Alosetron hydrochloride

Names

[ Name ]:
Alosetron hydrochloride

[Synonym ]:
Alosetron hydrochloride
5-méthyl-2-[(4-méthyl-1H-imidazol-5-yl)méthyl]-2,3,4,5-tétrahydro-1H-pyrido[4,3-b]indol-1-one chlorhydrate
gr 68755c
1H-pyrido[4,3-b]indol-1-one, 2,3,4,5-tetrahydro-5-methyl-2-[(4-methyl-1H-imidazol-5-yl)methyl]-, monohydrochloride
1H-Pyrido[4,3-b]indol-1-one, 2,3,4,5-tetrahydro-5-methyl-2-[(5-methyl-1H-imidazol-4-yl)methyl]-, hydrochloride (1:1)
1H-pyrido[4,3-b]indol-1-one, 2,3,4,5-tetrahydro-5-methyl-2-[(4-methyl-1H-imidazol-5-yl)methyl]-, hydrochloride (1:1)
LOTRONEX
MFCD03453647
Alosetron HCl
GR-68755C
5-methyl-2-[(4-methyl-1H-imidazol-5-yl)methyl]-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indol-1-one hydrochloride
5-Methyl-2-[(4-methyl-1H-imidazol-5-yl)methyl]-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indol-1-one hydrochloride (1:1)
5-Methyl-2-[(4-methyl-1H-imidazol-5-yl)methyl]-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indol-1-onhydrochlorid
Alosetron (Hydrochloride)

Biological Activity

[Description]:

Alosetron Hcl is a Serotonin 5HT3-receptor antagonist that is used in treatment of irritable bowel syndrome.IC50 Value: Target: 5-HT ReceptorAlosetron has an antagonist action on the 5-HT3 receptors of the enteric nervous system of the gastrointestinal tract. While being a 5-HT3 antagonist like ondansetron, it is not classified or approved as an antiemetic. Since stimulation of 5-HT3 receptors is positively correlated with gastrointestinal motility, alosetron's 5-HT3 antagonism slows the movement of fecal matter through the large intestine, increasing the extent to which water is absorbed, and decreasing the moisture and volume of the remaining waste products. From Wikipedia.

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor

Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor

Research Areas >> Neurological Disease

[References]

[1]. Targeting the 5-HT3 receptor in the treatment of irritable bowel syndrome By Spiller, Robin C. From Current Opinion in Pharmacology (2011), 11(1), 68-74.

[2]. Lucak SL. Optimizing outcomes with alosetron hydrochloride in severe diarrhea-predominant irritable bowel syndrome. Therap Adv Gastroenterol. 2010 May;3(3):165-72.

[3]. Lewis JH. Alosetron for severe diarrhea-predominant irritable bowel syndrome: safety and efficacy in perspective. Expert Rev Gastroenterol Hepatol. 2010 Feb;4(1):13-29.

[4]. Turgeon DK, Tayeh N, Fontana RJ. Acute hepatitis associated with alosetron (Lotronex). J Clin Gastroenterol. 2005 Aug;39(7):641-2.

[5]. Miller DP, Alfredson T, Cook SF, Sands BE, Walker AM. Incidence of colonic ischemia, hospitalized complications of constipation, and bowel surgery in relation to use of alosetron hydrochloride. Am J Gastroenterol. 2003 May;98(5):1117-22.

[Related Small Molecules]

Chemical & Physical Properties

[ Density]:
1.34g/cm3

[ Boiling Point ]:
648.1ºC at 760 mmHg

[ Melting Point ]:
288-291ºC

[ Molecular Formula ]:
C₁₇H₁₉ClN₄O

[ Molecular Weight ]:
330.812

[ Flash Point ]:
345.8ºC

[ Exact Mass ]:
330.124725

[ PSA ]:
53.92000

[ LogP ]:
3.14820

[ Vapour Pressure ]:
1.1E-16mmHg at 25°C

[ Storage condition ]:
Refrigerator

MSDS

Click to get detail MSDS

Safety Information

[ Symbol ]:

GHS06, GHS09

[ Signal Word ]:
Danger

[ Hazard Statements ]:
H301-H319-H411

[ Precautionary Statements ]:
P273-P301 + P310-P305 + P351 + P338

[ Hazard Codes ]:
T,Xi

[ Risk Phrases ]:
25-36-52/53

[ Safety Phrases ]:
26-45

[ RIDADR ]:
UN 2811 6.1 / PGIII

[ HS Code ]:
2933990090

Customs

[ HS Code ]: 2933990090

[ Summary ]:
2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

Articles

In silico binary classification QSAR models based on 4D-fingerprints and MOE descriptors for prediction of hERG blockage.

J. Chem. Inf. Model. 50(7) , 1304-18, (2010)

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Quantitative benefit-risk assessment using only qualitative information on utilities.

Med. Decis. Making 32(6) , E1-15, (2012)

Utilities of pertinent clinical outcomes are crucial variables for assessing the benefits and risks of drugs, but numerical data on utilities may be unreliable or altogether missing. We propose a meth...

Clinical trials in irritable bowel syndrome: a review.

Rev. Recent Clin. Trials 8(1) , 9-22, (2013)

Irritable bowel syndrome (IBS) is one of the most common gastrointestinal disorders and it is characterized by episodes of abdominal pain and altered bowel functions. The specific bowel disturbances o...