The endocannabinoid nervous system: Unique opportunities for therapeutic intervention

Pharmacology and Therapeutics

Volumn 90, Issue 1, 2001, Pages 45-60

  Porter, Amy C ^a   Felder, Christian C ^a  

^a ELI LILLY AND COMPANY   (United States)

Author keywords

Allosteric modulator; Anandamide; Cannabinoid; Fatty acid amidohydrolase

Indexed keywords

1 DEOXY 3 (1,1 DIMETHYLBUTYL) DELTA8 TETRAHYDROCANNABINOL; 2 ARACHIDONOYLGLYCEROL; 2 METHYL 3 (1 NAPHTHOYL) 1 PROPYLINDOLE; 2,3 DIHYDRO 5 METHYL 3 (MORPHOLINOMETHYL) 6 (1 NAPHTHOYL)PYRROLO[1,2,3 DE][1,4]BENZOXAZINE; 4 (1,1 DIMETHYLHEPTYL) 1',2',3',4',5',6' HEXAHYDRO 2,3' DIHYDROXY 6' (3 HYDROXYPROPYL)BIPHENYL; 4 [6 METHOXY 2 (4 METHOXYPHENYL) 3 BENZOFURANYLCARBONYL]BENZONITRILE; 5 (1,1 DIMETHYLHEPTYL) 2 (3 HYDROXY 7 HYDROXYMETHYLDECAHYDRO 1 NAPHTHYL)PHENOL; 5 (4 CHLORO 3 METHYLPHENYL) 1 (4 METHYLBENZYL) N (1,3,3 TRIMETHYLBICYCLO[2.2.1]HEPTAN 2 YL) 3 PYRAZOLECARBOXAMIDE; 6 IODO 3 (4 METHOXYBENZOYL) 2 METHYL 1 (2 MORPHOLINOETHYL)INDOLE; ANANDAMIDE; CANNABINOID 1 RECEPTOR; CANNABINOID 2 RECEPTOR; CANNABINOID RECEPTOR AGONIST; DEXANABINOL; DRONABINOL; LEVONANTRADOL; METHANANDAMIDE; NABILONE; PALMIDROL; RIMONABANT; UNCLASSIFIED DRUG;

ANXIETY NEUROSIS; BIOSYNTHESIS; CARDIOVASCULAR DISEASE; CELLULAR DISTRIBUTION; CENTRAL NERVOUS SYSTEM; DRUG DESIGN; DRUG DISPOSITION; DRUG RECEPTOR BINDING; DRUG RELEASE; DRUG SYNTHESIS; DRUG TRANSPORT; FEEDING BEHAVIOR; GLAUCOMA; HUMAN; MENTAL DISEASE; MOTOR DYSFUNCTION; NEUROPROTECTION; NONHUMAN; PAIN; PRIORITY JOURNAL; REVIEW; SIGNAL TRANSDUCTION; VOMITING;

AMIDOHYDROLASES; ANALGESICS; ANIMALS; ANTI-ANXIETY AGENTS; ANTIEMETICS; APPETITE STIMULANTS; ARACHIDONIC ACIDS; BRAIN CHEMISTRY; CANNABINOIDS; ENDOCANNABINOIDS; GLAUCOMA; HUMANS; MOVEMENT DISORDERS; NEUROPROTECTIVE AGENTS; POLYUNSATURATED ALKAMIDES; RECEPTORS, CANNABINOID; RECEPTORS, DRUG; SIGNAL TRANSDUCTION;

EID: 0034929449     PISSN: 01637258     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0163-7258(01)00130-9     Document Type: Review

References (181)

