I-K (Synthetics Pre-2010)

SYNTHETICS and COMPOUNDS THAT AFFECT the ENDOCANNABINOID SYSTEM Pre-2010

IBUPROFEN (Blocks Breakdown of Anandamide [Which is What Actually Relieves Your Pain])
JWH-015 (CB2 and GPR-55 Agonist, Mildly Activates CB1 Receptors)
JWH-018 (CB1 Agonist)
JWH-073 (CB1 and CB2 Agonist)
JWH-133 / 3-(1_1_-dimethylbutyl)-1-deoxy-_8-THC (CB2 Agonist)
JZL-184 (Blocks Breakdown of 2-AG)
KM-233 (CB2 Agonist)
KN38-7271 / BAY38-7271 (CB1 and CB2 Agonist)


IBUPROFEN
Ibuprofen inhibits rat brain deamidation of anandamide at pharmacologically relevant concentrations. Mode of inhibition and structure-activity relationship (full–1997) http://jpet.aspetjournals.org/content/283/2/729.long
Ibuprofen inhibits the metabolism of the endogenous cannabimimetic agent anandamide (abst–1997) http://www.ncbi.nlm.nih.gov/pubmed/9060042
Inhibition of anandamide hydrolysis by the enantiomers of ibuprofen, ketorolac, and flurbiprofen (abst–1999) http://www.ncbi.nlm.nih.gov/pubmed/9989926
Differences in the pharmacological properties of rat and chicken brain fatty acid amidohydrolase (full–2000) http://www.ncbi.nlm.nih.gov/pmc/articles/PMC1572338/
Effects of pH on the inhibition of fatty acid amidohydrolase by ibuprofen (full–2001) http://www.ncbi.nlm.nih.gov/pmc/articles/PMC1572815/
Acidic nonsteroidal anti-inflammatory drugs inhibit rat brain fatty acid amide hydrolase in a pH-dependent manner (abst–2003) http://www.ncbi.nlm.nih.gov/pubmed/12751821
Anandamide metabolism by fatty acid amide hydrolase in intact C6 glioma cells. Increased sensitivity to inhibition by ibuprofen and flurbiprofen upon reduction of extrabut not intracellular pH (abst–2003) http://www.ncbi.nlm.nih.gov/pubmed/12644895
Synergistic antinociceptive effects of anandamide, an endocannabinoid, and nonsteroidal anti-inflammatory drugs in peripheral tissue: a role for endogenous fatty-acid ethanolamides? (abst–2006) http://www.ncbi.nlm.nih.gov/pubmed/17027744
Local interactions between anandamide, an endocannabinoid, and ibuprofen, a nonsteroidal anti-inflammatory drug, in acute and inflammatory pain (abst–2006) http://www.ncbi.nlm.nih.gov/pubmed/16480822
Antihyperalgesic effects of local injections of anandamide, ibuprofen, rofecoxib and their combinations in a model of neuropathic pain (abst–2006) http://www.ncbi.nlm.nih.gov/pubmed/16442133
Inhibition of fatty acid amide hydrolase, a key endocannabinoid metabolizing enzyme, by analogues of ibuprofen and indomethacin (abst–2009) http://www.ncbi.nlm.nih.gov/pubmed/17397826
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JWH-015
Effects of cannabinoid receptor agonists on neuronally-evoked contractions of urinary bladder tissues isolated from rat, mouse, pig, dog, monkey and human (full-2000) http://www.ncbi.nlm.nih.gov/pmc/articles/PMC1571997/?tool=pmcentrez
Targeting CB2 cannabinoid receptors as a novel therapy to treat malignant lymphoblastic disease (full–2002) http://bloodjournal.hematologylibrary.org/cgi/content/full/100/2/627?ijkey=eb71d6d7a06f311440761cfac6a7d081bcc2771d
Species comparison and pharmacological characterization of rat and human CB2 cannabinoid receptors (abst-2004) http://www.ncbi.nlm.nih.gov/pubmed/15556131
CB2 cannabinoid receptors in trabecular meshwork cells mediate JWH015-induced enhancement of aqueous humor outflow facility (full-2005) http://www.iovs.org/content/46/6/1988.long
Stimulation of cannabinoid receptor 2 (CB2) suppresses microglial activation (link to PDF–2005) http://www.springerlink.com/content/tq777102q4185073/fulltext.html
