Role of cannabinoid CB2 receptors in glucose homeostasis in rats

Bermúdez‐Silva, Francisco Javier; Sánchez-Vera, Irene; Suárez, Juan; Serrano, Antonia; Fuentes, Esther; Juan-Picó, Pablo; Nadal, Ángel; Fonseca, Fernando Rodrı́guez de

doi:10.1016/j.ejphar.2007.02.066

Cited by 113 publications

(116 citation statements)

References 12 publications

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“…Given that the CB1 antagonist AM251 has also been reported to be a GPR55 agonist (Lauckner et al 2008), our results also suggest that the increased glucose tolerance previously reported in rats after AM251 treatment (Bermúdez-Silva et al 2006, Bermudez-Silva et al 2007 could be, at least partially, mediated through GPR55. Furthermore, given that Rimonabant has also been reported as being capable of activating the GPR55 receptor (Lauckner et al 2008), some of the beneficial effects on glucose metabolism reported after Rimonabant treatment, that has been attributed to CB1 blocking (Hildebrandt et al 2003), could be mediated, at least partially, through GPR55 activation.…”

Section: Discussionsupporting

confidence: 73%

A role for the putative cannabinoid receptor GPR55 in the islets of Langerhans

Romero-Zerbo¹,

Rafacho²,

Díaz-Arteaga³

et al. 2011

Journal of Endocrinology

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The cannabinoid CB1 receptor is a well-known player in energy homeostasis and its specific antagonism has been used in clinical practice for the treatment of obesity. The G protein-coupled receptor GPR55 has been recently proposed as a new cannabinoid receptor and, by contrast, its pharmacology is still enigmatic and its physiological role is largely unexplored, with no reports investigating its putative role in metabolism. Thus, we aim to investigate in rats the presence, distribution and putative physiological role of GPR55 in a key metabolic tissue, the endocrine pancreas. We found high Gpr55 mRNA content in pancreatic islets and considerable protein distribution in insulin-secreting b-cells. Activation of GPR55 by the agonist O-1602 increased calcium transients (P!0 . 01) and insulin secretion (P!0 . 001) stimulated by glucose. This latter effect was blunted in Gpr55 KO mice suggesting that O-1602 is acting, at least in part, through GPR55. Indeed, acute in vivo experiments showed that GPR55 activation increases glucose tolerance (P!0 . 05) and plasma insulin levels (P!0 . 05), suggesting an in vivo physiological relevance of GPR55 systemic stimulation. Taken together, these results reveal the expression of GPR55 receptors in the endocrine pancreas as well as its function at stimulus-secretion coupling of insulin secretion, suggesting a role in glucose homeostasis. In this context, it may also represent a new target for consideration in the management of type 2 diabetes and related diseases.

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Section: Discussionsupporting

confidence: 73%

A role for the putative cannabinoid receptor GPR55 in the islets of Langerhans

Romero-Zerbo¹,

Rafacho²,

Díaz-Arteaga³

et al. 2011

Journal of Endocrinology

Self Cite

105

100

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“…Moreover, CB1R hyperactivity in adipocytes facilitates fat accumulation and insulin resistance [14]. In cultured pancreatic islets exposure to endocannabinoids increases insulin release [15], suggesting that overactivity of the endocannabinoid system may contribute to the hyperinsulinaemia associated with insulin resistance.…”

Section: Introductionmentioning

confidence: 99%

Deficiency of CB2 cannabinoid receptor in mice improves insulin sensitivity but increases food intake and obesity with age

et al. 2010

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Aims/hypothesis The endocannabinoid system has a key role in energy storage and metabolic disorders. The endocannabinoid receptor 2 (CB2R), which was first detected in immune cells, is present in the main peripheral organs responsible for metabolic control. During obesity, CB2R is involved in the development of adipose tissue inflammation and fatty liver. We examined the long-term effects of CB2R deficiency in glucose metabolism. Methods Mice deficient in CB2R (Cb2 −/− [also known as Cnr2]) were studied at different ages (2-12 months). Twomonth-old Cb2 −/− and wild-type mice were treated with a selective CB2R antagonist or fed a high-fat diet.Results The lack of CB2R in Cb2 −/− mice led to greater increases in food intake and body weight with age than in Cb2 +/+ mice. However, 12-month-old obese Cb2 −/− mice did not develop insulin resistance and showed enhanced insulin-stimulated glucose uptake in skeletal muscle. In agreement, adipose tissue hypertrophy was not associated with inflammation. Similarly, treatment of wild-type mice with CB2R antagonist resulted in improved insulin sensitivity. Moreover, when 2-month-old Cb2 −/− mice were fed a high-fat diet, reduced body weight gain and normal insulin sensitivity were observed. Conclusions/interpretation These results indicate that the lack of CB2R-mediated responses protected mice from both age-related and diet-induced insulin resistance, suggesting that these receptors may be a potential therapeutic target in obesity and insulin resistance.