1. Marihuana
2. In-vitro and in-vivo action of cannabinoids
3. The cloned rat hydrolytic enzyme responsible for the breakdown of anandamide also catalyzes its formation via the condensation of arachidonic acid and ethanolamine
4. Fatty acid amides of ethanolamine in mammalian tissues
5. Cannabinoids control spasticity and tremor in a multiple sclerosis model
6. Neuroprotective activity of HU-211, a novel NMDA antagonist, in global ischemia in gerbils
7. HU-211, a nonpsychotropic cannabinoid, improves neurological signs and reduces brain damage after severe forebrain ischemia in rats
8. Functional role of high-affinity anandamide transport, as revealed by selective inhibition
9. Brain regional distribution of endocannabinoids: Implications for their biosynthesis and biological function
10. Triflouromethyl ketone inhibitors of fatty acid amide hydrolase: A probe of structural and conformartional features contributing to inhibition
11. Exceptionally potent inhibitors of fatty acid amide hydrolase: The enzyme responsible for degradation of endogenous oleamide and anandamide
12. Enhanced long-term potentiation in mice lacking cannabinoid CB1 receptors
13. Cannabinoid-receptor expression in human leukocytes
14. Activation of mitogen-activated protein kinases by stimulation of the central cannabinoid receptor CB1
15. Cannabinoid receptor CB1 activates the Na+/H+exchanger NHE-1 isoform via Gi-mediated mitogen activated protein kinase signaling transduction pathways
16. Gi protein modulation induced by a selective inverse agonist for the peripheral cannabinoid receptor CB2: Implication for intracellular signalization cross-regulation
17. Soft cannabinoid analogues as potential anti-glaucoma agents
18. Expression of the CB1 and CB2 receptor messenger RNAs during embryonic development in the rat
19. Immunomodulation by cannabinoids is absent in mice deficient for the cannabinoid CB(2) receptor
20. Occurrence and biosynthesis of endogenous cannabinoid precursor N-arachidonoyl phosphatidylethanolamine, in rat brain
21. Potentiation of anandamide hypotension by the transport inhibitor AM404
22. Control of pain initiation by endogenous cannabinoids
23. Cannabinoid receptor agonists inhibit Ca current in NG108-15 neuroblastoma cells via a pertussis toxin-sensitive mechanism
24. Appetite suppression and weight loss after the cannabinoid antagonist SR 141716
25. Molecular characterization of an enzyme that degrades neuromodulatory fatty-acid amides
26. Cannabinoids modulate potassium current in cultured hippocampal neurons
27. Anandamide amidohydrolase activity in rat brain microsomes. Identification and partial characterization
28. Enzymatic synthesis and degradation of anandamide, a cannabinoid receptor agonist
29. Production and physiological actions of anandamide in the vasculature of the rat kidney
30. Enzymatic synthesis of anandamide, an endogenous ligand for the cannabinoid receptor, by brain membranes
31. Determination and characterization of a cannabinoid receptor in rat brain
32. Isolation and structure of a brain constituent that binds to the cannabinoid receptor
33. "Endocannabinoids" and other fatty acid derivatives with cannabimimetic properties: Biochemistry and possible physiopathological relevance
34. Biochemistry of the endogenous ligands of cannabinoid receptors
35. Formation and inactivation of endogenous cannabinoid anandamide in central neurons
36. Biosynthesis of anandamide and related acylethanolamides in mouse J774 macrophages and N18 neuroblastoma cells
37. The novel endogenous cannabinoid 2-arachidonoylglycerol is inactivated by neuronal- and basophil-like cells: Connections with anandamide
38. Prospects for pharmacological intervention in Alzheimer disease
39. N-acylethanolamine accumulation in infacted myocardium
40. The efficacy and safety of nabilone (a synthetic cannabinoid) in the treatment of anxiety
41. Mast cells express a peripheral cannabinoid receptor with differential sensitivity to anandamide and palmitoylethanolamide
42. Nonpsychotropic cannabinoid acts as a functional N-methyl-D-aspartate receptor blocker
43. Cannabinoid agonists stimulate both receptor- and non-receptor-mediated signal transduction pathways in cells transfected with and expressing cannabinoid receptor clones
44. Anandamide, an endogenous cannabimimetic eicosanoid, binds to the cloned human cannabinoid receptor and stimulates receptor-mediated signal transduction
45. Comparison of the pharmacology and signal transduction of the human cannabinoid CB1 and CB2 receptors
46. Isolation and measurement of the endogenous cannabinoid receptor agonist, anandamide, in brain and peripheral tissues of human and rat
47. LY320135, a novel cannabinoid CB1 receptor antagonist, unmasks coupling of the CB1 receptor to stimulation of cAMP accumulation