Avoidance of Abeta[(25-35)] / (H(2)O(2)) -induced apoptosis in lymphocytes by the cannabinoid agonists CP55,940 and JWH-015 via receptor-independent and PI3K-dependent mechanisms: role of NF-kappaB and p53 (abst–2005) http://www.ncbi.nlm.nih.gov/pubmed/17017986
Chemical modification of the naphthoyl 3-position of JWH-015: In search of a fluorescent probe to the cannabinoid CB2 receptor (abst–2005) http://www.sciencedirect.com/science/article/pii/S0960894X05006803
CB2 cannabinoid receptor agonist, JWH-015 triggers apoptosis in immune cells: Potential role for CB2 selective ligands as immunosuppressive agents (full–2006) http://www.ncbi.nlm.nih.gov/pmc/articles/PMC1864948/
Potential role for CB2 selective ligands as immunosuppressive agents (full–2007) http://www.ncbi.nlm.nih.gov/pmc/articles/PMC1864948/?tool=pmcentrez
Opposing control of cannabinoid receptor stimulation on amyloid-beta-induced reactive gliosis: in vitro and in vivo evidence (full-2007) http://jpet.aspetjournals.org/content/322/3/1144.long
Spinal cannabinoid receptor type 2 activation reduces hypersensitivity and spinal cord glial activation after paw incision (full–2007) http://journals.lww.com/anesthesiology/Fulltext/2007/04000/Spinal_Cannabinoid_Receptor_Type_2_Activation.21.aspx
In vivo effects of CB2 receptor-selective cannabinoids on the vasculature of normal and arthritic rat knee joints (full-2008) http://www.pubmedcentral.nih.gov/articlerender.fcgi?artid=2219539&tool=pmcentrez
CB2 cannabinoid receptor agonist JWH-015 modulates human monocyte migration through defined intracellular signaling pathways (full–2008) http://ajpheart.physiology.org/content/294/3/H1145.long
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Endocannabinoids enhance lipid synthesis and apoptosis of human sebocytes via cannabinoid receptor-2-mediated signaling (full–2008) http://www.fasebj.org/content/22/10/3685.long
Behavioral effects of CB2 cannabinoid receptor activation and its influence on food and alcohol consumption (abst-2008) http://www.ncbi.nlm.nih.gov/pubmed/18991890
Presence and regulation of cannabinoid receptors in human retinal pigment epithelial cells (full–2009) http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2697670/?tool=pubmed
Inhibition of human tumour prostate PC-3 cell growth by cannabinoids R(+)-Methanandamide and JWH-015: Involvement of CB2 (full-2009) http://www.nature.com/bjc/journal/v101/n6/full/6605248a.html
The activation of cannabinoid CB2 receptors stimulates in situ and in vitro beta-amyloid removal by human macrophages (abst–2009) http://www.ncbi.nlm.nih.gov/pubmed/19505450?itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsPanel.Pubmed_RVDocSum&ordinalpos=18
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JWH-018
Withdrawal Phenomena and Dependence Syndrome After the Consumption of “Spice Gold” (full–2009) http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2719097/?tool=pmcentrez
Spice drugs: cannabinoids as a new designer drugs (abst–2009) http://www.ncbi.nlm.nih.gov/pubmed/19718488
Spice: a never ending story? (abst–2009) http://www.ncbi.nlm.nih.gov/pubmed/19589652
Synthetic cannabis mimic found in herbal incense (news–2009) http://www.rsc.org/chemistryworld/News/2009/January/15010901.asp


JWH-073
Spice drugs: cannabinoids as a new designer drugs (abst–2009) http://www.unboundmedicine.com/medline/ebm/record/19718488/abstract/%5BSpice_drugs:_cannabinoids_as_a_new_designer_drugs_%5D
Spice: a never ending story? (abst–2009) http://www.ncbi.nlm.nih.gov/pubmed/19589652


