Cannabinoid receptor brain

Westlake TM, Hewlett AC, Ali SF, Paule MG, Scallet AC, Slikker W Jr. (1991). Chronic exposure to delta 9-tetrahydrocannabinol fails to irreversibly alter brain cannabinoid receptors. Brain Res. 544(1) 145-49. 

Devane WA, Dysarz FA, Johnson MR, et al Determination and characterization of a cannabinoid receptor in rat brain. Mol Pharmacol 34 605—613, 1988 D Souza DC, Kosten TR Cannabinoid antagonists a treatment in search of an illness. Arch Gen Psychiatry 58 330—331,2001... 

HU-210 is (8.1) among the most potent cannabinoids known. Its enantiomer HU-211 (8.2) does not bind to the cannabinoid receptor and lacks psychotropic side effects (as long as optical purity is guaranteed). In animal models it shows analgesic and antiemetic activity. It also shows neuroprotec-tive effects after brain injury and was tested in humans as anti-traiuna agent, where it did not meet the expectations in a clinical phase III trial. 

The best studied of the endocarmabinoids are anandamide (A -arachidonyl-ethanolamine, AEA)(1) and 2-arachidonylglycerol (2-AG)(2). Anandamide was first identified from porcine brain extracts by Devane and co-workers in 1992 [13], while 2-AG was first reported in 1995 to have been isolated from canine gut [14] and rat brain [15]. More recently, noladin ether (2-arachidonyl-glyceryl ether, 2-AGE)(3) [16], virodhamine (D-arachidonyl-ethanolamine)(4) [17] and A-arachidonyl-dopamine (NADA)(5) [18] were proposed as endogenous ligands for the cannabinoid receptors. In a subsequent publication, the authors failed to detect noladin ether in mammalian brains and questioned the relevance of this compound as an endocarmabinoid [19]. Anandamide, noladin ether and NADA have functional selectivity for CBi receptors, virodhamine is CB2 selective and 2-AG is essentially non-selective. 

Breivogel CS, Childers SR. The functional neuroanatomy of brain cannabinoid receptors. Neurobiol Dis 1998 5 417—431. 

Childers SR, Sexton T, Roy MB. Effects of anandamide on cannabinoid receptors in rat brain membranes. Biochem Pharmacol 1994 47 711-715. 

Deadwyler S, Hampson RE, Childers SR. Functional ignificance of cannabinoid receptors in brain. In Pertwee RG, ed. Cannabinoid Receptors. New York Academic Press, 1995 206-227. 

Devane WA, Hanus L, Breuer A, Pertwee RG, Stevenson LA, Griffin G, Gibson D, Mandelbaum A, Etinger A, Mechoulam R. Isolation and structure of a brain constituent that binds to the cannabinoid receptors. Science 1992 258 1946-1949. 

Devane WA, Axelrod J. Enzymatic synthesis of anandamide, an endogenous ligand for the cannabinoid receptor, by brain membranes. Proc Natl Acad Sci USA 1994 91 6698-6701. 

Fride E, Mechoulam R. Pharmacological activity of the cannabinoid receptor agonist, anandamide, a brain constituent. Eur J Pharmacol 1993 231 313-314. 

Goparaju SK, Ueda N, Taniguchi K, Yamamoto S. Enzymes of porcine brain hydrolyzing 2-arachidonoylglycerol, an endogenous ligand of cannabinoid receptors. Biochem Pharmacol 2001 57 417 423. 

Hampson, AJ, Hill WA, Zan Phillips M, Makriyannis A, Leung E, Eglen, RM, Bornheim LM. Anandamide hydroxylation by brain lipoxygenase metabolite structures and potencies at the cannabinoid receptor. Biophys. Biochim. Acta 1995 1259 173-179. 

Hanus L, Gopher A, Almog S, Mechoulam R. Two new unsaturated fatty acid ethanolamides in brain that bind to the cannabinoid receptor. J Med... 

Herkenham M, Lynn AB, Little MD, Johnson MR, Melvin LS, DeCosta BR, Rice KC. Cannabinoid receptor localization in brain. Proc Natl Acad Sci 1990 87 1932-1936. 

Howlett AC. The CB1 cannabinoid receptor in the brain. Neurobiol Dis 1998a 5 405-416. 

Rinaldi-Carmona M, Bath F, Heaulme M, Shire D, Calandra B, Congy C, Martinez S, Maruani J, Neliat G, Caput D, Ferrara P, Soubrie P, Breliere JC, Lefur G. SR14176A, a potent and selective antagonist of the brain cannabinoid receptor. FEBS Lett 1994 350 240-244. 

Schuel H, Goldstein E, Mechoulam R, Zimmerman AM, Zimmerman S. Anandamide (arachidonylethanlamide), a brain cannabinoid receptor agonist, reduces sperm fertilizing capacity in sea urchins by inhibiting the acro-some reaction. Proc Natl Acad Sci USA, 1994 91 9460-9464. 

Vogel Z, Barg R, Levy D, Saya E Eleldman, Mechoulam R. Anandamide, a brain endogenous compound, interacts specifically with cannabinoid receptors and inhibits adenylate cyclase. J Neurochem 1993 61 352-355. 

Yamada K, Rice KC, Flippen-Anderson JL, Eissenstat MA, Ward SJ, Johnson MR, Howlett AC. (Ami noalky Ijindole iso thiocyanates as potential electrophylic affinity ligands for the brain cannabinoid receptor. J Med Chem 1996 39 1967-1974. 

Our development of [123I]AM281, an antagonist radioligand for brain cannabinoid receptors, has allowed us to image this receptor for the first time in vivo. Ex vivo autoradiographic experiments have been conducted in rodents, and SPECT studies have been conducted in baboons. Research... 

Jansen EM, Haycock DA, Ward SJ, Seybold VS. Distribution of cannabinoid receptors in rat brain determined with aminoalkylindoles. Brain Res 1992 575 93-102. 

JC, Lefur G. SR141716A, a potent and selective antagonist of the brain cannabinoid receptor. FEBS Lett 1994 350 240-244. 

Gatley SJ, Gilford AN, Volkow ND, Lan R, Makriyannis A. Iodine-123 labeled AM251 a radioiodinated ligand which binds in vivo to the mouse brain CB1 cannabinoid receptor. Eur J Pharmacol 1996 307 301-308. 

Mathews WB, Ravert HR, Musachio JL, Frank RA, Rinaldi-Carmona M, Barth F, Dannals RF. Synthesis of [1SF] SR144385 a selective radioligand for positron emission tomographic studies of brain cannabinoid receptors. J Labelled Compd Radiopharm 1994 42 589-596. 

Burkey TH, Quock RM, Consroe P, Roeske WR, Yamamura HI. delta-9-Tetrahydrocannabinol is a partial agonist of cannabinoid receptors in mouse brain. Eur J Pharmacol 1997 323 R3-R4. 

Gifford AN, Tang Y, Gatley SJ, Volkow ND, Lan R, Makriyannis A. Effect of the cannabinoid receptor SPECT agent, AM 281, on hippocampal acetylcholine release from rat brain slices. Neurosci Lett 1997 238 84-86. 

Herkenham M, Lynn AB, Johnson MR, Melvi LS, de Costa BR and Rice KC (1991). Characterisation and localisation of cannabinoid receptors in rat brain A quantitative in vitro autoradiographic study. Journal of Neuroscience, 11, 563-583. 

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