Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UNIPROT:P21554 (cannabinoid receptor)
 3,582 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Type 1 cannabinoid receptor (CB1) antagonists might be useful for treating obesity, liver disease, metabolic syndrome, and dyslipidemias. Unfortunately, inhibition of CB1 in the central nervous system (CNS) produces adverse effects, including depression, anxiety and suicidal ideation in some patients, which led to withdrawal of the pyrazole inverse agonist rimonabant (SR141716A) from European markets. Efforts are underway to produce peripherally selective CB1 antagonists to circumvent CNS-associated adverse effects. In this study, novel analogs of rimonabant (1) were explored in which the 1-aminopiperidine group was switched to a 4-aminopiperidine, attached at the 4-amino position (5). The piperidine nitrogen was functionalized with carbamates, amides, and sulfonamides, providing compounds that are potent inverse agonists of hCB1 with good selectivity for hCB1 over hCB2. Select compounds were further studied using in vitro models of brain penetration, oral absorption and metabolic stability. Several compounds were identified with predicted minimal brain penetration and good metabolic stability. In vivo pharmacokinetic testing revealed that inverse agonist 8c is orally bioavailable and has vastly reduced brain penetration compared to rimonabant.
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PMID:Pyrazole antagonists of the CB1 receptor with reduced brain penetration. 2682 37

Synthetic cannabinoids are a group of new psychoactive compounds (NPS) that act as agonists at the cannabinoid receptor. First reported in 2008, they currently represent one of the largest groups of NPS that are monitored by the European Monitoring Centre for Drugs and Drug Addiction (EMCDDA). Five samples (4 from the European RESPONSE project and one from daily casework) containing different synthetic cannabinoids were analyzed by a complex of analytical methods including gas chromatography-electron ionization mass spectrometry (GC-EI-MS), liquid chromatography-high resolution mass spectrometry (LC-HRMS), infrared spectroscopy (IR) and nuclear magnetic resonance spectroscopy (NMR). Five new synthetic cannabinoids containing a cumyl moiety as a linked group were identified: CUMYL-PINACA, 5F-CUMYL-PINACA, CUMYL-4CN-BINACA, 5F-CUMYL-P7AICA, CUMYL-4CN-B7AICA. 5F-CUMYL-PINACA and 5F-CUMYL-P7AICA as well as CUMYL-4CN-BINACA and CUMYL-4CN-B7AICA are constitutional isomers and only differ in the position of a nitrogen atom. The article contains all analytical data for a proper identification and differentiation of the five cumyl compounds.
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PMID:Structural characterization of the new synthetic cannabinoids CUMYL-PINACA, 5F-CUMYL-PINACA, CUMYL-4CN-BINACA, 5F-CUMYL-P7AICA and CUMYL-4CN-B7AICA. 2912 90


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