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Art. -Nr.: HY-109065A

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Minesapride hydrobromide

Name: Minesapride hydrobromide
Brand: MedChemExpress
SKU: HY-109065A
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(Synonyms: DSP-6952 hydrobromide)

Minesapride hydrobromide (DSP-6952 hydrobromide) is an orally active, selective 5-HT4 receptor partial agonist. Minesapride hydrobromide enhances gastrointestinal motility, colonic transit and defecation function, and inhibits visceral hypersensitivity. Minesapride hydrobromide does not inhibit/induce cytochrome P450 isozymes, has no significant affinity for hERG, and does not trigger the risk of cardiac ischemia via coronary vasoconstriction. Minesapride hydrobromide can be used in research related to constipation-predominant irritable bowel syndrome, chronic constipation, atonic constipation, spastic constipation, functional constipation and functional dyspepsia.

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CAS. Nr.: 1184661-33-3
Formel: C₂₁H₃₂BrClN₄O₅
Molecular Weight:535.86

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Minesapride hydrobromide Chemical Structure

CAS. Nr.: 1184661-33-3

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

5-HT₄ Receptor

Alle 5-HT Receptor Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO-K1	IC50	65.4 μM	Inhibition of hERG currents in hERG-transfected CHO-K1 cells assessed via whole-cell patch-clamp assay at room temperature using a voltage protocol holding at -80 mV, stepping to +40 mV for 1 s, then repolarizing to -50 mV for 2 s every 15 s. Inhibition of hERG currents in hERG-transfected CHO-K1 cells assessed via whole-cell patch-clamp assay at room temperature using a voltage protocol holding at -80 mV, stepping to +40 mV for 1 s, then repolarizing to -50 mV for 2 s every 15 s.	29501863

In Vitro

Minesapride hydrobromide exhibits no inhibitory or inductive activity against cytochrome P450 isozymes in in vitro assays^[1].
Minesapride hydrobromide shows no significant binding affinity for the hERG cardiac potassium channel in in vitro experiments^[1].
Minesapride hydrobromide shows no significant binding affinity for 5-HT₁B, 5-HT₁D or 5-HT₂A receptors in in vitro assays^[1].
Minesapride hydrobromide binds to cell membranes of CHO cells stably transfected with human 5-HT4 (a), 5-HT4 (b), and 5-HT4 (c) receptors, as well as to cell membranes of guinea pig striatal tissues, with a K_i range of 51.9-95.3 nM^[2].
Minesapride hydrobromide binds tightly to 5-HT₄ (a), 5-HT₄ (b), and 5-HT₄ (c) receptors (with K_i values of 66.9, 51.9, and 95.3 nM, respectively) as well as guinea pig striatal 5-HT₄ receptors (K_i = 63.1 nM)^[4].
Minesapride hydrobromide induces concentration-dependent contractions in distal colonic LMMP preparations of guinea pigs, with an EC₅₀ of 271.6 nM and an intrinsic activity of 57% relative to 5-HT^[4].
Minesapride (10-100 μM) hydrobromide inhibits hERG currents in hERG-transfected CHO-K1 cells, with an IC₅₀ of 65.4 μM^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Minesapride (0.1-3 mg/kg; i.g.) hydrobromide dose-dependently enhances gastric motility and induces colonic GMCs and defecation in conscious dogs, with ED₅₀ values of 1.56 mg/kg for GMC induction and 2.87 mg/kg for defecation induction^[2].
Minesapride (0.3-10 mg/kg; i.g.) hydrobromide dose-dependently enhances colonic transit rate in guinea pigs via activation of 5-HT₄ receptors, with significant effects seen at doses of 3 mg/kg and 10 mg/kg^[2].
Minesapride (0.3-10 mg/kg; p.o.) hydrobromide dose-dependently increases fecal wet weight in mice without altering fecal fluid content, indicating enhanced defecation without diarrhea^[2].
Minesapride (0.03-3 mg/kg; p.o.) hydrobromide dose-dependently improves Clonidine (HY-12721)-induced atonic constipation in mice, with an ED₅₀ of 0.429 mg/kg^[2].
DSP-6952 (6-180 mg/kg; p.o.; single dose) hydrobromide does not affect ECG parameters or blood pressure up to 180 mg/kg p.o. in conscious cynomolgus monkeys, but causes a transient, dose-dependent increase in heart rate that is significant at 180 mg/kg p.o^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Nosan-Beagle (male; surgically implanted force transducers on gastric antrum and colon, plus intragastric administration tube)^[2]
Dosage:

0.1 mg/kg; 0.3 mg/kg; 1 mg/kg; 3 mg/kg
Administration:

i.g.
Result:

Enhanced gastric motility in a dose-dependent manner, with gastric motor index values of 117.5%, 138.6%, 126.4%, and 140.7% for the 0.1, 0.3, 1, and 3 mg/kg doses, respectively.
Induced colonic GMCs in 0/10, 1/10, 4/10, and 6/9 dogs at the 0.1, 0.3, 1, and 3 mg/kg doses, respectively, with an ED₅₀ of 1.56 mg/kg for GMC induction.
Induced defecation in 0/10, 0/10, 3/10, and 4/9 dogs at the 0.1, 0.3, 1, and 3 mg/kg doses, respectively, with an ED₅₀ of 2.87 mg/kg for defecation induction.

Animal Model:

Slc: Hartley (male; surgically implanted intragastric and colonic administration tubes)^[2]
Dosage:

0.3 mg/kg; 1 mg/kg; 3 mg/kg; 10 mg/kg
Administration:

i.g.
Result:

Enhanced colonic transit rate in a dose-dependent manner, with significant increases at 3 mg/kg and 10 mg/kg.
Had its enhancement of colonic transit rate antagonized by the 5-HT₄ receptor antagonist SB-207266.

Animal Model:

Slc: ddY (male)^[2]
Dosage:

0.3 mg/kg; 1 mg/kg; 3 mg/kg; 10 mg/kg
Administration:

p.o.
Result:

Increased cumulative fecal wet weight over 0-120 minutes in a dose-dependent manner, with significant increases at 1 mg/kg, 3 mg/kg, and 10 mg/kg.
Did not increase fecal fluid content at any dose tested, with fluid content remaining near baseline levels of ~52-56%.

Animal Model:

Macaca fascicularis (male, 3-4 years old, 3.3-3.9 kg)^[4]
Dosage:

6 mg/kg; 20 mg/kg; 60 mg/kg; 180 mg/kg
Administration:

p.o.; single dose
Result:

Showed no statistically significant changes in PQ interval, QRS duration, QTc, or blood pressure at doses up to 180 mg/kg.
Caused a transient, dose-dependent increase in heart rate starting at 20 mg/kg (1 hour post-administration), with a significant increase at 180 mg/kg; all parameters returned to normal ranges by 3-7 hours post-administration.
Reached mean maximum plasma concentrations (Cmax) of 723 ng/mL (6 mg/kg), 4840 ng/mL (20 mg/kg), 19100 ng/mL (60 mg/kg), and 98100 ng/mL (180 mg/kg).
Showed no abnormal general behavior.

Chemical Information

CAS. Nr. 1184661-33-3
Molecular Weight 535.86
Formel C₂₁H₃₂BrClN₄O₅
SMILES

OCC(N(CC1)CCC1CN(CCO2)C[C@@H]2CNC(C3=C(C=C(C(Cl)=C3)N)OC)=O)=O.Br
Synonyms

DSP-6952 hydrobromide
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Fukudo S, et al. Efficacy and Safety of 5-HT4 Receptor Agonist Minesapride for Irritable Bowel Syndrome with Constipation in a Randomized Controlled Trial. Clinical gastroenterology and hepatology : the official clinical practice journal of the American Gastroenterological Association. 2021 Mar;19(3):538-546.e8. [Content Brief]

[2]. Mine Y, et al. DSP-6952, a novel 5-HT receptor partial agonist, inhibits visceral hypersensitivity and ameliorates gastrointestinal dysfunction in experimental animals. European journal of pharmacology. 2018 May 05;826:123-132.

[3]. Hamatani T, et al. Pharmacokinetics, safety and metabolite profiling of minesapride, a novel 5-HT receptor partial agonist, in healthy elderly and young subjects. Drug metabolism and pharmacokinetics. 2020 Dec;35(6):563-570.

[4]. Tsubouchi T, et al. The in vitro pharmacology and non-clinical cardiovascular safety studies of a novel 5-HT receptor agonist, DSP-6952. European journal of pharmacology. 2018 May 05;826:96-105.

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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