48. The endogenous cannabinoid system and brain development
49. Anti-tumoral action of cannabinoids: Involvement of sustained ceramide accumulation and extracellular signal-regulated kinase activation
50. Cannabinoid CB1 receptor of cat cerebral arterial muscle functions to inhibit L-type Ca2+ channel current
51. Large receptor reserve for cannabinoid actions in the central nervous system
52. Potentiation of the action of anandamide on hippocampal slices by the fatty acid amide hydrolase inhibitor, palmitylsulphonyl fluoride (AM 374)
53. Isotope dilution GC/MS determination of anandamide and other fatty acylethanolamides in rat blood plasma
54. Dopamine activation of endogenous cannabinoid signaling in dorsal striatum
55. The cannabinoid agonist HU 210 modifies rat behavioural responses to novelty and stress
56. Induction of the Krox 24 transcription factor in striosomes by a cannabinoid agonist
57. Concurrent stimulation of cannabinoid CB1 and dopamine D2 receptors augments cAMP accumulation in striatal neurons: Evidence for a Gs linkage to the CB1 receptor
58. Agonist selective regulation of G proteins by cannabinoid CB(1) and CB(2) receptors
59. Loss of cannabinoid receptors in the substantia nigra in Huntington's disease
60. Cannabinoid receptors in the human brain: A detailed anatomical and quantitative autoradiographic study in the fetal, neonatal and adult human brain
61. A single dose study of nabilone, a synthetic cannabinoid
62. The CB1 cannabinoid receptor is coupled to the activation of protein kinase B/Akt
63. Cloning and pharmacological characterization of the rat CB(2) cannabinoid receptor
64. Antianxiety effect of cannabidiol in the elevated plus-maze
65. Cannabidiol and (-)Delta9-tetrahydrocannabinol are neuroprotective antioxidants
66. Formation of N-acyl-phosphatidylethanolamine and N-acylethanolamine (including anandamide) during glutamate-induced neurotoxicity
67. Two new unsaturated fatty acid ethanolamides in brain that bind to the cannabinoid receptor
68. Marihuana smoking and intraocular pressure
69. Endocannabinoids and vascular function
70. Characterization of the kinetics and distribution of N-arachidonylethanolamine (anandamide) hydrolysis by rat brain
71. Accumulation of N-arachidonoylethanolamine (anandamide) into cerebellar granule cells occurs via facilitated diffusion
72. Cannabinoid CB1 receptors fail to cause relaxation, but couple via Gi/Go to the inhibition of adenylyl cyclase in carotid artery smooth muscle
73. Inhibition of neuroblastoma adenylate cyclase by cannabinoid and nantradiol compounds
74. Cannabinoid inhibition of adenylate cyclase. Pharmacology of the response of neuroblastoma cell membranes
75. Involvement of Gi in the inhibition of adenylate cyclase by cannabinoid drugs
76. Inhibition of exocytotic noradrenaline release by presynaptic cannabinoid CB1 receptors on peripheral sympathetic nerves
77. The anti-hyperalgesic actions of the cannabinoid anandamide and the putative CB2 receptor agonist palmitoylethanolamide in visceral and somatic inflammatory pain
78. Cannabinoid-induced mesenteric vasodilation through an endothelial site distinct from CB1 or CB2 receptors
79. Isolation, identification and synthesis of an endogenous arachidonic amide that inhibits calcium channel antagonist 1,4-dihydropyridine binding
80. The cannabinoid receptor-pharmacologic identification, anatomical localization and cloning
81. Equilibrium in the hydrolysis and synthesis of cannabimimetic anandamide demonstrated by a purified enzyme
82. Cannabinoid CB1 receptor-mediated inhibition of NMDA- and kainate-stimulated noradrenaline and dopamine release in the brain
83. Isotope dilution mass spectrometric measurements indicate that arachidonylethanolamide, the proposed endogenous ligand of the cannabinoid receptor, accumulates in rat brain tissue post mortem but is contained at low levels in or is absent from fresh tissue
84. SNaRIs, NaSSAs, and NaRIs: New agents for the treatment of depression
85. Liquid chromatographic-atmospheric pressure chemical ionization mass spectrometric determination of anandamide and its analogs in rat brain and peripheral tissues
86. The identification of an anti-inflammatory agent present in egg yolk, soybean lecithin and peanut oil
87. Reversible hydrolysis and synthesis of anandamide demonstrated by recombinant rat fatty-acid amide hydrolase
88. The palmitoylethanolamide and oleamide enigmas: Are these two fatty acid amides cannabimimetic?
89. SR141716A is an inverse agonist at the human cannabinoid CB1 receptor
90. AM630 is an inverse agonist at the human cannabinoid CB1 receptor
91. Allosteric interactions of staurosporine and other indolocarbazoles with N-[methyl-(3)H]scopolamine and acetylcholine at muscarinic receptor subtypes: Identification of a second allosteric site
