1. GPCR/G Protein Neuronal Signaling
  2. 5-HT Receptor
  3. Batanopride

Batanopride (BMY 25801) is a selective 5-HT3 receptor antagonist. Batanopride inhibits chemotherapy-induced emesis, and prevents Cisplatin (HY-17394)-, Cyclophosphamide (HY-17420)-, Doxorubicin (HY-15142A)-, and total body irradiation-induced emesis.

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Batanopride

Batanopride Chemische Struktur

CAS. Nr. : 102670-46-2

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Beschreibung

Batanopride (BMY 25801) is a selective 5-HT3 receptor antagonist. Batanopride inhibits chemotherapy-induced emesis, and prevents Cisplatin (HY-17394)-, Cyclophosphamide (HY-17420)-, Doxorubicin (HY-15142A)-, and total body irradiation-induced emesis[1].

IC50 & Target[1]

5-HT3 Receptor

241 nM (Ki)

In Vitro

Batanopride binds to 5-HT3 receptors with a Ki of 241.0 nM[1].
Batanopride (10000 nM) does not bind to dopamine D2 receptors at concentrations up to 10000 nM[1].
Batanopride does not bind to serotonergic 5-HT1, 5-HT2, dopamine D1, muscarinic, histamine H1, α-adrenergic, or μ-opioid receptors[1].

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

In Vivo

Batanopride (i.v.) inhibits the Serotonin (HY-B1473A)-induced Bezold-Jarisch reflex in anesthetized rats with an ED50 of 70 μg/kg[1].
Batanopride (s.c.) prevents Cisplatin (HY-17394)-induced emesis in dogs with an ED50 of 0.05 mg/kg × 2[1].
Batanopride (6-40 mg/kg; s.c.) does not inhibit Apomorphine (HY-12723)-induced stereotypy in the rat and Apomorphine-induced emesis in the dog[1].

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

Animal Model: Cisplatin-induced emesis in dogs[1]
Dosage: 0.05 mg/kg × 2
Administration: s.c.; 30 minutes before and 2 hours after Cisplatin administration
Result: Had an ED50 of 0.05 mg/kg × 2 s.c. for preventing Cisplatin-induced emesis, which was more potent than Metoclopramide (HY-17382) (ED50 = 0.18 mg/kg × 2 s.c.).
Was twice as long-acting as Metoclopramide, with a 50% decline in anti-emetic protection at 5 hours versus 2.5 hours for Metoclopramide at equipotent doses.
Molekulargewicht

355.86

Formel

C17H26ClN3O3

CAS. Nr.
SMILES

O=C(C1=CC(Cl)=C(C=C1OC(C)C(C)=O)N)NCCN(CC)CC

Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

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