129299-81-6
129299-81-6 structure
- Name: FK1052 hydrochloride
- Chemical Name: FK1052 hydrochloride
- CAS Number: 129299-81-6
- Molecular Formula: C18H20ClN3O
- Molecular Weight: 329.824
- Catalog: Signaling Pathways GPCR/G Protein 5-HT Receptor
- Create Date: 2018-05-24 23:01:18
- Modify Date: 2025-08-27 04:28:53
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FK1052 hydrochloride is a potent 5-HT3 and 5-HT4 receptor dual antagonist.
| Name | FK1052 hydrochloride |
|---|---|
| Synonyms |
10-Methyl-7-[(5-methyl-1H-imidazol-4-yl)methyl]-8,9-dihydropyrido[1,2-a]indol-6(7H)-one hydrochloride (1:1)
Pyrido[1,2-a]indol-6(7H)-one, 8,9-dihydro-10-methyl-7-[(5-methyl-1H-imidazol-4-yl)methyl]-, hydrochloride (1:1) |
| Description | FK1052 hydrochloride is a potent 5-HT3 and 5-HT4 receptor dual antagonist. |
|---|---|
| Related Catalog | |
| Target |
5-HT3 and 5-HT4 receptor[1] |
| In Vivo | In conscious rats, both 5-HT and 5-methoxytryptamine significantly increase fecal pellet output and accelerate colonic transit. In contrast, the effect of 2-methyl-5-HT is slight. Although Ondansetron and Granisetron slightly reduce 5-HT (1 mg/kg s.c.) stimulated colonic transit, FK1052, at 0.1 mg/kg p.o., inhibits completely the increases in the colonic transit. Furthermore, FK1052, Ondansetron and Granisetron significantly depress the increase in fecal pellet output caused by wrap-restraint stress, with ED50 values of 0.21, 3.0 and 1.1 mg/kg p.o., respectively. Intraperitoneal administration of 5-HT and 5-methoxytryptamine, but not 2-methyl-5-HT, produces a dose-related increase in the incidence of diarrhea in fasted mice. 5-HT (0.32 mg/kg i.p.)-induced diarrhea is also inhibited by FK1052, Ondansetron and Granisetron, with ED50 values of 0.09, 2.3 and 0.88 mg/kg p.o., respectively[1]. FK1052 (1 mg/kg i.v. ×4) apparently reduces delayed emesis caused by Methotrexate (MTX) and increases, but not significantly, the time for onset of emesis. Furthermore, increasing the dose to 3.2 mg/kg of FK1052 also significantly inhibits the number of the emetic episodes induced by MTX, of which the action is more effective than the treatment with FK1052 at 1 mg/kg[2]. |
| Animal Admin | Mice and Rats[1] Male Sprague-Dawley rats weighing 220 to 330 g and male ddy mice weighing 25 to 35 g are used. FK1052, Ondansetron, Granisetron, Methysergide, Ketanserin and Atropine are dissolved in distilled water. 5-HT, 2-methyl-5-HT, 1-phenylbiguanide and 5-MeOT are dissolved in physiological saline. Diazepam is suspended with 0.5% methylcellulose solution. The drugs are administered to rats at a volume of 2 mL/ kg and to mice at a volume of 5 mL/kg. Dogs[2] Beagle dogs of either sex weighting 8.0 to18.5 kg are used in the study. Dogs are injected i.v. with MTX (2.5 mg/kg/mL) at 7:30 AM. The animal behavior is recorded using a video camera with an automatic night photographing system for up to 72 h and analyzed at the end of the experiment. FK1052 (1 and 3.2 mg/kg), Ondansetron (1 mg/kg), Tropisetron (1 mg/kg), CP-122,721 (0.1 mg/kg), or vehicle (0.5 mL/kg) is administered i.v. at 24, 36, 48, and 60 h after MTX treatment. Episodes of emesis occurring within a few minutes are defined as a single emetic episode. A 12 h artificial light cycle (lights on between 7:30 AM and 7:30 PM) is used throughout the study. Dogs are given a standard laboratory dog chow (300 g/day) and water ad libitum. The animals are retested with MTX at least 6 weeks later. |
| References |
| Molecular Formula | C18H20ClN3O |
|---|---|
| Molecular Weight | 329.824 |
| Exact Mass | 329.129486 |