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81098-60-4

81098-60-4 structure
81098-60-4 structure
  • Name: Cisapride
  • Chemical Name: cisapride
  • CAS Number: 81098-60-4
  • Molecular Formula: C23H29ClFN3O4
  • Molecular Weight: 465.945
  • Catalog: API Digestive system medication Gastrointestinal drug
  • Create Date: 2018-06-23 18:24:39
  • Modify Date: 2024-01-02 17:50:51
  • Cisapride(R 51619) is a nonselective 5-HT4 receptor agonist, it is also a potent hERG potassium channel inhibitor.IC50 Value: 0.14 μM(EC50 for 5-HT4 receptor) [1]; 9.8 μM (Kv4.3) [2]Target: 5-HT4 Receptorin vitro: Cisapride showed higher inhibitory effects on a hERG current, as indicated by its IC50 of 9.4 × 10-9 M [1]. cisapride on cloned Kv4.3 channels stably expressed in Chinese hamster ovary cells were investigated using the whole-cell patch-clamp technique. Cisapride inhibited Kv4.3 in a concentration-dependent manner with IC50 values of 9.8 uM [2].in vivo: Cisapride (1 mg/kg i.v.), when administered 10 min after the start of GR113808 infusion, did not stimulate either antral or colonic motor activity under treatment with GR113808. The enhanced antral or colonic motor activity induced by these drugs was antagonized by treatment with GR113808 in dogs [3]. cisapride could not bring about more colitis damages through 5HT(4) receptors. Based on the present study further researches are required for investigating the exact roles of 5HT(4) receptors in the pathogenesis of ulcerative colitis[4].Toxicity: cardiac arrythmies
Name cisapride
Synonyms Cisapride
MFCD03305346
4-Amino-5-chloro-N-{1-[3-(4-fluorophenoxy)propyl]-3-methoxy-4-piperidinyl}-2-methoxybenzamide
prepulsid
EINECS 279-689-7
Benzamide, 4-amino-5-chloro-N-[1-[3-(4-fluorophenoxy)propyl]-3-methoxy-4-piperidinyl]-2-methoxy-
Risamol
ACENALIN
4-amino-5-chloro-N-{1-[3-(4-fluorophenoxy)propyl]-3-methoxypiperidin-4-yl}-2-methoxybenzamide
Alimix
4-Amino-5-chlor-N-{1-[3-(4-fluorphenoxy)propyl]-3-methoxypiperidin-4-yl}-2-methoxybenzolcarboxamid
CIPRIL
propulsid
4-amino-5-chloro-N-[1-{3-[(4-fluorophenyl)oxy]propyl}-3-(methyloxy)piperidin-4-yl]-2-(methyloxy)benzamide
Risamal
Description Cisapride(R 51619) is a nonselective 5-HT4 receptor agonist, it is also a potent hERG potassium channel inhibitor.IC50 Value: 0.14 μM(EC50 for 5-HT4 receptor) [1]; 9.8 μM (Kv4.3) [2]Target: 5-HT4 Receptorin vitro: Cisapride showed higher inhibitory effects on a hERG current, as indicated by its IC50 of 9.4 × 10-9 M [1]. cisapride on cloned Kv4.3 channels stably expressed in Chinese hamster ovary cells were investigated using the whole-cell patch-clamp technique. Cisapride inhibited Kv4.3 in a concentration-dependent manner with IC50 values of 9.8 uM [2].in vivo: Cisapride (1 mg/kg i.v.), when administered 10 min after the start of GR113808 infusion, did not stimulate either antral or colonic motor activity under treatment with GR113808. The enhanced antral or colonic motor activity induced by these drugs was antagonized by treatment with GR113808 in dogs [3]. cisapride could not bring about more colitis damages through 5HT(4) receptors. Based on the present study further researches are required for investigating the exact roles of 5HT(4) receptors in the pathogenesis of ulcerative colitis[4].Toxicity: cardiac arrythmies
Related Catalog
References

[1]. Toga, T., Y. Kohmura, and R. Kawatsu, The 5-HT(4) agonists cisapride, mosapride, and CJ-033466, a Novel potent compound, exhibit different human ether-a-go-go-related gene (hERG)-blocking activities. J Pharmacol Sci, 2007. 105(2): p. 207-10.

[2]. Sung, K.W. and S.J. Hahn, Effect of mosapride on Kv4.3 potassium channels expressed in CHO cells. Naunyn Schmiedebergs Arch Pharmacol, 2013. 386(10): p. 905-16.

