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

Prucalopride succinate (Synonyms: R-108512)

Cat. No.: HY-12694 Purity: 99.97%
Handling Instructions

Prucalopride succinate is a selective, high affinity 5-HT4 receptor agonist with pKi of 8.6/8.1 for 5-HT4a/4b.

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

Prucalopride succinate Chemical Structure

Prucalopride succinate Chemical Structure

CAS No. : 179474-85-2

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10 mM * 1 mL in DMSO USD 106 In-stock
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50 mg USD 96 In-stock
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200 mg USD 270 In-stock
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Description

Prucalopride succinate is a selective, high affinity 5-HT4 receptor agonist with pKi of 8.6/8.1 for 5-HT4a/4b. IC50 value: Target: 5-HT4 agonist in vitro: Prucalopride was a 5-HT(4) receptor agonist in the guinea-pig colon, as it induced contractions (pEC(50)=7.48+/-0.06; insensitive to a 5-HT(2A) or 5-HT(3) receptor antagonist, but inhibited by a 5-HT(4) receptor antagonist) as well as the facilitation of electrical stimulation-induced noncholinergic contractions (blocked by a 5-HT(4) receptor antagonist). Prucalopride did not cause relevant inhibition of 5-HT(2A), 5-HT(2B), or 5-HT(3), motilin or cholecystokinin (CCK(1)) receptor-mediated contractions, nor nicotinic or muscarinic acetylcholine receptor-mediated contractions, up to 10 microM [1]. in vivo: Rat microdialysis studies revealed that prucalopride maximally increased ACh and histamine levels in the prefrontal cortex at 5 and 10 mg/kg, whereas PRX-03140 significantly increased cortical histamine levels at 50 mg/kg, failing to affect ACh release at doses lower than 150 mg/kg [2].

IC50 & Target

5-HT4A Receptor

8.6 (pKi)

5-HT4B Receptor

8.1 (pKi)

Clinical Trial
Molecular Weight

485.96

Formula

C₂₂H₃₂ClN₃O₇

CAS No.

179474-85-2

SMILES

O=C(O)CCC(O)=O.O=C(C1=C(OCC2)C2=C(N)C(Cl)=C1)NC3CCN(CCCOC)CC3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 36 mg/mL (74.08 mM)

*"≥" means soluble, but saturation unknown.

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Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0578 mL 10.2889 mL 20.5778 mL
5 mM 0.4116 mL 2.0578 mL 4.1156 mL
10 mM 0.2058 mL 1.0289 mL 2.0578 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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Keywords:

PrucaloprideR-108512R108512R 1085125-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorInhibitorinhibitorinhibit

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Prucalopride succinate
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