Home >> Current Pharmaceutical Design, Volume 6, Number 13

The Search for Selective Ligands for the CB2 Receptor

Author: Huffman, J.W.

Source: Current Pharmaceutical Design, Volume 6, Number 13, 1 September 2000 , pp. 1323-1337(15)

Publisher: Bentham Science Publishers

Buy & download fulltext article:

OR

Price: $63.10 plus tax (Refund Policy)

Abstract:

Following the identification of the CB2 receptor several groups explored the development of selective ligands for this receptor which occurs principally in the periphery. This led to the discovery that two cannabimimetic indoles, 1-(2,3-dichlorobenzoyl)- 2-methyl-3-(2-[1-morpholino]ethyl)-5-methoxyindole (L768242) and 2-methyl-1-propyl-3-(1-naphthoyl)indole (JWH-015) have high affinity for the CB2 receptor with low affinity for the CB1 receptor. Shortly thereafter two 1- methoxy-Delta 8 -THC analogues, 1-methoxy-Delta 8 -THC-DMH (L759633) and 1-methoxy-Delta 9(11) -THC-DMH (L759656), were also found to have high affinity for the CB2 receptor and very little affinity for the CB1 receptor. Almost simultaneously two 1-deoxy-Delta 8 -THC analogues, 1-deoxy-11-hydroxy-Delta 8 -THC-DMH (JWH-051) and 1-deoxy-Delta 8 -THC-DMH (JWH-057) were reported to have high affinity for the CB1 receptor, but even greater affinity for the CB 2 receptor. These discoveries gave rise to a concerted effort by Huffman and co-workers to explore the structure-activity relationships (SAR) at CB2 of cannabimimetic indoles and 1-deoxy-Delta 8 -THC analogues. These efforts have resulted in the synthesis and pharmacological evaluation of a number of derivatives of 3-(1-naphthoyl)indoles and 1-deoxy-Delta 8 -THC analogues with various side chains. This review will describe the current status of the results of these studies and discuss the SAR for both these classes of ligands.
More about this publication?
  • Current Pharmaceutical Design publishes timely in-depth reviews covering all aspects of current research in rational drug design. Each issue is devoted to a single major therapeutic area. A Guest Editor who is an acknowledged authority in a therapeutic field has solicits for each issue comprehensive and timely reviews from leading researchers in the pharmaceutical industry and academia.

    Each thematic issue of Current Pharmaceutical Design covers all subject areas of major importance to modern drug design, including: medicinal chemistry, pharmacology, drug targets and disease mechanism.
Related content
Marked list

Tools

Key

Free Content
Free content
New Content
New content
Open Access Content
Open access content
Subscribed Content
Subscribed content
Free Trial Content
Free trial content

Text size:

A | A | A | A
^ Back to top
Share this item with others: These icons link to social bookmarking sites where readers can share and discover new web pages. print icon Print this page