JWH-133 / 3-(1_1_-dimethylbutyl)-1-deoxy-_8-THC
Inhibition of tumor angiogenesis by cannabinoids (full–2003) http://www.fasebj.org/cgi/reprint/02-0795fjev1?maxtoshow=&hits=10&RESULTFORMAT=&fulltext=cannabis&andorexactfulltext=and&searchid=1&FIRSTINDEX=20&sortspec=relevance&resourcetype=HWCIT
Inhibition of guinea-pig and human sensory nerve activity and the cough reflex in guinea-pigs by cannabinoid (CB2) receptor activation (full-2003) http://www.ncbi.nlm.nih.gov/pmc/articles/PMC1574031/?tool=pubmed
Effects of cannabinoid receptor-2 activation on accelerated gastrointestinal transit in lipopolysaccharide-treated rats (full-2004) http://www.ncbi.nlm.nih.gov/pmc/articles/PMC1575196/?tool=pmcentrez
Non-psychoactive CB2 cannabinoid agonists stimulate neural progenitor proliferation (full–2006) http://www.fasebj.org/cgi/content/full/20/13/2405?maxtoshow=&hits=10&RESULTFORMAT=&fulltext=cannabis&andorexactfulltext=and&searchid=1&FIRSTINDEX=0&sortspec=relevance&resourcetype=HWCIT
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Agonists of cannabinoid receptor 1 and 2 inhibit experimental colitis induced by oil of mustard and by dextran sulfate sodium (full–2006) http://ajpgi.physiology.org/content/291/2/G364.long
Signaling pathways involved in the cardioprotective effects of cannabinoids (full-2006) https://www.jstage.jst.go.jp/article/jphs/102/2/102_2_155/_pdf
Cannabinoid-2 receptor mediates protection against hepatic ischemia/reperfusion injury (full-2007) http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2228252/?tool=pmcentrez
Cannabinoids Induce Glioma Stem-like Cell Differentiation and Inhibit Gliomagenesis (full-2007) http://www.jbc.org/content/282/9/6854.long
Anti-inflammatory property of the cannabinoid receptor-2-selective agonist JWH-133 in a rodent model of autoimmune uveoretinitis (full–2007) http://www.jleukbio.org/cgi/reprint/82/3/532?maxtoshow=&hits=80&RESULTFORMAT=&fulltext=cannabinoid&searchid=1&FIRSTINDEX=240&resourcetype=HWCIT
Influence of nicotinic receptor modulators on CB2 cannabinoid receptor agonist (JWH133)-induced antinociception in mice (abst–2007) http://www.ncbi.nlm.nih.gov/pubmed/17912054
Attenuation of Experimental Autoimmune Hepatitis by Exogenous and Endogenous Cannabinoids: Involvement of Regulatory T Cells (full–2008) http://molpharm.aspetjournals.org/content/74/1/20.full?maxtoshow=&hits=80&RESULTFORMAT=&fulltext=cannabinoid&searchid=1&FIRSTINDEX=320&resourcetype=HWCIT#content-block
In vivo effects of CB2 receptor-selective cannabinoids on the vasculature of normal and arthritic rat knee joints (full-2008) http://www.pubmedcentral.nih.gov/articlerender.fcgi?artid=2219539&tool=pmcentrez
Regression of Fibrosis after Chronic Stimulation of Cannabinoid CB2 Receptor in Cirrhotic Rats (full–2008) http://jpet.aspetjournals.org/content/324/2/475.full?maxtoshow=&hits=80&RESULTFORMAT=&fulltext=cannabinoid&searchid=1&FIRSTINDEX=320&resourcetype=HWCIT#content-block
Additive Interaction of the Cannabinoid Receptor I Agonist Arachidonyl-2-chloroethylamide with Etomidate in a Sedation Model in Mice (full–2008) http://journals.lww.com/anesthesiology/Fulltext/2008/04000/Additive_Interaction_of_the_Cannabinoid_Receptor_I.19.aspx
Cannabinoid 2 receptor induction by IL-12 and its potential as a therapeutic target for the treatment of anaplastic thyroid carcinoma (full–2008) http://www.nature.com/cgt/journal/v15/n2/full/7701101a.html
Cannabinoid receptor agonists inhibit growth and metastasis of breast cancer (abst–2008) http://www.aacrmeetingabstracts.org/cgi/content/meeting_abstract/2008/1_Annual_Meeting/4081?maxtoshow=&hits=80&RESULTFORMAT=&fulltext=cannabinoid&searchid=1&FIRSTINDEX=480&resourcetype=HWCIT
Involvement of central cannabinoid CB2 receptor in reducing mechanical allodynia in a mouse model of neuropathic pain (abst–2008) http://www.sciencedirect.com/science/article/pii/S0014299908000630
Down-regulation of tissue inhibitor of metalloproteinases-1 in gliomas: a new marker of cannabinoid antitumoral activity? (abst-2008) http://www.ncbi.nlm.nih.gov/pubmed/17675107
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Activation of the cannabinoid 2 receptor (CB2) protects against experimental colitis (full-2009) http://onlinelibrary.wiley.com/doi/10.1002/ibd.20960/full
Cannabinoid CB2 Receptor Potentiates Obesity-Associated Inflammation, Insulin Resistance and Hepatic Steatosis (full–2009) http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2688760/?tool=pubmed
Cannabinoids as novel anti-inflammatory drugs (full–2009) http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2828614/?tool=pubmed
Synthetic cannabinoid receptor agonists inhibit tumor growth and metastasis of breast cancer (full-2009) http://mct.aacrjournals.org/content/8/11/3117.full
CB2 cannabinoid receptor activation is cardioprotective in a mouse model of ischemia/reperfusion (abst-2009) http://www.ncbi.nlm.nih.gov/pubmed/19162037