92. Unresponsiveness to cannabinoids and reduced addictive effects of opiates in CB1 receptor knockout mice
93. Nabilone: A synthetic cannabinoid of medicinal value
94. Effect of nabilone on nausea and vomiting after total abdominal hysterectomy
95. Cloning of two mouse genes encoding alpha 2-adrenergic receptor subtypes and identification of a single amino acid in the mouse alpha 2-C10 homolog responsible for an interspecies variation in antagonist binding
96. Pharmacology and stereoselectivity of structurally novel cannabinoids in mice
97. Functional CB1 cannabinoid receptors in human vascular endothelial cells
98. Localization of cannabinoid receptors and nonsaturable high-density cannabinoid binding sites in peripheral tissues of the rat: Implications for receptor-mediated immune modulation by cannabinoids
99. Cannabinoids inhibit N-type calcium channels in neuroblastoma-glioma cells
100. Cannabinoids activate an inwardly rectifying potassium conductance and inhibit Q-type calcium currents in AtT20 cells transfected with rat brain cannabinoid receptor
101. Localization of cannabinoid receptor in the human developing and adult basal ganglia. Higher levels in the striatonigral neurons
102. Pharmacological and biochemical interactions between opioids and cannabinoids
103. Two distinctive antinociceptive systems in rats with pathological pain
104. Cannabinoid transmission and pain perception
105. Spinal cannabinoids are anti-allodynic in rats with persistent inflammation
106. Lack of morphine-induced dopamine release in the nucleus accumbens of cannabinoid CB(1) receptor knockout mice
107. Structure of a cannabinoid receptor and functional expression of the cloned cDNA
108. Two novel classes of neuroactive fatty acid amides are substrates for mouse neuroblastoma "anandamide amidohydrolase"
109. Recent advantages in cannabinoid research
110. A total synthesis of d1 delta-1 tetrahydrocannabinol, the active constituent of hashish
111. Identification of an endogenous 2-monoglyceride, present in canine gut, that binds to cannabinoid receptors
112. Structure-activity relationships of tricyclic and nonclassical bicyclic cannabinoids
113. An analgesia circuit activated by cannabinoids
114. Cannabinoid receptors differentially modulate potassium A and D currents in hippocampal neurons in culture
115. Cannabinoids: Possible role in patho-physiology and therapy of Gilles de la Tourette syndrome
116. Molecular characterization of a peripheral receptor for cannabinoids
117. The non-psychotropic cannabinoid (+)-(3S,4S)-7-hydroxy-delta 6-tetrahydrocannabinol 1,1-dimethylheptyl (HU-211) attenuates N-methyl-D-aspartate receptor-mediated neurotoxicity in primary cultures of rat forebrain
118. Cannabinoids and neuroprotection in global and focal cerebral ischemia and in neuronal cultures
119. Inhibition of serotonin release in the mouse brain via presynaptic cannabinoid CB1 receptors
120. Acute administration of the CB1 cannabinoid receptor antagonist SR 141716A induces anxiety-like responses in the rat
121. A single amino acid difference accounts for the pharmacological distinctions between the rat and human 5-hydroxytryptamine1B receptors
122. Ophthalmic arachidonylethanolamide decreases intraocular pressure in normotensive rabbits
123. Effect of the CB1 receptor antagonist, SR141716A, on cannabinoid-induced ocular hypotension in normotensive rabbits
124. Fatty acid amide hydrolase competitively degrades bioactive amides and esters through a nonconventional catalytic mechanism
125. Further evidence for the presence of cannabinoid CB1 receptors in mouse vas deferens
126. SR 144528, an antagonist for the peripheral cannabinoid receptor that behaves as an inverse agonist
127. A double-blind randomised cross-over comparison of nabilone and metoclopramide in the control of radiation-induced nausea
128. Mead ethanolamide, a novel eicosanoid, is an agonist for the central (CB1) and peripheral (CB2) cannabinoid receptors
129. Carrier-mediated uptake of the endogenous cannabinoid anandamide in RBL-2H3 cells
130. Endocannabinoids: A new class of vasoactive substances
131. Expression of a brain-type cannabinoid receptor (CB1) in alveolar type II cells in the lung: Regulation by hydrocortisone
132. Selective vulnerability in Huntington's disease: Preferential loss of cannabinoid receptors in lateral globus pallidus
133. Characterization of two cloned human CB1 cannabinoid receptor isoforms
134. Modulation of CB1 cannabinoid receptor functions after a long-term exposure to agonist or inverse agonist in the Chinese hamster ovary cell expression system
135. Presence of cannabinoid binding sites in the brain from early postnatal ages
136. Activation of corticotropin-releasing factor in the limbic system during cannabinoid withdrawal
