Nemifitide
Nemifitide (INN 00835) is a 5-HT2A receptor ligand that crosses the blood-brain barrier. Nemifitide is used in research related to major depressive disorder.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- CAS No.: 173240-15-8
- Formule: C33H43FN10O6
- Masse moléculaire:694.77
-
Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Activité biologique
-
Chemical Information
- Pureté et documentation
- Références
-
Help & FAQs
Voir tous les produits spécifiques à Isoform 5-HT Receptor
More
Activité biologique
Description
|
5-HT2A Receptor |
In Vitro
Nemifitide (INN 00835) and its active metabolite (M1) bind to 5-HT2A, 5-HT2C, melanocortin MC4, MC5, and bombesin receptors at micromolar concentrations in cell-free biochemical assays[1].
Nemifitide binds to 5-HT2A, 5-HT2C, NPY1, MC4, MC5, and bombesin receptors in cell-free biochemical assays[2].
Nemifitide undergoes extensive metabolism in rat and human intestinal and liver enzyme preparations in vitro[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Nemifitide (0.3 mg/kg; i.p.; daily; 5 days) produces a rapid-onset antidepressant-like effect in male FSL rats, significantly increasing forced swim test swimming time after just 5 days of daily intraperitoneal administration of 0.3 mg/kg[2].
Nemifitide (0.3 mg/kg; i.p.; daily; 14 days) produces prolonged antidepressant-like effects in male FSL rats, with significantly increased forced swim test swimming time persisting for at least 5 days after cessation of 14 days of daily intraperitoneal administration of 0.3 mg/kg[2].
Nemifitide (0.3 mg/kg; i.p.; daily; 14 days) does not produce antidepressant-like effects in male FRL control rats, as 14 days of daily intraperitoneal administration of 0.3 mg/kg does not significantly increase forced swim test swimming time[2].
Nemifitide (0.3 mg/kg; i.p.; daily; 14 days) produces antidepressant-like effects in male HDS and LDS rats, significantly increasing forced swim test swimming time after 14 days of daily intraperitoneal administration of 0.3 mg/kg[2].
Nemifitide (0.3 mg/kg; i.p.; daily; 14 days) produces antidepressant-like effects in female FSL rats, significantly increasing forced swim test swimming time after 14 days of daily intraperitoneal administration of 0.3 mg/kg[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Flinders Sensitive Line (FSL) (male, ~70 days old, 280-320 g, genetic depression model)[2]
-
Dosage:0.0125 mg/kg; 0.025 mg/kg; 0.05 mg/kg; 0.1 mg/kg; 0.2 mg/kg; 0.3 mg/kg; 0.4 mg/kg; 0.6 mg/kg; 0.8 mg/kg; 1.2 mg/kg; 2.4 mg/kg; 3.0 mg/kg; 4.0 mg/kg; 5.0 mg/kg; 15.0 mg/kg
-
Administration:i.p.; daily; 14 days
-
Result:Significantly increased swimming time in the forced swim test at doses 0.025 mg/kg, 0.05 mg/kg, 0.1 mg/kg, 0.2 mg/kg, 0.3 mg/kg, 3.0 mg/kg, 4.0 mg/kg, 5.0 mg/kg, and 15.0 mg/kg.
Did not significantly increase swimming time at doses 0.4 mg/kg, 0.6 mg/kg, 0.8 mg/kg, and 1.2 mg/kg.
Produced intermediate effects at 0.0125 mg/kg and 2.4 mg/kg, with swimming time significantly higher than vehicle-treated FSL rats but significantly lower than untreated FRL control rats.
Identified 0.3 mg/kg as the most effective dose.
-
Animal Model:Flinders Sensitive Line (FSL) (male, ~70 days old, 280-320 g, genetic depression model)[2]
-
Dosage:0.3 mg/kg
-
Administration:i.p.; daily; 5 days
-
Result:Significantly increased swimming time in the forced swim test compared to vehicle-treated FSL rats.
-
Animal Model:Flinders Sensitive Line (FSL) (male, ~70 days old, 280-320 g, genetic depression model)[2]
-
Dosage:0.3 mg/kg
-
Administration:i.p.; daily; 14 days
-
Result:Significantly increased swimming time 22-24 hours after the final dose.
Maintained the effect 5 days after treatment cessation, with treated rats swimming significantly more than vehicle-treated rats at the 5-day follow-up.
-
Animal Model:Flinders Resistant Line (FRL) (male, ~70 days old, genetic control strain for depression model)[2]
-
Dosage:0.3 mg/kg
-
Administration:i.p.; daily; 14 days
-
Result:Did not significantly increase swimming time in FRL rats; treated rats swam an average of 199.8 seconds, which did not differ from untreated FRL controls.
-
Animal Model:High DPAT Sensitive (HDS) (male, selectively bred depression model); Low DPAT Sensitive (LDS) (male, selectively bred depression model)[2]
-
Dosage:0.3 mg/kg
-
Administration:i.p.; daily; 14 days
-
Result:Significantly increased swimming time in both HDS and LDS rats compared to vehicle-treated controls of the same strain.
-
Animal Model:Flinders Sensitive Line (FSL) (female, genetic depression model)[2]
-
Dosage:0.3 mg/kg
-
Administration:i.p.; daily; 14 days
-
Result:Significantly increased swimming time in female FSL rats; treated rats swam an average of 428 seconds, compared to 288.9 seconds in vehicle-treated female FSL rats.
Chemical Information
-
CAS No. 173240-15-8
-
Masse moléculaire 694.77
-
Formule C33H43FN10O6
-
SMILES
C([C@H](CC1=CC=C(F)C=C1)N)(=O)N2[C@H](C(N[C@H](C(NCC(N[C@@H](CC=3C=4C(NC3)=CC=CC4)C(N)=O)=O)=O)CCCNC(=N)N)=O)C[C@@H](O)C2
-
Synonyms
INN 00835
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Montgomery SA, et al. Efficacy and safety of 30 mg/d and 45 mg/d nemifitide compared to placebo in major depressive disorder. The international journal of neuropsychopharmacology. 2006 Oct;9(5):517-28. [Content Brief]
[2]. Overstreet DH, et al. Antidepressant-like effects of a novel pentapeptide, nemifitide, in an animal model of depression. Psychopharmacology. 2004 Sep;175(3):303-9. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Nemifitide Related Classifications
HY-105077 Related Classifications
Powered by Bioz