., & Makriyannis, A. (2009). Latest advances in cannabinoid receptor agonists. Expert Opinion On Therapeutic Patents, 19(12), pp. 1647-73. doi:10.1517/13543770903436505.
Thakur GA, et al. Latest Advances in Cannabinoid Receptor Agonists. Expert Opin Ther Pat. 2009;19(12):1647-73. PubMed PMID: 19939187.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Latest advances in cannabinoid receptor agonists. AU - Thakur,Ganesh A, AU - Tichkule,Ritesh, AU - Bajaj,Shama, AU - Makriyannis,Alexandros, PY - 2009/11/27/entrez PY - 2009/11/27/pubmed PY - 2010/2/3/medline SP - 1647 EP - 73 JF - Expert opinion on therapeutic patents JO - Expert Opin Ther Pat VL - 19 IS - 12 N2 - BACKGROUND: Since the discovery of cannabinoid receptors and their endogenous ligands in early 1990s, the endocannabinoid system has been shown to play a vital role in several pathophysiological processes. It has been targeted for the treatment of several diseases including neurodegenerative diseases (Parkinson's disease, Alzheimer's disease, Huntington's disease and MS), cancer, obesity, inflammatory bowel disease, neuropathic and inflammatory pain. The last decade has witnessed remarkable advances in the development of cannabinergic ligands displaying high selectivity and potency towards two subtypes of cannabinoid receptors, namely CB1 and CB2. OBJECTIVE: In this review, we highlight the latest advances made in the development of cannabinoid agonists and summarize recently disclosed, novel chemical scaffolds as CB-selective agonists in patents that appeared during January 2008 - June 2009. METHODS: Data presented here are obtained through the search of PubMed for research articles and reviews, and the website of European patents (http://ep.espacenet.com), SciFinder Scholar and US patents (www.uspto.gov). CONCLUSIONS: Our analysis reveals prolific patenting activity mainly in the CB2 selective agonist area. Limiting the BBB penetrability, thereby, leading to peripherally restricted CB1/CB2 agonists and enhancing CB2-selectivity emerge as likely prerequisites for avoidance of adverse central CB1 mediated side effects. SN - 1744-7674 UR - https://www.unboundmedicine.com/medline/citation/19939187/Latest_advances_in_cannabinoid_receptor_agonists_ L2 - http://www.tandfonline.com/doi/full/10.1517/13543770903436505 DB - PRIME DP - Unbound Medicine ER -