[3]. Mine, Y, et al. Comparison of effect of mosapride citrate and existing 5-HT4 receptor agonists on gastrointestinal motility in vivo and in vitro. J Pharmacol Exp Ther, 1997. 283(3): p. 1000-8.

[4]. Motavallian, A, et al., Does Cisapride, as a 5HT(4) Receptor Agonist, Aggravate the Severity of TNBS-Induced Colitis in Rat. Gastroenterol Res Pract, 2012. 2012: p. 362536.
Density 1.3±0.1 g/cm3
Boiling Point 605.4±55.0 °C at 760 mmHg
Melting Point 107 - 111ºC
Molecular Formula C23H29ClFN3O4
Molecular Weight 465.945
Flash Point 319.9±31.5 °C
Exact Mass 465.183075
PSA 86.05000
LogP 3.12
Vapour Pressure 0.0±1.7 mmHg at 25°C
Index of Refraction 1.593
Storage condition Store at RT
Water Solubility DMSO: ~30 mg/mL

CHEMICAL IDENTIFICATION

RTECS NUMBER :
CU9372000
CHEMICAL NAME :
Benzamide, 4-amino-5-chloro-N-(1-(3-(4-fluorophenoxy)propyl)-3-m ethoxy-4-piperidinyl) -2- methoxy-, monohydrate, cis-
CAS REGISTRY NUMBER :
81098-60-4
LAST UPDATED :
199504
DATA ITEMS CITED :
12
MOLECULAR FORMULA :
C23-H29-Cl-F-N3-O4.H2-O
MOLECULAR WEIGHT :
484.02

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Unreported
SPECIES OBSERVED :
Human - woman
DOSE/DURATION :
400 ug/kg/2D-I
TOXIC EFFECTS :
Kidney, Ureter, Bladder - other changes
REFERENCE :
MJAUAJ Medical Journal of Australia. (Australasian Medical Pub. Co. Ltd., 71-79 Arundel St., Glebe, N.S.W., Australia) V.1- 1914- Volume(issue)/page/year: 160,579,1994
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Unreported
SPECIES OBSERVED :
Human - woman
DOSE/DURATION :
200 ug/kg
TOXIC EFFECTS :
Kidney, Ureter, Bladder - urine volume increased
REFERENCE :
MJAUAJ Medical Journal of Australia. (Australasian Medical Pub. Co. Ltd., 71-79 Arundel St., Glebe, N.S.W., Australia) V.1- 1914- Volume(issue)/page/year: 160,579,1994
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
4166 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - ptosis Behavioral - changes in motor activity (specific assay) Lungs, Thorax, or Respiration - other changes
REFERENCE :
IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 19,599,1988
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
3435 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - ptosis Behavioral - changes in motor activity (specific assay) Lungs, Thorax, or Respiration - other changes
REFERENCE :
IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 19,599,1988
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
>2250 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - ptosis Behavioral - changes in motor activity (specific assay) Lungs, Thorax, or Respiration - other changes
REFERENCE :
IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 19,599,1988
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
27400 ug/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - ptosis Behavioral - changes in motor activity (specific assay) Lungs, Thorax, or Respiration - other changes
REFERENCE :
IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 19,599,1988
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
8715 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - ptosis Behavioral - changes in motor activity (specific assay) Lungs, Thorax, or Respiration - other changes
REFERENCE :
IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 19,599,1988
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
>1 gm/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - ptosis Behavioral - changes in motor activity (specific assay) Lungs, Thorax, or Respiration - other changes
REFERENCE :
IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 19,599,1988
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
>1 gm/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - ptosis Behavioral - changes in motor activity (specific assay) Lungs, Thorax, or Respiration - other changes
REFERENCE :
IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 19,599,1988
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
32200 ug/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - ptosis Behavioral - changes in motor activity (specific assay) Lungs, Thorax, or Respiration - other changes
REFERENCE :
IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 19,599,1988 ** OTHER MULTIPLE DOSE TOXICITY DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
14600 mg/kg/52W-C
TOXIC EFFECTS :
Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Related to Chronic Data - death Related to Chronic Data - changes in uterine weight
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 35,85,1988
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
3600 mg/kg/90D-I
TOXIC EFFECTS :
Liver - changes in liver weight Blood - pigmented or nucleated red blood cells Related to Chronic Data - changes in ovarian weight
REFERENCE :
IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 19,599,1988
Hazard Codes Xi:Irritant
Risk Phrases R41
Safety Phrases S26-S39
WGK Germany 2
RTECS CU9372000
HS Code 2942000000
HS Code 2942000000

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