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Piboserod

CAT: 0804-HY-15574-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-15574-01Size:5 mg
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Description
Piboserod is an orally available selective antagonist of the 5-HT4 receptor, with a Ki value of approximately 0.1 nM for human 5-HT4 receptors. Piboserod can competitively bind to the 5-HT4 receptor and block the activation of the 5-HT4 receptor. Piboserod can inhibit the enhancing effect of 5-HT on the nerve-mediated contraction response of the human bladder detrusor muscle. Piboserod is mainly used in the research of urinary system diseases (such as overactive bladder) and cardiovascular diseases (such as chronic heart failure) [1][2][3][4].
CAS Number
152811-62-6
Product Name Alternative
SB-207266
UNSPSC
12352005
Hazard Statement
H301
Target
5-HT Receptor
Type
Reference compound
Related Pathways
GPCR/G Protein; Neuronal Signaling
Applications
COVID-19-immunoregulation
Field of Research
Cardiovascular Disease
Assay Protocol
https://www.medchemexpress.com/Piboserod.html
Purity
99.09
Solubility
DMSO : 25 mg/mL (ultrasonic; warming; heat to 60°C)
Smiles
O=C(C1=C(OCCC2)N2C3=C1C=CC=C3)NCC4CCN(CCCC)CC4
Molecular Formula
C22H31N3O2
Molecular Weight
369.50
Precautions
H301
References & Citations
[1]Darblade B, et al. Piboserod (SB 207266), a selective 5-HT4 receptor antagonist, reduces serotonin potentiation of neurally-mediated contractile responses of human detrusor muscle. World J Urol. 2005 Jun;23 (2) :147-51.|[2]Kjekshus JK, et al. Effect of piboserod, a 5-HT4 serotonin receptor antagonist, on left ventricular function in patients with symptomatic heart failure. Eur J Heart Fail. 2009 Aug;11 (8) :771-8.|[3]Nirogi R, et al. In-vivo rat striatal 5-HT4 receptor occupancy using non-radiolabelled SB207145. J Pharm Pharmacol. 2013 May;65 (5) :704-12.|[4]McCullough JL, et al. The 5-HT2B antagonist and 5-HT4 agonist activities of tegaserod in the anaesthetized rat. Pharmacol Res. 2006 Apr;53 (4) :353-8.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 2
Isoform
Apolipoprotein D