137. Role of the endogenous cannabinoid system in the regulation of motor activity
138. Cannabis for migraine treatment: The once and future prescription? An historical and scientific review
139. Cannabinoid effects in basal ganglia in a rat model of Parkinson's disease
140. The N-acylation-phosphodiesterase pathway and cell signalling
141. Properties of rat liver N-acylethanolamine amidohydrolase
142. Occurrence and postmortem generation of anandamide and other long-chain N-acylethanolamines in mammalian brain
143. Anandamide and other N-acylethanolamines in mouse peritoneal macrophages
144. Changes in anandamide levels in mouse uterus are associated with uterine receptivity for embryo implantation
145. Cannabinoid receptor agonists protect cultured rat hippocampal neurons from excitotoxicity
146. Cannabinoid receptor agonists inhibit glutamatergic synaptic transmission in rat hippocampal cultures
147. An amino-terminal variant of the central cannabinoid receptor resulting from alternative splicing
148. A nonpsychotropic cannabinoid, HU-211, has cerebroprotective effects after closed head injury in the rat
149. Evaluation of binding in a transfected cell line expressing a peripheral cannabinoid receptor (CB2): Identification of cannabinoid receptor subtype selective ligands
150. The endogenous lipid anandamide is a full agonist at the human vanilloid receptor (hVR1)
151. Interactions between delta 9-tetrahydrocannabinol and kappa opioids in mice
152. Behavioral, pharmacological, and molecular characterization of an amphibian cannabinoid receptor
153. Involvement of cannabinoid receptors in the intraocular pressure-lowering effects of WIN55212-2
154. Localization of cannabinoid CB1 receptors in the human anterior eye and retina
155. Transacylase-mediated and phosphodiesterase-mediated synthesis of N-arachidonoylethanolamine, an endogenous cannabinoid-receptor ligand, in rat brain microsomes. Comparison with synthesis from free arachidonic acid and ethanolamine
156. Enzymatic synthesis of anandamide, an endogenous cannabinoid receptor ligand, through N-acylphosphatidylethanolamine pathway in testis: Involvement of Ca(2+)-dependent transacylase and phosphodiesterase activities
157. Evidence that 2-arachidonoylglycerol but not N-palmitoylethanolamine or anandamide is the physiological ligand for the cannabinoid CB2 receptor. Comparison of the agonistic activities of various cannabinoid receptor ligands in HL-60 cells
158. Effects of cannabinoids on dopamine release in the corpus striatum and the nucleus accumbens in vitro
159. Bidirectional allosteric effects of agonists and GTP at alpha(2A/D)-adrenoceptors
160. Hashish
161. Cannabinoids inhibit N- and P/Q-type calcium channels in cultured rat hippocampal neurons
162. Anandamide amidohydrolase (fatty acid amide hydrolase)
163. Partial purification and characterization of the porcine brain enzyme hydrolyzing and synthesizing anandamide
164. Anandamide amidohydrolase from porcine brain. Partial purification and characterization
165. Reduction of stress-induced analgesia but not of exogenous opioid effects in mice lacking CB1 receptors
166. Cholinesterase inhibitors for the treatment of Alzheimer's disease in the elderly
167. Platelet- and macrophage-derived endogenous cannabinoids are involved in endotoxin-induced hypotension
168. The CB1 cannabinoid receptor can sequester G-proteins, making them unavailable to couple to other receptors
169. Cardiovascular effects of (-)-11-OH-delta 8-tetrahydrocannabinol-dimethylheptyl in rats
170. Activation of peripheral CB1 cannabinoid receptors in haemorrhagic shock
171. Mesenteric vasodilation mediated by endothelial anandamide receptors
172. Pain modulation by release of the endogenous cannabinoid anandamide
173. Distribution and characterization of anandamide amidohydrolase in mouse brain and liver
174. Marijuana and medicine: Assessing the science base: A summary of the 1999 Institute of Medicine report
175. Antinociceptive activity of intrathecally administered cannabinoids alone, and in combination with morphine, in mice
176. Anandamide induces overeating: Mediation by central cannabinoid (CB1) receptors
177. Prozac (fluoxetine, Lilly 110140), the first selective serotonin uptake inhibitor and an antidepressant drug: Twenty years since its first publication
178. GC/MS analysis of anandamide and quantification of N-arachidonoylphosphatidylethanolamides in various brain regions, spinal cord, testis, and spleen of the rat
179. Increased mortality, hypoactivity, and hypoalgesia in cannabinoid CB1 receptor knockout mice
180. Vanilloid receptors on sensory nerves mediate the vasodilator action of anandamide
181. The anandamide transport inhibitor AM404 activates vanilloid receptors