Alosetron HCl - CAS 122852-69-1
Not Intended for Therapeutic Use. For research use only.
Category:
Inhibitor
Product Name:
Alosetron HCl
Catalog Number:
122852-69-1
Synonyms:
2,3,4,5-Tetrahydro-5-methyl-2-[(4-methyl-1H-imidazol-5-yl)methyl]-1H-pyrido[4,3-b]indol-1-one Hydrochloride;
CAS Number:
122852-69-1
Description:
The hydrochloride salt form of Alosetron which is an effective 5-HT3 receptor antagonist and could be commonly used against irritable bowel syndrome.
Molecular Weight:
330.81
Molecular Formula:
C17H18N4O. HCl
Quantity:
Milligrams-Grams
COA:
Inquire
MSDS:
Inquire
Canonical SMILES:
CC1=C(N=CN1)CN2CCC3=C(C2=O)C4=CC=CC=C4N3C.Cl
InChI:
InChI=1S/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
InChIKey:
FNYQZOVOVDSGJH-UHFFFAOYSA-N
Targets:
5-HT Receptor
Chemical Structure
CAS 122852-69-1 Alosetron HCl

Related 5-HT Receptor Products


CAS 30123-17-2 Tianeptine sodium

Tianeptine sodium
(CAS: 30123-17-2)

Tianeptine sodium is a selective serotonin reuptake enhancer (SSRE), used for treating major depressive episodes.

(S)-6-Hydroxybuspirone
(CAS: 477930-31-7)

(S)-6-Hydroxybuspirone is a major active metabolite of Buspirone. (R)-Enantiomer showed higher affinity and selectivity for the 5HT1A receptor compared to the ...

RU-24969
(CAS: 66611-26-5)

RU 24969 is a 5-HT1A and 5-HT1B receptors act as serotonin 1A/1B receptor agonists.

CAS 554403-49-5 WAY181187

WAY181187
(CAS: 554403-49-5)

WAY181187 is a potent and selective 5-HT6 receptor full agonist. It possesses high affinity binding at the human 5-HT6 receptor and profile as full receptor ago...

CAS 27833-64-3 Loxapine Succinate

Loxapine Succinate
(CAS: 27833-64-3)

Loxapine Succinate is a D2DR and D4DR inhibitor, serotonergic receptor antagonist and also a dibenzoxazepine anti-psychotic agent.oxapine is a typical antipsych...

Risperidone mesylate
(CAS: 666179-96-0)

Risperidone is a serotonin 5-HT2 receptor blocker and a potent dopamine D2 receptor antagonist.

CAS 138112-76-2 Agomelatine

Agomelatine
(CAS: 138112-76-2)

Agomelatine is a melatoninergic agonist and selective antagonist of 5-HT2C receptors, and has been shown to be active in several animal models of depression. Ag...

CAS 222551-17-9 Adoprazine

Adoprazine
(CAS: 222551-17-9)

Adoprazine, also known as SLV 313, with potential antipsychotic property, is a agonist of cloned h5-HT(1A) receptors (pEC(50)=9.0) and a full antagonist of hD(2...

CAS 64887-14-5 Urapidil HCl

Urapidil HCl
(CAS: 64887-14-5)

Urapidil HCl is a hydrochloride salt form of urapidil which is α1-adrenoceptor antagonist and 5-HT1A receptor agonist with pIC50 of 6.13 and 6.4 respectively.

TG6-10-1
(CAS: 1415716-58-3)

TG6-10-1, a potent and selective antagonist for the prostaglandin E2 receptor subtype EP2, has been shown antagonist activity at human EP2 receptor expressed in...

CAS 98224-03-4 Eltoprazine

Eltoprazine
(CAS: 98224-03-4)

Eltoprazine belongs the phenylpiperazine class which is a serenic or antiaggressive agent. It acts as an agonist at the 5-HT1A and 5-HT1B receptors and as an an...

CAS 199864-87-4 RS 127445

RS 127445
(CAS: 199864-87-4)

RS 127445 is a high affinity, orally bioavailable, selective serotonin antagonist of 5-HT2B receptor (pIC50= 10.4) with 1000 fold selectivity over the human rec...

CAS 17321-77-6 Clomipramine HCl

Clomipramine HCl
(CAS: 17321-77-6)

Clomipramine HCl is a hydrochloride salt of clomipramine which is a serotonin transporter (SERT), norepinephrine transporter (NET) dopamine transporter (DAT) bl...

CAS 115338-32-4 NAN-190 hydrobromide

NAN-190 hydrobromide
(CAS: 115338-32-4)

The hydrobromide salt form of NAN-190 which is an effective antagonist of 5-HT1A serotonin receptor.

CAS 189188-57-6 Tegaserod maleate

Tegaserod maleate
(CAS: 189188-57-6)

Tegaserod maleate is a partial agonist of the 5-HT4 receptor (Ki = 12 nM) that can treat irritable bowel syndrome (IBS).

CAS 162760-96-5 WAY-100635

WAY-100635
(CAS: 162760-96-5)

WAY-100635 is an achiral analogue of WAY-100135 which is significantly more potent and selective than the latter compound and which displays unequivocal 5-HTIA ...

CAS 85650-56-2 Asenapine Maleate

Asenapine Maleate
(CAS: 85650-56-2)

Asenapine Maleate is a 5-HT receptor antagonist used for the treatment of acute schizophrenia and bipolar mania. It is a second-generation (atypical) antipsycho...

