(S)-4-(4-((2-(3,5-diMethylphenyl)pyrrolidin-1-yl)Methyl)phenoxy)-3-fluorobenzaMide
(S)-4-(4-((2-(3,5-diMethylphenyl)pyrrolidin-1-yl)Methyl)phenoxy)-3-fluorobenzaMide Basic information
- Product Name:
- (S)-4-(4-((2-(3,5-diMethylphenyl)pyrrolidin-1-yl)Methyl)phenoxy)-3-fluorobenzaMide
- Synonyms:
-
- (S)-4-(4-((2-(3,5-diMethylphenyl)pyrrolidin-1-yl)Methyl)phenoxy)-3-fluorobenzaMide
- LY2456302
- LY2456302;LY 2456302;CERC501;CERC 501
- CS-2732
- CERC-501(LY-2456302,Aticaprant)
- Aticaprant
- Benzamide, 4-[4-[[(2S)-2-(3,5-dimethylphenyl)-1-pyrrolidinyl]methyl]phenoxy]-3-fluoro-
- 4-[4-[[(2S)-2-(3,5-Dimethylphenyl)-1-pyrrolidinyl]methyl]phenoxy]-3-fluorobenzamide
- CAS:
- 1174130-61-0
- MF:
- C26H27FN2O2
- MW:
- 418.5
- Mol File:
- 1174130-61-0.mol
(S)-4-(4-((2-(3,5-diMethylphenyl)pyrrolidin-1-yl)Methyl)phenoxy)-3-fluorobenzaMide Chemical Properties
- Boiling point:
- 519.2±50.0 °C(Predicted)
- Density
- 1.201±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMF: 1 mg/ml; DMSO: 5 mg/ml; Ethanol: 3 mg/ml; PBS (pH 7.2): insol
- form
- A solid
- pka
- 15.61±0.50(Predicted)
- color
- White to off-white
(S)-4-(4-((2-(3,5-diMethylphenyl)pyrrolidin-1-yl)Methyl)phenoxy)-3-fluorobenzaMide Usage And Synthesis
Uses
Aticaprant is a κ-?opioid receptor agonist which may be used in the treatment of neurological diseases and disorders such as Alzheimer''s disease.
in vivo
Aticaprant (CERC-501) has a rapid absorption (tmax=1-2 h) and good oral bioavailability (F=25%). Oral Aticaprant (CERC-501) administration selectively and potently occupies central kappa opioid receptors (ED50=0.33 mg/kg), without evidence of mu or delta receptor occupancy. LY2456302 potently blocks kappa-agonist-mediated analgesia and disruption of prepulse inhibition, without affecting mu-agonist-mediated effects at doses >30-fold higher. Aticaprant (CERC-501) produces antidepressant-like effects in the mouse forced swim test and enhances the effects of imipramine and citalopram. Aticaprant (CERC-501) reduces ethanol self-administration in alcohol-preferring rats[1]. Aticaprant (CERC-501) alleviates the nicotine withdrawal syndrome, as evidenced by decreased expression of nicotine withdrawal induced anxiety-related behavior, somatic signs, and CPA, and increased hotplate latency in nicotine withdrawn mice following pre-treatment[2].
(S)-4-(4-((2-(3,5-diMethylphenyl)pyrrolidin-1-yl)Methyl)phenoxy)-3-fluorobenzaMideSupplier
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(S)-4-(4-((2-(3,5-diMethylphenyl)pyrrolidin-1-yl)Methyl)phenoxy)-3-fluorobenzaMide(1174130-61-0)Related Product Information
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