Lerisetron
- Product Name
- Lerisetron
- CAS No.
- 143257-98-1
- Chemical Name
- Lerisetron
- Synonyms
- CID 65997;F-0930-RS;Lerisetron;Lerisetron, 10 mM in DMSO;1-benzyl-2-piperazin-1-ylbenzimidazole;1-BENZYL-2-PIPERAZIN-1-YL-1H-BENZIMIDAZOLE;1-Benzyl-2-(piperazin-1-yl)-1H-1,3-benzodiazole;1-Benzyl-2-(piperazin-1-yl)-1H-benzo[d]imidazole;1H-Benzimidazole, 1-(phenylmethyl)-2-(1-piperazinyl)-;1-benzyl-2-piperazin-1-yl-1H-benzimidazole dihydrochloride
- CBNumber
- CB61179015
- Molecular Formula
- C18H20N4
- Formula Weight
- 292.38
- MOL File
- 143257-98-1.mol
Lerisetron Property
- storage temp.
- Store at -20°C
- solubility
- DMSO: 58 mg/mL (198.37 mM);Ethanol: 58 mg/mL (198.37 mM)
- form
- Solid
- color
- White to off-white
- Water Solubility
- Water: Insoluble
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P270Do not eat, drink or smoke when using this product.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P321Specific treatment (see … on this label).
P330Rinse mouth.
P332+P313IF SKIN irritation occurs: Get medical advice/attention.
P362Take off contaminated clothing and wash before reuse.
P501Dispose of contents/container to..…
N-Bromosuccinimide Price
- Product number
- API0009131
- Product name
- LERISETRON
- Purity
- 95.00%
- Packaging
- 5MG
- Price
- $500.83
- Updated
- 2021/12/16
- Product number
- 137090
- Product name
- 1-Benzyl-2-piperazin-1-yl-1H-benzimidazole dihydrochloride
- Purity
- 95%
- Packaging
- 1g
- Price
- $611
- Updated
- 2021/12/16
- Product number
- 3845CA
- Product name
- Lerisetron
- Packaging
- 100mg
- Price
- $623
- Updated
- 2021/12/16
- Product number
- 137090
- Product name
- 1-Benzyl-2-piperazin-1-yl-1H-benzimidazole dihydrochloride
- Purity
- 95%
- Packaging
- 2.500g
- Price
- $1334
- Updated
- 2021/12/16
- Product number
- 3845CA
- Product name
- Lerisetron
- Packaging
- 5g
- Price
- $1724
- Updated
- 2021/12/16
Lerisetron Chemical Properties,Usage,Production
Uses
Lerisetron is a potent 5-HT3 antagonists and possess high-affinity binding for the 5-HT3 receptors with pKi value of 9.2. Lerisetron has a potent ability to inhibit the 5-HT-evoked reflex bradycardia in urethane-anesthetized rats[1].
in vivo
Lerisetron (50-200 μg/kg; IV; single) exhibits CL of 0.004-0.005 L/min, Vds of 0.88-0.96 L, MRT0-LAST of 224-337.1 min and AUC∞ of 57.7-66.1 μg·min/L in rats[2].
Lerisetron (2-10 μg/kg; IV; single) causes rapid recovery from bradycardia[2].
Pharmacokinetic Parameters of Lerisetron in Sprague-Dawley rats[2].
| IV (50 μg/kg) | IV (100 μg/kg) | IV (200 μg/kg) | |
| CL (L/min) | 0.005 | 0.004 | 0.004 |
| Vds (L) | 0.9 | 0.88 | 0.96 |
| MRT0-LAST (min) | 224 | 337.1 | 226.3 |
| AUC∞ (μg·min/L) | 66.1 | 57.7 | 58.1 |
References
[1] Orjales A, Mosquera R, Labeaga L, Rodes R. New 2-piperazinylbenzimidazole derivatives as 5-HT3 antagonists. Synthesis and pharmacological evaluation. J Med Chem. 1997;40(4):586-593.
[2] Jauregizar N, Calvo R, Suarez E, Quintana A, Raczka E, Lukas JC. Pharmacokinetics and pharmacological effect of lerisetron, a new 5-HT3 antagonist, in rats. J Pharm Sci. 2002;91(1):41-52. DOI:10.1002/jps.1169
Lerisetron Preparation Products And Raw materials
Raw materials
Preparation Products
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