I.URB597 basic Characters:
|Purity :||≥99% (HPLC)|
|Synonyms:||N-Cyclohexylcarbamic acid 3′-(aminocarbonyl)[1,1′-biphenyl]-3-yl ester;3′-CarbaMoyl-[1,1′-biphenyl]-3-yl cyclohexylcarbaMate;3-(3-carbaMoylphenyl)phenyl N-cyclohexylcarbaMate;CarbaMic acid,N-cyclohexyl-, 3′-(aMinocarbonyl)[1,1′-biphenyl]-3-yl ester;KDS 4103 N-Cyclohexylcarbamic acid 3′-(aminocarbonyl)[1,1′-biphenyl]-3-yl ester;N-Cyclohexylcarbamic acid 3′-(aminocarbonyl)[1,1′-biphenyl]-3-yl ester URB 597 KDS 4103;URB 597, >=98%;APD597(URB597)|
|Alpha:||D +5° (c = 0.437 in chloroform)|
|Solubility DMSO:||soluble2mg/mL, clear (warmed)|
II. URB597 usage in cycle:
2.How is the work for URB597?
Rationale: A major clinical concern with the use of cannabinoid receptor 1 (CB1) direct agonists is that these compounds increase alcohol drinking and drug abuse-related behaviours. As an alternative approach, CB1-receptor-mediated activity can be facilitated by increasing anandamide levels with the use of hydrolase fatty acid amide hydrolase (FAAH) inhibitors. Objective: Using the selective FAAH inhibitor URB597, we investigated whether activation of the endogenous cannabinoid tone increases alcohol abuse liability, as what happens with the CB1 receptor direct agonists. Materials and methods: URB597 was tested on alcohol self-administration in Wistar rats and on homecage alcohol drinking in genetically selected Marchigian Sardinian alcohol-preferring (msP) rats. In Wistar rats, URB597 effects on alcohol-induced anxiety and on stress-, yohimbine- and cue-induced reinstatement of alcohol seeking were also evaluated. For comparison, the effect of the CB1 receptor antagonist rimonabant on ethanol self-administration was also tested. Results: Under our experimental condition, intraperitoneal (IP) administration of URB597 (0.0, 0.3 and 1.0 mg/kg) neither increased voluntary homecage alcohol drinking in msP rats nor facilitated fixed ratio 1 and progressive ratio alcohol self-administration in nonselected Wistars. In the reinstatement tests, the compound did not have effects on cue-, footshock stress- and yohimbine-induced relapse. Conversely, URB597 completely abolished the anxiogenic response measured during withdrawal after an acute IP administration of alcohol (3.0 g/kg). Rimonabant (0.0, 0.3, 1.0 and 3.0 mg/kg) significantly reduced ethanol self-administration. Conclusions: Results demonstrate that activation of the endocannabinoid anandamide system by selective inhibition of FAAH does not increase alcohol abuse risks but does reduce anxiety associated to alcohol withdrawal. We thus can speculate that medication based on the use of endocannabinoid system modulators such as URB597 may offer important advantages compared to treatment with direct CB1 receptor activators.
3.Is effect URB597?
The effects of URB 597 alone and in combination with anandamide were investigated in one group of monkeys (n= 4) that discriminated Δ9‐THC (0.1 mg·kg−1 i.v.) from vehicle, and in another group (n= 5) receiving chronic Δ9‐THC (1 mg·kg−112 h−1 s.c.) that discriminated the cannabinoid antagonist rimonabant (1 mg·kg−1 i.v.).
URB 597 enhanced the behavioural effects of anandamide but not other CB1 agonists. However, URB 597 did not significantly enhance the attenuation of Δ9‐THC withdrawal induced by anandamide. Collectively, these data suggest that endogenous anandamide in primate brain does not readily mimic the behavioural effects of exogenously administered anandamide.
Potent and selective fatty acid amide hydrolase (FAAH) inhibitor (IC50 values are 3 and 5 nM in human liver and rat brain, respectively). Exhibits no significant inhibitory activity against a variety of receptors, ion channels and enzymes, including human cannabinoid receptors and rat monoacylglycerol lipase. Displays antiallodynic and antihyperalgesic activity in an inflammatory pain model. In vitro, KDS-4103 inhibits FAAH activity with median inhibitory concentrations (IC(50)) of 5 nM in rat brain membranes and 3 nM in human liver microsomes. In vivo, KDS-4103 inhibits rat brain FAAH activity after intraperitoneal (i.p.) administration with a median inhibitory dose (ID(50)) of 0.15 mg/kg. The compound does not significantly interact with other cannabinoid-related targets, including cannabinoid receptors and anandamide transport, or with a broad panel of receptors, ion channels, transporters and enzymes. By i.p. administration to rats and mice KDS-4103 elicits significant, anxiolytic-like, antidepressant-like and analgesic effects, which are prevented by treatment with CB1 receptor antagonists. By contrast, at doses that significantly inhibit FAAH activity and substantially raise brain anandamide levels, KDS-4103 does not evoke classical cannabinoid-like effects (e.g., catalepsy, hypothermia, hyperphagia), does not cause place preference, and does not produce generalization to the discriminative effects of the active ingredient of cannabis, Delta9-tetrahydrocannabinol (Delta9-THC). These findings suggest that KDS-4103 acts by enhancing the tonic actions of anandamide on a subset of CB(1) receptors, which may normally be engaged in controlling emotions and pain. KDS-4103 is orally available in rats and cynomolgus monkeys. Sub-chronic repeated dose studies (1,500 mg/kg, per os) in these two species have not demonstrated systemic toxicity. Likewise, no toxicity was noted in bacterial cytotoxicity tests in vitro and in the Ames test. Furthermore, no deficits were observed in rats on the rotarod test after acute i.p. treatment with KDS-4103 at doses up to 5 mg/kg or in a functional observation battery after oral doses up to 1,500 mg/kg. The results suggest that KDS-4103 will offer a novel approach with a favorable therapeutic window for the treatment of anxiety, depression and pain.
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6. URB597 Recipes:
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7. URB597 Marketing:
To be provided in the coming future.
III. URB597 HNMR
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