122852-69-1 Usage
Description
Lotronex (alosetron) was developed for the treatment of severe
irritable bowel syndrome (IBS), and was approved for use by
the US Food and Drug Administration (FDA) in 2000.
Although Lotronex had a relatively high improvement rate in
patients taking the drug for IBS, it was voluntarily pulled from
the market by GlaxoWellcome that same year due to reports of
severe adverse side effects, some resulting in death.
In 2002, Lotronex was reapproved in a supplemental New
Drug Application for use under more restrictive conditions.
Now with a risk management program to be consulted prior to
administration of the drug, Lotronex is designated to be
prescribed only when its medical benefits outweigh the risks of
toxic effects; women with severe diarrhea-predominant IBS are
now the focal point of prescriptions for Lotronex.
Chemical Properties
Alosetron hydrochloride is Crystalline Solid
Uses
Different sources of media describe the Uses of 122852-69-1 differently. You can refer to the following data:
1. Alosetron hydrochloride is used in treatment of irritable bowel syndrome
2. Lotronex is used for severe diarrhea-predominant IBS in
women. There are other potential uses, as animal models have
shown at least some evidence for the ability of Lotronex to
mitigate the effects of psychosis, anxiety, cognitive impairment,
emesis, and drug withdrawal. These possibilities have not been
verified in humans, however.
Definition
ChEBI: The hydrochloride salt of alosetron.
Therapeutic Function
Antidiarrheal
Biochem/physiol Actions
Alosetron is a potent and highly selective antagonist of serotonin 5-HT3 receptors, nonselective cation channels found predominantly in the enteric nervous system of the gastrointestinal tract. These receptors are involved in the regulation of visceral pain, colonic transit and GI secretions that can contribute to the pathophysiology of irritable bowel syndrome (IBS). Alosetron is used clinically for treatment of women with severe diarrhea-predominant IBS.
Environmental Fate
The environmental fate and behavior of Lotronex is uncertain,
as formal studies regarding its release into the environment are
virtually nonexistent in the literature. Limited water solubility
(61 mg ml-1) may lead to persistence in soils, and in sediment
following aquatic release, although specific fates with regard to
degradation, bioaccumulation, and transport are unknown.
Toxicity evaluation
A highly potent and selective 5-HT3 receptor agonist, Lotronex
rapidly binds to cation channels that exist on enteric neurons in
the human gastrointestinal tract in addition to other central
and peripheral locations. Lotronex inhibits the activation of
these channels, resulting in effects to the enteric nervous system
whereas the activation of these channels regulates (promotes)
colonic transit, visceral pain pathways, and gastrointestinal
secretions – all of which are processes related to the pathophysiology
of IBS. The binding of Lotronex to 5-HT3 receptors
reduces the rate at which fecal matter moves through the large
intestine and increases water absorption. The toxic effects of Lotronex are related to the relative activation/inactivation of
the cation channels responsible for mediating these processes.
Check Digit Verification of cas no
The CAS Registry Mumber 122852-69-1 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,2,2,8,5 and 2 respectively; the second part has 2 digits, 6 and 9 respectively.
Calculate Digit Verification of CAS Registry Number 122852-69:
(8*1)+(7*2)+(6*2)+(5*8)+(4*5)+(3*2)+(2*6)+(1*9)=121
121 % 10 = 1
So 122852-69-1 is a valid CAS Registry Number.
InChI:InChI=1/C17H18N4O.ClH/c1-11-13(19-10-18-11)9-21-8-7-15-16(17(21)22)12-5-3-4-6-14(12)20(15)2;/h3-6,10H,7-9H2,1-2H3,(H,18,19);1H
