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BOC Sciences
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Product Name:Drinabant
CAS:358970-97-5
Purity:≥98% Remarks:Drinabant is a highly potent, selective antagonist for the CB1 receptor with Ki values of 0.16-0.44 nM.
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| Company Name: |
ChemeGen(Shanghai) Biotechnology Co.,Ltd.
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18818260767 |
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| Products Intro: |
Product Name:AVE-1625
CAS:358970-97-5
Purity:98% Package:10 mg;50 mg;100 mg;500 mg;1 g;5 g;10 g
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| | Drinabant Basic information |
| Product Name: | Drinabant | | Synonyms: | drinabant;N-[1-[Bis(4-chlorophenyl)methyl]azetidin-3-yl]-N-(3,5-difluorophenyl)methanesulfonamide;AVE-1625;Methanesulfonamide, N-[1-[bis(4-chlorophenyl)methyl]-3-azetidinyl]-N-(3,5-difluorophenyl)- | | CAS: | 358970-97-5 | | MF: | C23H20Cl2F2N2O2S | | MW: | 497.38 | | EINECS: | | | Product Categories: | | | Mol File: | 358970-97-5.mol |  |
| | Drinabant Chemical Properties |
| Boiling point | 581.7±60.0 °C(Predicted) | | density | 1.458 | | storage temp. | Store at -20°C | | solubility | ≤0.15mg/ml in ethanol;15mg/ml in DMSO;15mg/ml in dimethyl formamide | | form | crystalline solid | | pka | 5.44±0.10(Predicted) | | color | White to off-white |
| | Drinabant Usage And Synthesis |
| Description | The central cannabinoid (CB1) receptor is a G protein-coupled receptor that is widely distributed in the central nervous system and several peripheral tissues and binds the active component of cannabis, Δ9-tetrahydrocannabinol. Signaling through the CB1 receptor is implicated in attentional and working memory deficits as well as obesity. AVE-1625 is a highly potent, selective antagonist for the CB1 receptor with Ki values of 0.16-0.44 nM. At 1-3 mg/kg, AVE-1625 significantly improves the performance of rodents in working memory tasks. At 30 mg/kg, AVE-1625 reduces caloric intake by more than 50% of controls and significantly increases lipolysis from fat tissues and reduces hepatic glycogen levels in rodents. | | Uses | AVE-1625 is a selective antagonist for the CB1 receptor. | | in vivo | AVE1625 (10 mg/kg orally once daily), combined with Olanzapine (HY-14541) attenuates body weight gain, diminishing the enhanced food intake while maintaining increased energy expenditure and decreased motility[2].
AVE1625 (1, 3, and 10 mg/kg ip), reverses abnormally persistent LI induced by MK-801 (HY-15084B) or neonatal nitric oxide synthase inhibition in rodents, and improves both working and episodic memory[3].
| Animal Model: | Rats[1]. | | Dosage: | 30 mg/kg. | | Administration: | Oral gavage, single dose. | | Result: | Had free access to food during the preceding night (postprandial state) caused a pronounced reduction of food intake during the subsequent 10-12 h without differences in
their locomotor activity relative to that of the control group.
Caused an increase in FFA and glycerol, indicating increased lipolysis from fat tissue.
Immediately resulted in a pronounced increase in VCO2 and VO2, indicating increased oxidation of energetic substrates and increased TEE.
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| Animal Model: | Female Hanover Wistar rats weighing 225 ± 8.6 g[2]. | | Dosage: | 10 mg/kg. | | Administration: | Orally once daily. | | Result: | Reduced their weight markedly within the first 3 days of treatment where upon animals maintained lower body weight, although they lost about 7.3 ± 1.3 g fat during the 12 days of treatment.
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| | IC 50 | hCB1-R: 25 nM (IC50); rCB1-R: 10 nM (IC50); CB2: 10000 nM (IC50) | | storage | Store at -20°C | | references | [1] borowsky b, stevens r, mark b, et al. ave1625, a cannabinoid cbi antagonist, as a co-treatment for schizophrenia: improvement in cognitive function and reduction of antipsychotic-side effects in animal models[c]//neuropsychopharmacology. macmillan building, 4 crinan st, london n1 9xw, england: nature publishing group, 2005, 30: s116-s117.
[2] herkenham m, lynn a b, little m d, et al. cannabinoid receptor localization in brain[j]. proceedings of the national academy of sciences, 1990, 87(5): 1932-1936.
[3] herling a w, gossel m, haschke g, et al. cb1 receptor antagonist ave1625 affects primarily metabolic parameters independently of reduced food intake in wistar rats[j]. american journal of physiology-endocrinology and metabolism, 2007, 293(3): e826-e832. |
| | Drinabant Preparation Products And Raw materials |
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