Cannabinoid type 1 receptor

Mouse vas deferens (MVD) seems to express CB1 and at least one CB2-like cannabinoid receptor type, as is demonstrated by the presence of CB1 and CB2-like mRNA as well as by data collected from experiments with cannabinoid receptor selective agonists and antagonists (Pertwee, 1999). Furthermore, evidence indicates that a CBl-like receptor exists in vascular endothelium, which upon activation produces significant hypotension (Wagner, 1999). This receptor differs from CB1 in its pharmacological response to some well-characterized cannabimimetics. 

Domenici MR, Azad SC, Marsicano G, Schierloh A, Wotjak CT, Dodt HU, Zieglgansberger W, Futz B, Rammes G (2006) Cannabinoid receptor type 1 located on presynaptic terminals of principal neurons in the forebrain controls glutamatergic synaptic transmission. J Neurosci 26(21) 5794-9... 

Azad, S. C., Eder, M., Marsicano, G., Lutz, B., Zieglgansberger, W., and Rammes, G. (2003). Activation of the cannabinoid receptor type 1 decreases glutamatergic and gabaergic synaptic transmission in the lateral amygdala of the mouse. Leam. Mem. 10, 116-128. 

Leroy S, Griffon N, Bourdel MC et al (2001) Schizophrenia and the cannabinoid receptor type 1 (CB1) association study using a single-base polymorphism in coding exon 1. Am J Med Genet 105 749-752... 

Rossi F, Bellini G, Tolone C et al (2012) The cannabinoid receptor type 2 Q63R variant increases the risk of celiac disease implication for a novel molecular biomarker and future therapeutic intervention. Pharmacol Res 66 88-94... 

Rossi F, Bellini G, Alisi A et al (2012) Cannabinoid receptor type 2 functional variant influences liver damage in children with nonalcoholic fatty liver disease. PLoS One 7 e42259. doi 10.1371/journal.pone.0042259... 

Karsak M, Cohen-Solal M, Freudenberg J (2005) Cannabinoid receptor type 2 gene is... 

Karsak M, Malkin I, Toliat MR (2009) The cannabinoid receptor type 2 (CNR2) gene is associated with hand bone strength phenotypes in an ethnically homogeneous family sample. Hum Genet 126 629-636... 

Gelfand, E. V, Cannon, C. P. Rimonabant a cannabinoid receptor type 1 blocker for management of multiple cardiometabolic risk factors. J. Am. Coll. Cardiol. 2006, 47, 1919-1926. 

Price TJ, Helesic G, Parghi D, Hargreaves KM, Flores CM (2003) The neuronal distribution of cannabinoid receptor type 1 in the trigeminal ganglion of the rat. Neuroscience 120 155-162... 

Storr M, Sibaev A, Marsicano G, Lutz B, Schusdziarra V, Timmermans JP, Allescher HD (2004) Cannabinoid receptor type 1 modulates excitatory and inhibitory neurotransmission in mouse colon. Am J Physiol Gastrointest Liver Physiol 286 G110-Gl 17... 

Fagotto U, Marsicano G, Fezza F, Theodoropoulou M, Grubler Y Arzberger T, Milone A, Losa M, Di Marzo V, Lutz B, Stalla GK (2001) Normal human pituitary gland and pituitary adenomas express cannabinoid receptor type 1 and synthesise endogenous cannabinoids first evidence for a direct role of cannabinoids on hormone modulation at the human pituitary level. J Clin Endocrinol Metab 86 2687-2696... 

Bomer, C., HoUt, V., Sebald, W. and Kraus, J., Transcriptional regulation of the cannabinoid receptor type 1 gene in T cells by caimabinoids, J Leukoc Biol, 81 (2007) 336-343. 

Hermann H, Marsicano G, Lutz B. Coexpression of the cannabinoid receptor type 1 with dopamine and serotonin receptors in distinct neuronal subpopulations of the adult mouse forebrain. Neuroscience 109, 451-460 (2002). 

Not many pyrazoles and indazoles exist in nature. However, many synthetic medicines do contain pyrazoles, pyrazolones, and indazoles. For instance, an anti-inflammatory cyclooxygenase-2 (COX-2) selective inhibitor celecoxib (Celebrex) has the tri-substituted pyrazole as its core structure. A fully substituted pyrazole, rimonabant (Acomplia), is a selective inverse agonist for the cannabinoid receptor type 1 (CBi). Acomplia was marketed in 56 countries for the treatment of obesity by Sanofi-Aventis starting in... 

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