An L-type calcium channel inhibitor
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Pinaverium (bromide)

Item No. 40653

Technical Information
Formal Name
4-[(2-bromo-4,5-dimethoxyphenyl)methyl]-4-[2-[2-(6,6-dimethylbicyclo[3.1.1]hept-2-yl)ethoxy]ethyl]-morpholinium, monobromide
CAS Number
53251-94-8
Synonyms
  • PVB
Molecular Formula
C26H41BrNO4 • Br
Formula Weight
Purity
≥98%
Formulation
A solid
DMSO: Soluble: ≥10 mg/mlEthanol: Soluble: ≥10 mg/mlPBS (pH 7.2): Soluble: ≥10 mg/ml
SMILES
CC1(C2C(CCOCC[N+]3(CC4=C(Br)C=C(OC)C(OC)=C4)CCOCC3)CCC1C2)C.[Br-]
InChi Code
InChI=1S/C26H41BrNO4.BrH/c1-26(2)21-6-5-19(22(26)16-21)7-11-31-12-8-28(9-13-32-14-10-28)18-20-15-24(29-3)25(30-4)17-23(20)27;/h15,17,19,21-22H,5-14,16,18H2,1-4H3;1H/q+1;/p-1
InChi Key
IKGXLCMLVINENI-UHFFFAOYSA-M
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Pinaverium is an inhibitor of L-type voltage-gated calcium channels (Cav; IC50 = 1.5 µM in a patch-clamp assay using isolated rabbit jejunal smooth muscle cells).1,2 It binds to CHO cells expressing the Cav1.2 α1C-a or α1C-b subunits (Kis = 1.5 and 2.92 µM, respectively).1 Pinaverium inhibits contractions induced by acetylcholine (ACh; Item No. 23829) or potassium chloride in colonic circular muscle strips isolated from non-stressed or cold-restraint-stressed rats (IC50s = 0.91 and 1.66 µM for ACh, respectively, and 3.8 and 8.13 µM for potassium chloride, respectively) in a model of stress-induced smooth muscle contractility disorder.3 It increases survival and decreases pulmonary neutrophil infiltration in a mouse model of LPS-induced septic shock when administered at doses ranging from 1 to 10 mg/kg.4 Formulations containing pinaverium have been used in the treatment of irritable bowel syndrome (IBS).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Morel, N., Buryi, V., Feron, O., et alThe action of calcium channel blockers on recombinant L-type calcium channel α1-subunits. Br. J. Pharmacol. 125(5), 1005-1012 (1998).

    2. Beech, D.J., Mackenzie, I., Bolton, T.B., et alEffects of pinaverium on voltage-activated calcium channel currents of single smooth muscle cells isolated from the longitudinal muscle of the rabbit jejunum. Br. J. Pharmacol. 99(2), 374-378 (1990).

    3. Dai, Y., Liu, J.-X., Li, J.-X., et alEffect of pinaverium bromide on stress-induced colonic smooth muscle contractility disorder in rats. World J. Gastroenterol. 9(3), 557-561 (2003).

    4. Chen, X., Liu, Y., Dolin, H., et alPinaverium bromide attenuates lipopolysaccharide-induced excessive systemic inflammation via inhibiting neutrophil priming. J. Immunol. 206(8), 1858-1865 (2021).