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“…Inoltre, JWH-133 ha aumentato l'accumulo epatico di trigliceridi in topi DIO (96). I risultati suggeriti da questi studi, sulla resistenza all'insulina indotta nei topi dai CB2, sono contrari al noto effetto nei ratti di sensibilizzazione all'insulina prodotto dagli agonisti CB 2 (91). Sarebbero perciò necessari ulteriori studi per chiarire questa discrepanza.…”

Section: Endocannabinoidi E Fibrosi Epaticaunclassified

Che cosa so di... Il ruolo della Cannabis e dei Cannabinoidi nelle malattie del fegato: review della letteratura

Vivo¹,

Bellinato²,

Marucco³

et al. 2017

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IntroduzioneL'utilizzo della cannabis a scopo terapeutico risale a migliaia di anni prima di Cristo, oggi il suo utilizzo è illegale in quasi tutti i paesi occidentali, ma da anni esiste un forte movimento, attivo soprattutto negli Stati Uniti, a favore della sua reintroduzione anche a scopo ricreativo. Ad oggi, sono 20 Stati e il Distretto di Columbia, ad aver approvato regolamenti che hanno permesso di depenalizzare o legalizzare la produzione e l'uso della cannabis a fini terapeutici. Secondo i dati pubblicati dall'International Narcotics Control Board (Narcotic Drugs: Estimated world requirements for 2015; statistics for 2013), i Paesi produttori di cannabis oltre gli Stati Uniti, sono: Canada, Regno Unito, Olanda, Danimarca, Francia, Romania, Repubblica Ceca e Israele.In Italia con il decreto del 9 novembre 2015, il Ministro della Salute ha rilasciato la concessione delle autorizzazioni per la coltivazione, la produzione, la fabbricazione, l'impiego, il commercio, l'esportazione, l'importazione, il transito, l'acquisto, la vendita e la detenzione delle sostanze stupefacenti o psicotrope prestando particolare attenzione ai medicinali di origine vegetale a base di cannabis. La rimborsabilità a carico del Servizio sanitario regionale prevede che la produzione nazionale di sostanze e preparazioni di origine vegetale a base di cannabis, avvenga presso lo Stabilimento chimico farmaceutico militare di Firenze e sia subordinata alle indicazioni emanate da parte delle Regioni o Province autonome. Le regioni che attualmente hanno approvato l'utilizzo della cannabis a scopo terapeutico sono rappresentate da: Puglia, Toscana, Veneto, Liguria, Marche, Friuli Venezia Giulia, Abruzzo, Sicilia, Umbria, Basilicata, Emilia Romagna, Piemonte e Valle D'Aosta. La prescrizione medica di questi preparati non deve essere considerata una terapia propriamente detta, bensì un trattamento sintomatico di supporto ai trattamenti standard, quando questi ultimi non hanno prodotto gli effetti desiderati, hanno provocato effetti secondari non tollerabili, o necessitano di incrementi posologici che potrebbero determinare la comparsa di effetti collaterali . Mission 46.......................................................................................................................................................................................................... SummaryIn many States of USA and some Italian regions, marijuana has been legalized as medical drug. So, a process of cannabis decriminalization is in place throughout the West. The debate about cannabis goes on politically and socially with contrasting aspects. Both as regards the recreational use, it should be recalled that is considered harmful (to a different extent) by virtually all the experts; both in terms of therapeutic use, considered promising by many researchers, but for which the results really sure still seem limited to a few ambit. This paper provides a review to groped to shed light on this topic both on the legal peculiarities and medical prescribing, and espe...

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Role of cannabinoid CB2 receptors in glucose homeostasis in rats

Cited by 113 publications

References 12 publications

A role for the putative cannabinoid receptor GPR55 in the islets of Langerhans

A role for the putative cannabinoid receptor GPR55 in the islets of Langerhans

Deficiency of CB2 cannabinoid receptor in mice improves insulin sensitivity but increases food intake and obesity with age

Che cosa so di... Il ruolo della Cannabis e dei Cannabinoidi nelle malattie del fegato: review della letteratura

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