An α-AR antagonist and vasoactive compound
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Buflomedil (hydrochloride)

Item No. 31184

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-(1-pyrrolidinyl)-1-(2,4,6-trimethoxyphenyl)-1-butanone, monohydrochloride
CAS Number
35543-24-9
Synonyms
  • LL-1656
Molecular Formula
C17H25NO4 • HCl
Formula Weight
343.9
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 3mg/mLDMSO: 2mg/mLEthanol: 3mg/mLPBS (pH 7.2): 10mg/mL
SMILES
COC1=CC(OC)=C(C(CCCN2CCCC2)=O)C(OC)=C1.Cl
InChi Code
InChI=1S/C17H25NO4.ClH/c1-20-13-11-15(21-2)17(16(12-13)22-3)14(19)7-6-10-18-8-4-5-9-18;/h11-12H,4-10H2,1-3H3;1H
InChi Key
ZDPACSAHMZADFZ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 g

    $103

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    10 g

    $173

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    Product Description

    Buflomedil is a non-selective antagonist of α-adrenergic receptors (α-ARs) and vasoactive compound.1,2,3,4 It binds to rat α1A- and α1B-ARs (Kis = 4.06 and 6.84 µM, respectively) and human platelet α2-ARs (IC50 = 1 µM) in radioligand binding assays.1,2 Buflomedil (0.06-60 µM) inhibits contraction of isolated canine saphenous veins induced by phenylephrine, clonidine (Item No. 15949), sympathetic nerve stimulation, or norepinephrine.3 It inhibits ADP-, collagen-, or epinephrine-induced aggregation of isolated human platelets when used at a concentration of 100 µM.2 Buflomedil (10 mg/kg) reduces hippocampal neuronal cell death in a rat model of carotid clamping-induced ischemia-reperfusion injury.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Tang, L.-M., Cheng, J.-T., and Tong, Y.-C. Inhibitory effect of buflomedil on prostate α1A adrenoceptor in the Wistar rat. Neurosci. Lett. 367(2), 224-227 (2004).

    2. Ryckewaert, J.J., Maurel, A., and Marguerie, G. In vitro studies of the effect of buflomedil on platelet responsiveness. Haemostasis 20(3), 181-191 (1990).

    3. Clissold, S.P., and Lynch, S.S., E.M. Buflomedil. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in peripheral and cerebral vascular diseases. Drugs 33(5), 430-460 (1987).

    4. Briguglio, F.S., Mondello, M.R., Galluzzo, M., et al. Protective effect of buflomedil in a rat model of moderate cerebral ischemia. Arzneimittelforschung. 55(8), 437-442 (2005).