FK 1052

a serotonin 3 & 4 dual receptor antagonist; structure given in first source

Also Known As:

8,9-dihydro-10-dihydro-10-methyl-7-((5-methyl-4-imidazolyl)methyl)pyrido-(1-2a)-indol-6(7H)-one; FK 1052, (+)-isomer; FK 1052, (-)-isomer; FK 1052, hydrochloride; FK 1052, hydrochloride, (+)-isomer; FK-1052; FK1052

Networked: 4 relevant articles (0 outcomes, 1 trials/studies)

Bio-Agent Context: Research Results

Heterocyclic Compounds: 198
- 1-Ring Heterocyclic Compounds
  - Azoles: 2138
    - Imidazoles: 150
      - FK 1052: 4
- Fused-Ring Heterocyclic Compounds
  - 2-Ring Heterocyclic Compounds
    - Indoles: 200
      - FK 1052: 4

Experts

1.	Higaki, Mika: 1 article (08/2005)
2.	Imazumi, Katsunori: 1 article (08/2005)
3.	Ishikawa, Hirofumi: 1 article (08/2005)
4.	Matsuo, Masahiko: 1 article (08/2005)
5.	Mutoh, Seitaro: 1 article (08/2005)
6.	Nakayama, Hiroe: 1 article (08/2005)
7.	Yamakuni, Hisashi: 1 article (08/2005)
8.	Imazumi, K: 1 article (03/2000)
9.	Maeda, Y: 1 article (03/2000)
10.	Matsuo, M: 1 article (03/2000)

Related Diseases

1.	Vomiting 08/01/2005 - "The present study suggests that FK1052 may be useful against both acute and delayed emesis induced by cancer chemotherapy. " 03/01/2000 - "These results suggest that the 5-HT(4) receptor may be in part involved in the production of delayed emesis induced by MTX in dogs and that FK1052 may be a useful drug against both acute and delayed emesis induced by cancer chemotherapy." 08/01/2005 - "In Suncus murinus, oral administration of FK1052 (100 microg/kg) completely prevented emesis induced by cisplatin (18 mg/kg, i.p.). " 08/01/2005 - "In ferrets, copper sulfate (40 mg/kg, p.o.)-induced emesis was moderately prevented by FK1052 (3.2 mg/kg), but not by granisetron (3.2 mg/kg). " 08/01/2005 - "We investigated the effect of FK1052 [(+)-8,9-dihydro-10-methyl-7-[(5-methyl-1H-imidazol-4-yl)methyl]pyrido[1,2-a]indol-6(7H)-one hydrochloride], a 5-HT3- and 5-HT4-receptor antagonist, on the emesis induced by motion stimuli, copper sulfate, or cisplatin in either Suncus murinus or ferrets and also clarified the role of the 5-HT3 and 5-HT4 receptors in these models. "
2.	Neoplasms (Cancer) 08/01/2005 - "The present study suggests that FK1052 may be useful against both acute and delayed emesis induced by cancer chemotherapy. " 03/01/2000 - "These results suggest that the 5-HT(4) receptor may be in part involved in the production of delayed emesis induced by MTX in dogs and that FK1052 may be a useful drug against both acute and delayed emesis induced by cancer chemotherapy."
3.	Irritable Bowel Syndrome (Syndrome, Irritable Bowel) 07/01/1993 - "These findings suggest that 5-HT3 and 5-HT4 receptors may have an important role in colonic function and FK1052 may have therapeutic potential in the treatment of gastrointestinal dysfunction such as irritable bowel syndrome."
4.	Diarrhea 07/01/1993 - "5-HT (0.32 mg/kg i.p.)-induced diarrhea was also inhibited by FK1052, ondansetron and granisetron, with ED50 values of 0.09, 2.3 and 0.88 mg/kg p.o., respectively. "

Related Drugs and Biologics

1.	Cisplatin (Platino)
2.	Copper Sulfate (Sulfate, Copper)
3.	Granisetron (Kytril)
4.	Ondansetron (Zofran)
5.	Serotonin (5 Hydroxytryptamine)
6.	Antiemetics
7.	5-HT3 Serotonin Receptors (5 HT3 Receptor)
8.	Emetics
9.	Tropisetron (Navoban)
10.	(2S,3S)- 2- phenyl- 3- ((5- trifluoromethoxy- 2- methoxy)benzylamino)piperidine

Related Therapies and Procedures

1.	Drug Therapy (Chemotherapy)
2.	Intravenous Injections
3.	Injections
4.	Oral Administration