Biochemistry and pharmacology of endovanilloids

Starowicz, Katarzyna; Nigam, Santosh; Marzo, Vincenzo Di

doi:10.1016/j.pharmthera.2007.01.005

Cited by 348 publications

(280 citation statements)

References 229 publications

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“…We also tested the effects of the endocannabinoid AEA, which, like NADA, activates CBRs and TRPV1 (6,49). However, AEA is a less potent TRPV1 agonist than NADA (36).…”

Section: Nada's Anti-inflammatory Activity In Vivo Requires Trpv1mentioning

confidence: 99%

N-Arachidonoyl Dopamine Modulates Acute Systemic Inflammation via Nonhematopoietic TRPV1

Lawton

Tran

et al. 2017

The Journal of Immunology

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N-Arachidonoyl dopamine (NADA) is an endogenous lipid that potently activates the transient receptor potential vanilloid 1 (TRPV1), which mediates pain and thermosensation. NADA is also an agonist of cannabinoid receptors 1 and 2. We have reported that NADA reduces the activation of cultured human endothelial cells by LPS and TNF-α. Thus far, in vivo studies using NADA have focused on its neurologic and behavioral roles. In this article, we show that NADA potently decreases in vivo systemic inflammatory responses and levels of the coagulation intermediary plasminogen activator inhibitor 1 in three mouse models of inflammation: LPS, bacterial lipopeptide, and polymicrobial intra-abdominal sepsis. We also found that the administration of NADA increases survival in endotoxemic mice. Additionally, NADA reduces blood levels of the neuropeptide calcitonin gene-related peptide but increases the neuropeptide substance P in LPS-treated mice. We demonstrate that the anti-inflammatory effects of NADA are mediated by TRPV1 expressed by nonhematopoietic cells and provide data suggesting that neuronal TRPV1 may mediate NADA’s anti-inflammatory effects. These results indicate that NADA has novel TRPV1-dependent anti-inflammatory properties and suggest that the endovanilloid system might be targeted therapeutically in acute inflammation.

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“…We also tested the effects of the endocannabinoid AEA, which, like NADA, activates CBRs and TRPV1 (6,49). However, AEA is a less potent TRPV1 agonist than NADA (36).…”

Section: Nada's Anti-inflammatory Activity In Vivo Requires Trpv1mentioning

confidence: 99%

N-Arachidonoyl Dopamine Modulates Acute Systemic Inflammation via Nonhematopoietic TRPV1

Lawton

Tran

et al. 2017

The Journal of Immunology

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“…AEA acts as a partial agonist for the cannabinoid receptors, being more selective for CB1 [25]. However, it also binds to the transient receptor potential cation channel subfamily V member 1 (TRPV1) or type-1 vanilloid receptor [26,27]. It is metabolized, after cellular uptake by EMT, inside the cell to ethanolamine and arachidonic acid (AA) by fatty acid amide hydrolase (FAAH) which is membrane bound [28].…”

Section: The Endocannabinoidsmentioning

confidence: 99%

Marijuana, phytocannabinoids, the endocannabinoid system, and male fertility

Plessis

Agarwal

Syriac

2015

J Assist Reprod Genet

127

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Marijuana has the highest consumption rate among all of the illicit drugs used in the USA, and its popularity as both a recreational and medicinal drug is increasing especially among men of reproductive age. Male factor infertility is on the increase, and the exposure to the cannabinoid compounds released by marijuana could be a contributing cause. The endocannabinoid system (ECS) is deeply involved in the complex regulation of male reproduction through the endogenous release of endocannabinoids and binding to cannabinoid receptors. Disturbing the delicate balance of the ECS due to marijuana use can negatively impact reproductive potential. Various in vivo and in vitro studies have reported on the empirical role that marijuana plays in disrupting the hypothalamus-pituitary-gonadal axis, spermatogenesis, and sperm function such as motility, capacitation, and the acrosome reaction. In this review, we highlight the latest evidence regarding the effect of marijuana use on male fertility and also provide a detailed insight into the ECS and its significance in the male reproductive system.

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“…These proteins, together with the ECs and the type 1 and 2 cannabinoid receptors (CB 1 and CB 2 ), constitute the EC system. Since anandamide, but not 2-AG, is also an agonist of transient receptor vanilloid type-1 (TRPV1) [7], some authors consider this unselective cation channel to be part of the EC system. Anandamide and that part of 2-AG that acts as an endocannabinoid (2-AG is also an intermediate in triacylglycerol and phospholipid metabolism) are released from cells immediately after their production (i.e.…”

Section: Introductionmentioning

confidence: 99%

The endocannabinoid system in obesity and type 2 diabetes

2008

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Endocannabinoids (ECs) are defined as endogenous agonists of cannabinoid receptors type 1 and 2 (CB 1 and CB 2 ). ECs, EC anabolic and catabolic enzymes and cannabinoid receptors constitute the EC signalling system. This system participates in the control of lipid and glucose metabolism at several levels, with the possible endpoint of the accumulation of energy as fat. Following unbalanced energy intake, however, the EC system becomes dysregulated, and in most cases overactive, in several organs participating in energy homeostasis, particularly, in intraabdominal adipose tissue. This dysregulation might contribute to excessive visceral fat accumulation and reduced adiponectin release from this tissue, and to the onset of several cardiometabolic risk factors that are associated with obesity and type 2 diabetes. This phenomenon might form the basis of the mechanism of action of CB 1 antagonists/ inverse agonists, recently developed by several pharmaceutical companies as adjuvants to lifestyle modification for weight reduction, glycaemic control and dyslipidaemia in obese and type 2 diabetes patients. It also helps to explain why some of the beneficial actions of these new therapeutics appear to be partly independent from weight loss.

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Biochemistry and pharmacology of endovanilloids

Cited by 348 publications

References 229 publications

N-Arachidonoyl Dopamine Modulates Acute Systemic Inflammation via Nonhematopoietic TRPV1

N-Arachidonoyl Dopamine Modulates Acute Systemic Inflammation via Nonhematopoietic TRPV1

Marijuana, phytocannabinoids, the endocannabinoid system, and male fertility

The endocannabinoid system in obesity and type 2 diabetes

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