You could be based in a university, combining chemical research with teaching; or in a public-sector research center, helping to ensure national healthcare provision keeps pace with new discoveries. Like 584-02-1, Name is 3-Pentanol. In a document, author is Ford, Benjamin M., introducing its new discovery. Computed Properties of https://www.ambeed.com/products/584-02-1.html.
Most cannabinoid 1 receptor (CB1R) agonists will signal through both G protein-dependent and -independent pathways in an unbiased manner. Recruitment of beta-arrestin 2 desensitizes and internalizes receptors, producing tolerance that limits therapeutic utility of cannabinoids for chronic conditions. We developed the indole quinuclidinone (IQD) analog (Z)-2-((1-(4-fluorobenzyl)1H-indol-3-yl)nnethylene)quinuclidin-3-one (PNR-4-20) as a novel G protein-biased agonist at CB(1)Rs, and the present studies determine if repeated administration of PNR-4-20 produces lesser tolerance to in vivo effects compared with unbiased CB1R agonists, Delta(9)-tetrahydrocannabinol (Delta(9)-THC) and 1-pentyl-3-(1-naphthoyl)indole (JWH-018). Adult male National Institutes of Health Swiss mice were administered comparable doses of PNR-4-20 (100 mg/kg), Delta(9)-THC (30 mg/kg), or JWH-018 (3 mg/kg) once per day for five consecutive days to determine tolerance development to hypothermic, antinociceptive, and cataleptic effects. Persistence of tolerance was then determined after a drug abstinence period. We found that unbiased CB1R agonists Delta(9)-THC and JWH-018 produced similar tolerance to these effects, but lesser tolerance was observed with PNR-4-20 for hypothermic and cataleptic effects. Tolerance to the effects of PNR-4-20 completely recovered after drug abstinence, while residual tolerance was always observed with unbiased CB1R agonists. Repeated treatment with PNR-4-20 and Delta(9)-THC produced asymmetric cross-tolerance to hypothermic effects. Importantly, binding studies suggest PNR-4-20 produced significantly less down-regulation of CB(1)Rs relative to Delta(9)-THC in hypothalamus and thalamus of chronically treated mice. These studies suggest that the G protein-biased CB1R agonist PNR-4-20 produces significantly less tolerance than unbiased cannabinoid agonists, and that the IQD analogs should be investigated further as a novel molecular scaffold for development of new therapeutics.
The reactant in an enzyme-catalyzed reaction is called a substrate. Enzyme inhibitors cause a decrease in the reaction rate of an enzyme-catalyzed reaction.Interested yet? Keep reading other articles of 584-02-1, you can contact me at any time and look forward to more communication. Computed Properties of https://www.ambeed.com/products/584-02-1.html.
Reference:
Quinuclidine – Wikipedia,
,Quinuclidine | C7H13N | ChemSpider