A β-adrenergic receptor antagonist
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Carteolol (hydrochloride)

Item No. 23758

Technical Information
Formal Name
5-[3-[(1,1-dimethylethyl)amino]-2-hydroxypropoxy]-3,4-dihydro-2(1H)-quinolinone, monohydrochloride
CAS Number
51781-21-6
Synonyms
  • NSC 300906
  • OPC 1085
Molecular Formula
C16H24N2O3 • HCl
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
DMF: 14 mg/mlDMSO: 16 mg/mlEthanol: 11 mg/mlPBS (pH 7.2): 5 mg/ml
λmax
217, 251 nm
SMILES
O=C1CCC2=C(OCC(CNC(C)(C)C)O)C=CC=C2N1.Cl
InChi Code
InChI=1S/C16H24N2O3.ClH/c1-16(2,3)17-9-11(19)10-21-14-6-4-5-13-12(14)7-8-15(20)18-13;/h4-6,11,17,19H,7-10H2,1-3H3,(H,18,20);1H
InChi Key
FYBXRCFPOTXTJF-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Carteolol is an antagonist of β-adrenergic receptors (Kd = 13 nM).1,2 It blocks isoproterenol-induced increases in heart rate, contractile force, and blood pressure in vagotomized dogs (ED50s = 2.3, 3.1, and 1.8 µg/kg, respectively).3 The (R) and (S)-enantiomers of carteolol reduce intraocular pressure to similar levels in rabbits when applied topically as a 1% solution.4 Formulations containing carteolol have been used in the treatment of open-angle glaucoma.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Takayanagi, I., Ogishima, M., Koike, K., et alDose difference in beta-adrenergic blockers with intrinsic sympathomimetic action to block beta-adrenoceptors and induce sympathomimetic action. Gen. Pharmacol. 20(4), 417-419 (1989).

    2. Gwathmey, J.K., Kim, C.S., Haijar, R.J., et alCellular and molecular remodeling in a heart failure model treated with the β-blocker carteolol. Am. J. Physiol. 276(5 Pt. 2), H1678-H1690 (1999).

    3. Yabuochi, Y., and Kinoshita, D. Cardiovascular studies of 5-(3-tert-butylamino-2-hydroxy) propoxy-3,4-dihydrocarbostyril hydrochloride (OPC-1085), a new potent β-adrenergic blocking agent. Jpn. J. Pharmacol. 24(6), 853-861 (1974).

    4. Takayanagi, I., Haiwara, H., Koike, K., et alEffects of the R(+)- and S(−)-isomers of β-adrenoceptor blockers with intrinsic sympathomimetic activity, befunolol and carteolol, on rabbit intraocular pressure. Can. J. Physiol. Pharmacol. 69(8), 1243-1245 (1991).