JZL-184
Selective blockade of 2-arachidonoylglycerol hydrolysis produces cannabinoid behavioral effects (full–2009) http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2605181/
Blockade of 2-arachidonoylglycerol hydrolysis by selective monoacylglycerol lipase inhibitor 4-nitrophenyl 4-(dibenzo[d][1,3]dioxol-5-yl(hydroxy)methyl)piperidine-1-carboxylate (JZL184) Enhances retrograde endocannabinoid signaling (full–2009) http://jpet.aspetjournals.org/content/331/2/591.long
Monoacylglycerol lipase limits the duration of endocannabinoid-mediated depolarization-induced suppression of excitation in autaptic hippocampal neurons (full–2009) http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2784730/


KM-233
Safety and efficacy of a novel cannabinoid chemotherapeutic, KM-233, for the treatment of high-grade glioma (abst–2006) http://www.ncbi.nlm.nih.gov/pubmed/16314952
Preclinical studies of KM-233, a safe and effective classical cannabinoid chemotherapeutic for the treatment of high-grade glioma (news–2006) http://www.aans.org/Media/Article.aspx?ArticleId=36969
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KN38-7271 / BAY38-7271
Characterization of the diarylether sulfonylester (-)-(R)-3-(2-hydroxymethylindanyl-4-oxy)phenyl-4,4,4-trifluoro-1-sulfonate (BAY 38-7271) as a potent cannabinoid receptor agonist with neuroprotective properties (full–2002) http://jpet.aspetjournals.org/content/302/1/359.long
BAY 38-7271: a novel highly selective and highly potent cannabinoid receptor agonist for the treatment of traumatic brain injury (abst–2003) http://www.ncbi.nlm.nih.gov/pubmed/14647528
Neuroprotective and brain edema-reducing efficacy of the novel cannabinoid receptor agonist BAY 38-7271 (abst–2003) http://www.ncbi.nlm.nih.gov/pubmed/14519516
Breakthrough in treatment of Traumatic Brain Injury: KeyNeurotek’s clinical study reaches primary endpoint and shows significant increase in survival (news-2009) http://www.drugs.com/clinical_trials/breakthrough-traumatic-brain-injury-keyneurotek-s-clinical-study-reaches-primary-endpoint-shows-8667.html


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