Having gained chemical understanding at molecular level, chemistry graduates may choose to apply this knowledge in almost unlimited ways, as it can be used to analyze all matter and therefore our entire environment. Like 7779-30-8, Name is 1-(2,6,6-Trimethylcyclohex-2-en-1-yl)pent-1-en-3-one. In a document, author is Ford, Benjamin M., introducing its new discovery. Application of 7779-30-8.
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.
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Reference:
Quinuclidine – Wikipedia,
,Quinuclidine | C7H13N | ChemSpider