Download PDF by Raphael Mechoulam: Cannabinoids as therapeutics

By Raphael Mechoulam

ISBN-10: 3764370556

ISBN-13: 9783764370558

ISBN-10: 376437358X

ISBN-13: 9783764373580

Only many years in the past the endocannabinoid procedure used to be unknown. at the present time we're conscious that endocannabinoids are inquisitive about a number of the capabilities of the mammalian physique - in neuroprotection, urge for food and suckling, ache, replica, anxiousness, reminiscence, bone formation and so on. This quantity offers an up to date photo of a few of the most important fields of endocannabinoid learn. It summarizes the activities of the endocannabinoids on numerous physiological structures and opens new healing home windows to plenty of diseases.
The first bankruptcy, at the use of hashish in India, might be considered as an expression of due to the natural practitioners, who for hundreds of years handed at the scientific traditions linked to the drug. The bankruptcy on chemistry is a brief precis of energetic plant, artificial and endogenous cannabinoids being investigated this present day, a lot of that are pointed out later within the e-book. Cannabidiol is an strange cannabinoid - it doesn't bind to the identified receptors and but exerts various results. accordingly a bankruptcy is dedicated to it. extra chapters care for the endocannabinoid process and the endocannabinoids in a number of stipulations and physiological structures. The concluding bankruptcy describes the examine performed on Sativex®, a standardized plant extract, almost immediately to be brought in Canada as a drug for a number of sclerosis.
The meant viewers is drug researchers (medicinal chemists, pharmacologists, clinicians), neuroscientists, physiologists, and clinicians drawn to the impact of the endocannabinoid approach in quite a few physiological systems.

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Selectivity data for several of the compounds with regard to CB2/CB1 affinities are described. 3 nM and a Ki value of >5000 nM for CB1. 2 nM at the CB2 receptor and 80 nM at the CB1 receptor. When dosed orally at 100 mg/kg in a mouse pruritis model, this compound reduced scratching by 98% relative to control animals. Structure 22 Shionogi has disclosed a series of amide-containing CB2 modulators stated to be useful in the treatment of inflammation, nephritis, pain, allergies, rheumatoid arthritis, multiple sclerosis, brain tumors and glaucoma [115].

Shionogi & Co. Ltd (JP): WO03070277. 115 Tada Y, Iso Y, Hanasaki K (2002) Pyridone derivative having affinity for cannabinoid 2-type receptor. Shionogi & Co. Ltd (JP): WO02053543. 116 Ferrarini PL, Calderone V, Cavallini T, Manera C, Saccomanni G, Pani L, Ruiu S, Gessa GL (2004) Synthesis and biological evaluation of 1,8-naphthyridin- 4(1H)-on-3-carboxamide derivatives as new ligands of cannabinoid receptor. Bioorg Med Chem 12: 1921–1933 46 M. Maccarrone 117 Huffman JW, Zengin G, Wu MJ, Lu J, Hynd G, Bushell K, Thompson ALS, Bushell S, Tartal C, Hurst DP et al.

Abstr. MEDI, 2 Johnson MR, Melvin LS (1986) The discovery of nonclassical cannabinoid analgetics. ): Cannabinoids as therapeutic agents. CRC Press, Boca Raton, FL, pp 121–145 Devane WA, Dysarz FA, Johnson MR, Melvin LS, Howlett AC (1988) Determination and characterization of a cannabinoid receptor in rat-brain. Mol Pharmacol 34: 605–613 Gerard CM, Mollereau C, Vassart G, Parmentier M (1991) Molecular-cloning of a human cannabinoid receptor which is also expressed in testis. J Biochem 279: 129–134 Mechoulam R, Feigenbaum JJ, Lander N, Segal M, Jarbe TUC, Hiltunen AJ, Consroe P (1988) Enantiomeric cannabinoids: stereospecificity of psychotropic activity.

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Cannabinoids as therapeutics by Raphael Mechoulam


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