Recent Patents on CNS Drug Discovery

Vincenzo Di Marzo
Istituto di Chimica Biomolecolare (I.C.B.)
Consiglio Nazionale delle Ricerche (C.N.R.)
Via Campi Flegrei 34
Pozzuoli, Napoli 80078


Pharmacology and Toxicology of Cannabis Derivatives and Endocannabinoid Agonists

Author(s): Gilberto Gerra, Amir Zaimovic, Maria L. Gerra, Roberto Ciccocioppo, Andrea Cippitelli, Giovanni Serpelloni and Lorenzo Somaini

Affiliation: Health and Human Development Section, Division for Operations, United Nations Office on Drugs and Crime, Room D1438, P.O. Box 500, 1400 Vienna, Austria.

Keywords: Cannabis, endocannabinoids, receptor agonists, abuse


For centuries Cannabis sativa and cannabis extracts have been used in natural medicine. Δ9- tetrahydrocannabinol (THC) is the main active ingredient of Cannabis. THC seems to be responsible for most of the pharmacological and therapeutic actions of cannabis. In a few countries THC extracts (i.e. Sativex®) or THC derivatives such as nabilone, and dronabinol are used in the clinic for the treatment of several pathological conditions like chemotherapy-induced nausea and vomiting, multiple sclerosis and glaucoma. On the other hand the severe side effects and the high abuse liability of these agents represent a serious limitation in their medical use. In addition, diversion in the use of these active ingredients for recreational purpose is a concern. Over recent years, alternative approaches using synthetic cannabinoid receptor agonists or agents acting as activators of the endocannabinoid systems are under scrutiny with the hope to develop more effective and safer clinical applications. Likely, in the near future few of these new molecules will be available for clinical use. The present article reviews recent study and patents with focus on the cannabinoid system as a target for the treatment of central nervous system disorders with emphasis on agonists.

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Article Details

Page: [46 - 52]
Pages: 7
DOI: 10.2174/157488910789753521