N-PIPERIDINYL-[8-CHLORO-1-(2,4-DICHLOROPHENYL)-1,4,5,6-TETRAHYDROBENZO-[6,7]CYCLOHEPTAL[1,2-C]PYRAZOLE-3-CARBOXAMIDE Struktur

N-PIPERIDINYL-[8-CHLORO-1-(2,4-DICHLOROPHENYL)-1,4,5,6-TETRAHYDROBENZO-[6,7]CYCLOHEPTAL[1,2-C]PYRAZOLE-3-CARBOXAMIDE

Bezeichnung:N-PIPERIDINYL-[8-CHLORO-1-(2,4-DICHLOROPHENYL)-1,4,5,6-TETRAHYDROBENZO-[6,7]CYCLOHEPTAL[1,2-C]PYRAZOLE-3-CARBOXAMIDE

CAS-Nr494844-07-4

Englisch Name:N-PIPERIDINYL-[8-CHLORO-1-(2,4-DICHLOROPHENYL)-1,4,5,6-TETRAHYDROBENZO-[6,7]CYCLOHEPTAL[1,2-C]PYRAZOLE-3-CARBOXAMIDE

CBNumberCB9825071

SummenformelC24H23Cl3N4O

Molgewicht489.82

MOL-Datei494844-07-4.mol

N-PIPERIDINYL-[8-CHLORO-1-(2,4-DICHLOROPHENYL)-1,4,5,6-TETRAHYDROBENZO-[6,7]CYCLOHEPTAL[1,2-C]PYRAZOLE-3-CARBOXAMIDE physikalisch-chemischer Eigenschaften

storage temp.	Store at -20°C
Löslichkeit	≤0.25mg/ml in ethanol;0.25mg/ml in DMSO;0.5mg/ml in dimethyl formamide
Aggregatzustand	crystalline solid
Farbe	White to off-white

N-PIPERIDINYL-[8-CHLORO-1-(2,4-DICHLOROPHENYL)-1,4,5,6-TETRAHYDROBENZO-[6,7]CYCLOHEPTAL[1,2-C]PYRAZOLE-3-CARBOXAMIDE Chemische Eigenschaften,Einsatz,Produktion Methoden

Verwenden
NESS 0327 is a potent, selective CB1 receptor antagonist. Synthetic Cannabinoids
Biologische Aktivität
ki: 0.35 pm and 21 nm for cb1 and cb2 receptor, respectively.ness 0327 is an extremely potent cannabinoid (cb) receptor antagonist.cannabinoid cb1 receptors are present in the central nervous system with the highest densities in the hippocampus, and to a lesser extent in some peripheral tissues. cannabinoid cb2 receptors are predominantly located in peripheral tissues. both receptors can negatively regulate adenylate cyclase and control the release of arachidonic acid.
in vitro
previous study found that ness 0327 exhibited a stronger selectivity for cb1 receptor compared with sr 141716a, showing a much higher affinity for cb1 receptor and a higher affinity for the cb2 receptor. affinity ratios demonstrated that ness 0327 was more than 60,000-fold selective for the cb1 receptor. ness 0327 alone did not produce concentration-dependent stimulation of guanosine 5'-o-(3-[35s]thio)-triphosphate binding in rat cerebella membranes. conversely, ness 0327 antagonized win 55,212-2-stimulated guanosine 5'-o-(3-[35s]thio)-triphosphate binding. in functional assay, ness 0327 could antagonize the inhibitory effects of win 55,212-2 on electrically evoked contractions in mouse isolated vas deferens preparations [1].
in vivo
in vivo studies showed that ness 0327 could antagonize the antinociceptive effect produced by win 55,212-2 in both tail-flick and hot-plate test, suggesting that ness 0327 was a novel cannabinoid antagonist with high selectivity for the cannabinoid cb1 receptor [1].
Lager
Store at -20°C
Einzelnachweise
[1] ruiu, s. ,pinna, g.a.,marchese, g., et al. synthesis and characterization of ness 0327: a novel putative antagonist of the cb1 cannabinoid receptor. journal of pharmacology and experimental therapeutics 306(1), 363-370 (2003).

N-PIPERIDINYL-[8-CHLORO-1-(2,4-DICHLOROPHENYL)-1,4,5,6-TETRAHYDROBENZO-[6,7]CYCLOHEPTAL[1,2-C]PYRAZOLE-3-CARBOXAMIDE Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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