A 5-HT2B receptor antagonist
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RS 127445 (hydrochloride)

Item No. 23451

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-(4-fluoro-1-naphthalenyl)-6-(1-methylethyl)-2-pyrimidinamine, monohydrochloride
CAS Number
199864-86-3
Molecular Formula
C17H16FN3 • HCl
Formula Weight
317.8
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 30 mg/mlEthanol:PBS (pH 7.2) (1:3): 0.25 mg/ml
λmax
223, 309 nm
SMILES
FC1=CC=C(C2=CC(C(C)C)=NC(N)=N2)C3=C1C=CC=C3.Cl
InChi Code
InChI=1S/C17H16FN3.ClH/c1-10(2)15-9-16(21-17(19)20-15)13-7-8-14(18)12-6-4-3-5-11(12)13;/h3-10H,1-2H3,(H2,19,20,21);1H
InChi Key
MKJPYBJBPRFMHL-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $120

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    10 mg

    $219

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    Product Description

    RS 127445 is an orally bioavailable and potent antagonist of the serotonin (5-HT) receptor subtype 5-HT2B (Ki = 0.32 nM).1 It is selective for 5-HT2B over other 5-HT receptor subtypes (Ki = >3 μM for 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2C, 5-HT3, 5-HT5, and 5-HT6). RS 127445 reduces contraction of rat isolated stomach fundus (pA2 = 9.5) and lowers intracellular increases in calcium (IC50 = 0.04 nM) induced by 5-HT (Item No. 14332). It also blocks (±)-α-methyl-5-HT-induced relaxation of isolated rat jugular veins (pA2 = 9.95). RS 127445 (1-30 mg/kg) reduces peristaltic frequency and fecal output in mice in a dose-dependent manner.2 Systemic administration of RS 127445 (0.16 mg/kg) reduces basal, but not cocaine-induced, dopamine outflow in the nucleus accumbens of rats and decreases hyperlocomotion induced by cocaine (Item Nos. ISO60176 | 16186 | 22165) or quinpirole.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Bonhaus, D.W., Flippin, L.A., Greenhouse, R.J., et al. RS-127445: A selective, high affinity, orally bioavailable 5-HT2B receptor antagonist. Br. J. Pharmacol. 127(5), 1075-1082 (1999).

    2. Bassil, A.K., Taylor, C.M., Bolton, V.J., et al. Inhibition of colonic motility and defecation by RS-127445 suggests an involvement of the 5-HT2B receptor in rodent large bowel physiology. Br. J. Pharmacol. 158(1), 252-258 (2009).

    3. Devroye, C., Cathala, A., Di Marco, B., et al. Central serotonin2B receptor blockade inhibits cocaine-induced hyperlocomotion independently of changes of subcortical dopamine outflow. Neuropharmacology 97, 329-337 (2015).