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

Relenopride hydrochloride (Synonyms: YKP10811 hydrochloride)

Cat. No.: HY-16729A
Handling Instructions

Relenopride (YKP10811) hydrochloride is a specific and selective 5-HT4 receptor agonist (Ki=4.96 nM). Relenopride hydrochloride has 120-fold and 6-fold lower affinity, respectively, for 5-HT2A (Ki=600 nM) and 5-HT2B receptors (Ki=31 nM) than for 5-HT4. Relenopride hydrochloride increases gastrointestinal (GI) motility.

For research use only. We do not sell to patients.

Relenopride hydrochloride Chemical Structure

Relenopride hydrochloride Chemical Structure

CAS No. : 1221416-42-7

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Description

Relenopride (YKP10811) hydrochloride is a specific and selective 5-HT4 receptor agonist (Ki=4.96 nM). Relenopride hydrochloride has 120-fold and 6-fold lower affinity, respectively, for 5-HT2A (Ki=600 nM) and 5-HT2B receptors (Ki=31 nM) than for 5-HT4. Relenopride hydrochloride increases gastrointestinal (GI) motility[1][2].

IC50 & Target[1]

5-HT4 Receptor

4.96 nM (Ki)

5-HT2A Receptor

600 nM (Ki)

5-HT2B Receptor

31 nM (Ki)

5-HT2B Receptor

2.1 μM (IC50)

In Vitro

Relenopride hydrochloride do not show any significant off-target binding to any other receptors, enzymes, orserotonin-receptor subtypes at 1 μM, except for binding to the 5-HT2A receptor and the 5-HT2B receptor. Relenopride hydrochloride shows antagonist activity at the 5-HT2B receptor with an IC50 of 2.1 μM and no significant activity at the 5-HT2A receptor up to 10 μM. Relenopride hydrochloride shows no activity against serotonin-receptor subtypes 5-HT1B, 5-HT1D, or 5-HT2A at 1 nM to 10 μM, or for serotonin-receptor subtype 5-HT7 at 10 nM to 30 μM[1].

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

Molecular Weight

529.43

Formula

C₂₄H₃₁Cl₂FN₄O₄

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

References
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Product Name:
Relenopride hydrochloride
Cat. No.:
HY-16729A
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