AM251 - CAS 183232-66-8
Catalog number: 183232-66-8
Category: Inhibitor
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Cannabinoid Receptor
AM251 block the inhibitory effects of endocannabinoids and synthetic cannabinoid agonists on transmitter release through an action at presynaptic cannabinoid 1 receptors in brain.
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1.Cannabinoids Regulate the Diameter of Pericyte-Containing Retinal Capillaries in Rats.
Zong Y;Zhou X;Cheng J;Yu J;Wu J;Jiang C Cell Physiol Biochem. 2017;43(5):2088-2101. doi: 10.1159/000484193. Epub 2017 Oct 23.
BACKGROUND/AIMS: ;Cannabinoids are vasoactive substances that act as key regulators of arterial tone in the blood vessels supplying peripheral tissues and the central nervous system. We therefore investigated the effect of cannabinoids on retinal capillaries and pericytes.;METHODS: ;The effects of cannabinoids on capillary diameters were determined using an ex vivo whole-mount rat retinal model. Western blotting, quantitative PCR, and immunohistochemistry were performed to explore the underlying mechanism.;RESULTS: ;Endogenous cannabinoid 2-arachidonoylglycerol and anandamide and exogenous cannabinoid (R-(+)-WIN55212-2) dilated the noradrenaline-precontracted capillaries in a concentration-dependent manner (1 µM to 0.1 mM). The extent of vasorelaxation was positively correlated with changes in pericyte width. The effects of R-(+)-WIN55212-2 on vasorelaxation and pericyte width were inhibited by a cannabinoid receptor type-1 (CB1) antagonist, AM251 or rimonabant (SR141716A), the nitric oxide synthase inhibitor l-NAME, and the guanylate cyclase inhibitor ODQ. They were also abolished by the removal of the endothelium, but not by the cannabinoid receptor-2 antagonist SR144528, the endothelial cannabinoid receptor antagonist O-1918, or the cyclooxygenase inhibitor indomethacin.
2.Anxiolytic-like effect of cannabinoids injected into the rat dorsolateral periaqueductal gray.
Moreira FA;Aguiar DC;Guimarães FS Neuropharmacology. 2007 Mar;52(3):958-65. Epub 2006 Dec 5.
Contradictory results exist concerning the effects of systemic injections of CB(1) cannabinoid receptor agonists on anxiety-related behaviors. Direct drug administration into brain structures related to aversive responses can potentially help to clarify the role of cannabinoids on anxiety. One such structure is the midbrain dorsolateral periaqueductal gray (dlPAG). Therefore, the aim of this study was to test the hypothesis that the activation of the CB(1) receptor in the dlPAG would attenuate anxiety-related behaviors. Male Wistar rats with cannula aimed at the dlPAG received injections of the endogenous cannabinoid anandamide, the anandamide transport inhibitor AM404, the anandamide analogue ACEA or the CB(1) receptor antagonist AM251, and were submitted to the elevated plus maze (EPM), an animal model of anxiety. Anandamide (0.5-50pmol) and ACEA (0.05-5pmol) induced anxiolytic-like effects with bell-shaped dose-response curves, the higher doses being ineffective. The anandamide anxiolytic effect was potentiated by AM404 (50pmol) and prevented by AM251 (100pmol). Neither AM404 (0.5-50pmol) nor AM251 (1-100pmol) alone modified the animal behavior in the EPM. The present study suggests that the dlPAG is a possible neuroanatomical site for anxiolytic-like effects mediated by CB(1) agonists.
3.Role of the endocannabinoid system in ethanol-induced inhibition of salivary secretion.
Prestifilippo JP;Fernández-Solari J;Medina V;Rettori V;Elverdin JC Alcohol Alcohol. 2009 Sep-Oct;44(5):443-8. doi: 10.1093/alcalc/agp040. Epub 2009 Jul 9.
AIM: ;The aim of the present study was to determine whether the endocannabinoid system could be involved in the ethanol-induced inhibition of salivation in adult male Wistar rats.;METHODS: ;Salivary secretion induced by different concentrations of methacholine, a cholinergic agonist, and the endocannabinoid arachidonoyl ethanolamide (anandamide, AEA) production in the submandibular gland (SMG) were determined in rats after ethanol (3 g/kg) administration by gastric gavage. To study the participation of cannabinod receptors in ethanol action, we evaluated methacholine-induced salivary secretion after ethanol administration when CB1 or CB2 receptors were blocked by intra-SMG injections of their selective antagonists AM251 and AM630, respectively. Additionally, we evaluated the in vitro effect of ethanol (0.1 M) on SMG production of cAMP, alone or combined with AM251 or AM630.;RESULTS: ;Acute ethanol administration increased AEA production in SMG and also inhibited the methacholine-induced saliva secretion that was partially restored by intraglandular injection of AM251 or AM630. In addition, ethanol significantly reduced the forskolin-induced increase in cAMP content in SMG in vitro while treatment with AM251 blocked this response.
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CAS 183232-66-8 AM251

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