An α1-AR antagonist
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Bunazosin (hydrochloride)

Item No. 45574

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-[4-(4-amino-6,7-dimethoxy-2-quinazolinyl)hexahydro-1H-1,4-diazepin-1-yl]-1-butanone, monohydrochloride
CAS Number
52712-76-2
Synonyms
  • DDQ
  • E-643
Molecular Formula
C19H27N5O3 • HCl
Formula Weight
409.9
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Slightly soluble: 0.1-1 mg/ml
SMILES
O=C(CCC)N1CCN(CCC1)C2=NC3=C(C=C(C(OC)=C3)OC)C(N)=N2.Cl
InChi Code
InChI=1S/C19H27N5O3.ClH/c1-4-6-17(25)23-7-5-8-24(10-9-23)19-21-14-12-16(27-3)15(26-2)11-13(14)18(20)22-19;/h11-12H,4-10H2,1-3H3,(H2,20,21,22);1H
InChi Key
NBGBEUITCPENLJ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

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    10 mg

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    25 mg

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    Product Description

    Bunazosin is an antagonist of the α1-adrenergic receptor (α1-AR; Kd = 0.59 nM).1 It reduces glutamate-induced decreases in viability in primary rat retinal cells when used at concentrations of 1 and 10 µM.2 Ocular instillation of bunazosin (0.01%) prevents phenylephrine- or endothelin-1-induced constriction of retinal arteries in rabbits. It also prevents reductions in refractive error and increases in axial elongation in a mouse model of lens-induced myopia.3 Formulations containing bunazosin have been used in the treatment of glaucoma and ocular hypertension.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Hata, F., Kondo, E., Kondo, S., et al. Characteristics of [3H]E-643-binding to alpha adrenoceptors. Japan J. Pharmacol. 32(1), 181-187 (1982).

    2. Hara, H., Ichikawa, M., Oku, H., et al. Bunazosin, a selective α1-adrenoceptor antagonist, as an anti-glaucoma drug: Effects on ocular circulation and retinal neuronal damage. Cardiovasc. Res. 23(1), 43-56 (2005).

    3. Jeong, H., Lee, D., Jiang, X., et al. Topical application of bunazosin hydrochloride suppresses myopia progression with an increase in choroidal blood perfusion. Invest. Ophthalmol. Vis. Sci. 64(14), 15 (2023).