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    Prucalopride Succinate (R-108512, R-93877)
    Prucalopride Succinate (R-108512, R-93877)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0973
    CAS #: 179474-85-2 Purity ≥98%

    Description: Prucalopride (R 108512; R108512; R 108512; trade names: Resolor; Resotran; Motegrity), a novel enterokinetic and benzofuran-based compound, is a novel, selective, high affinity 5-HT (serotonin) receptor agonist for 5-HT4A and 5-HT4B receptor with anti-idiopathic constipation activity. It inhibits 5-HT4A and 5-HT4B with Ki values of 2.5 nM and 8 nM, respectively, and exhibits >290-fold selectivity for 5-HT4A and 5-HT4B over other 5-HT receptor subtypes. Prucalopride induces contractions in a concentration-dependent manner with pEC50 of 7.5. Prucalopride significantly amplifies the rebound contraction of the guinea-pig proximal colon after electrical field stimulation. Prucalopride was approved by FDA in December 2018 to treat chronic idiopathic constipation.

    References: Eur J Pharmacol. 2001 Jun 29;423(1):71-83; Neurogastroenterol Motil. 2001 Oct;13(5):465-72.

    Related CAS#: 179474-81-8 (free base); 179474-80-7 (HCl)

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    Molecular Weight (MW)485.96 
    FormulaC18H26ClN3O3.C4H6O4 
    CAS No.179474-85-2 (Succinate); 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 97 mg/mL (199.6 mM)
    Water: 97 mg/mL (199.6 mM) 
    Ethanol: <1 mg/mL
    SMILES CodeO=C(O)CCC(O)=O.O=C(C1=C(OCC2)C2=C(N)C(Cl)=C1)NC3CCN(CCCOC)CC3
    SynonymsR-108512; R-108512; R108512; Prucalopride Succinate; R 108512; R108512; R 108512; Resolor; Resotran.


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    In Vitro

    In vitro activity: Prucalopride induces contractions in a concentration-dependent manner with pEC50 of 7.5. Prucalopride (1 mM) significantly amplifies the rebound contraction of the guinea-pig proximal colon after electrical field stimulation. Prucalopride induces relaxation of the rat oesophagus preparation of rat oesophagus tunica muscularis mucosae with pEC50 of 7.8, yielding a monophasic concentration–response curve. Prucalopride (0.1 μM) concentration-dependently increases the amplitude of submaximal cholinergic contractions and of acetylcholine release induced by electrical field stimulation in pig gastric circular muscle, and the effect is induced and enhanced IBMX (10 μM). Prucalopride (1 μM) significantly enhances the electrically induced cholinergic contractions in pig descending colon, and the facilitating effect is significantly enhanced by Rolipram.


    Kinase Assay: ucalopride is a novel enterokinetic compound and is the first representative of the benzofuran class. We set out to establish its pharmacological profile in various receptor binding and organ bath experiments. Receptor binding data have demonstrated prucalopride's high affinity to both investigated 5-HT(4) receptor isoforms, with mean pK(i) estimates of 8.60 and 8.10 for the human 5-HT(4a) and 5-HT(4b) receptor, respectively. From the 50 other binding assays investigated in this study only the human D(4) receptor (pK(i) 5.63), the mouse 5-HT(3) receptor (pK(i) 5.41) and the human sigma(1) (pK(i) 5.43) have shown measurable affinity, resulting in at least 290-fold selectivity for the 5-HT(4) receptor. Classical organ bath experiments were done using isolated tissues from the rat, guinea-pig and dog gastrointestinal tract, using various protocols. 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). Furthermore, it caused relaxation of a rat oesophagus preparation (pEC(50)=7.81+/-0.17), in a 5-HT(4) receptor antagonist sensitive manner. 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. It is concluded that prucalopride is a potent, selective and specific 5-HT(4) receptor agonist. As it is intended for treatment of intestinal motility disorders, it is important to note that prucalopride is devoid of anti-cholinergic, anticholinesterase or nonspecific inhibitory activity and does not antagonise 5-HT(2A), 5-HT(2B) and 5-HT(3) receptors or motilin or CCK(1) receptors.


    Cell Assay: Classical organ bath experiments were done using isolated tissues from the rat, guinea-pig and dog gastrointestinal tract, using various protocols. 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). Furthermore, it caused relaxation of a rat oesophagus preparation (pEC(50)=7.81+/-0.17), in a 5-HT(4) receptor antagonist sensitive manner.

    In VivoPrucalopride alters colonic contractile motility patterns in a dose-dependent fashion by stimulating high-amplitude clustered contractions in the proximal colon and by inhibiting contractile activity in the distal colon of fasted dogs. Prucalopride also causes a dose-dependent decrease in the time to the first giant migrating contraction (GMC); at higher doses of prucalopride, the first GMC generally occurres within the first half-hour after treatment. 
    Animal modelRat 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
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    ReferencesEur J Pharmacol. 2001 Jun 29;423(1):71-83; Neurogastroenterol Motil. 2001 Oct;13(5):465-72. 


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Prucalopride Succinate
    N Engl J Med. 2008 May 29;358(22):2344-54. N Engl J Med. 2008 May 29;358(22):2344-54.
    Prucalopride Succinate
    N Engl J Med. 2008 May 29;358(22):2344-54.

     


    Prucalopride Succinate
    N Engl J Med. 2008 May 29;358(22):2344-54.


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