122852-69-1 Usage
Description
Alosetron hydrochloride, also known as Lotronex, is a hydrochloride salt of alosetron, a selective 5-HT3 receptor antagonist. It is a crystalline solid that 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.
Used in Pharmaceutical Industry:
Alosetron hydrochloride is used as a therapeutic agent for the treatment of irritable bowel syndrome (IBS). It works by blocking the action of serotonin on the 5-HT3 receptors in the gut, which helps to reduce the symptoms of IBS, such as abdominal pain, diarrhea, and bloating.
Alosetron hydrochloride is used as a medication for women with severe diarrhea-predominant IBS. Initially approved by the FDA in 2000, it was voluntarily pulled from the market by GlaxoWellcome in the same year due to reports of severe adverse side effects, some resulting in death. In 2002, it was reapproved under more restrictive conditions and a risk management program, with a focus on prescribing it only when its medical benefits outweigh the risks of toxic effects.
There are other potential uses for alosetron hydrochloride, as animal models have shown some evidence for its ability to mitigate the effects of psychosis, anxiety, cognitive impairment, emesis, and drug withdrawal. However, these possibilities have not been verified in humans.
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