CAS 132539-06-1 Olanzapine

Olanzapine
(CAS: 132539-06-1)

Olanzapine interacts with key receptors of interest in schizophrenia, having a nanomolar affinity for dopaminergic, serotonergic, alpha 1-adrenergic, and muscar...

CAS 158876-82-5 Rupatadine

Rupatadine
(CAS: 158876-82-5)

Rupatadine, with the potential to treat allergic rhinitis and urticaria, is a potent and long-lasting dual antagonist of PAF/H1. in vitro: Without affecting con...

CAS 122852-43-1 Alosetron (Z)-2-butenedioate

Alosetron (Z)-2-butenedioate
(CAS: 122852-43-1)

The maleic acid salt form of Alosetron which is an effective 5-HT3 receptor antagonist and could be commonly used against irritable bowel syndrome.

Reference Reading


1.Development of a Forced Degradation Profile of Alosetron by Single Mode Reversed-Phase HPLC, LC-MS, and its Validation.
Karthik Y1, Babu B1, Meyyanathan SN1. Sci Pharm. 2014 Dec 29;83(2):311-20. doi: 10.3797/scipharm.1411-07. eCollection 2015.
Determination of alosetron in the presence of its degradation products was studied and validated by a novel HPLC method. The separation of the drug and its degradation products was achieved with the Jones Chromatography C18 analytical column (150 mm x 4.6 mm; 3 µm) with a stationary phase in isocratic elution mode. The mobile phase used was 0.01 M ammonium acetate, pH-adjusted to 3.5 with glacial acetic acid and acetonitrile in the ratio of 75:25 (V/V) at a flow rate of 1 ml/min and UV detection was carried out at 217 nm. Further, the drug was subjected to stress studies for acidic, basic, neutral, oxidative, and thermal degradations as per ICH guidelines and the drug was found to be labile in base hydrolysis and oxidation, while stable in acid, neutral, thermal, and photolytic degradation conditions. An MS study has been performed on the major degradation products to predict the degradation pathway of alosetron. The method provided linear responses over the concentration range of 100-1500 ng/ml and regression analysis showed a correlation coefficient value (r(2)) of 0.
2.Novel pharmacological therapies for irritable bowel syndrome.
Corsetti M1, Whorwell P2. Expert Rev Gastroenterol Hepatol. 2016 Mar 18:1-9. [Epub ahead of print]
Irritable bowel syndrome (IBS) is a prevalent functional gastrointestinal disorder, which represents a major cost to healthcare services. Current pharmacological treatment includes fibre supplements, antispasmodics, laxatives, loperamide and antidepressants. This article reviews the novel pharmacological treatments already or recently approved for patients with IBS-C (lubiprostone, linaclotide) and IBS-D (alosetron, ramosetron, rifaximin, eluxadoline). Furthermore, results for drugs in development (plecanatide, ibudutant and ebastine) or used in chronic constipation or for other indications, with potential application in IBS (prucalopride, elobixibat, mesalazine, ondansetron and colesevelam) are also reviewed.
3.Diagnosis and treatment of diarrhea-predominant irritable bowel syndrome.
Lacy BE1. Int J Gen Med. 2016 Feb 11;9:7-17. doi: 10.2147/IJGM.S93698. eCollection 2016.
Irritable bowel syndrome (IBS) is one of the most common gastrointestinal disorders worldwide. The economic impact of IBS on the health care system is substantial, as is the personal impact on patients. Patients with diarrhea-predominant IBS (IBS-D) comprise a substantial proportion of the overall IBS population. Primary care providers are often the first point of contact for patients with IBS-D and can accurately diagnose IBS after a careful history and examination without extensive diagnostic tests. Several pharmacologic treatments (eg, loperamide, alosetron, and antidepressants) and non-pharmacologic treatments (eg, dietary modification and probiotics) are available for IBS-D, but restrictions on use (eg, alosetron) or the lack of controlled trial data showing reductions in both global and individual IBS-D symptoms (eg, bloating, pain and stool frequency) emphasize the need for alternative treatment options. Two newer medications (eluxadoline and rifaximin) were approved in May 2015 for the treatment of IBS-D, and represent new treatment options for this common gastrointestinal condition.
4.Novel Therapies in IBS-D Treatment.
Nee J1, Zakari M2, Lembo AJ2. Curr Treat Options Gastroenterol. 2015 Dec;13(4):432-40. doi: 10.1007/s11938-015-0068-5.
OPINION STATEMENT: Irritable bowel syndrome (IBS) is a common gastrointestinal disease characterized by abdominal pain and change in bowel habits. IBS diarrhea predominant (IBS-D), which is arguably the most common subset of IBS, is also associated with rectal urgency, increased frequency, abdominal bloating, and loose to watery stools. Current treatments for diarrhea include mu-opioid agonists (i.e., loperamide, lomotil) and bile acid sequestrants (i.e., cholestyramine) while treatments for abdominal pain include antispasmodics (i.e., hyoscyamine, dicyclomine) and tricyclic antidepressants (i.e., amitriptyline). There are currently 3 FDA-approved treatments for IBS-D, which have been shown to improve both abdominal pain and diarrhea. Alosetron was initially approved by FDA 2000; however, its use is now limited to women with severe IBS-D symptoms refractory to other treatment. Eluxadoline, a mixed mu-opioid agonist, and rifaximin, a broad spectrum gut specific antibiotic, were both FDA approved in 2015.