A β2-adrenergic receptor agonist
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Procaterol (hydrochloride)

Item No. 28479

Technical Information
Formal Name
rel-8-hydroxy-5-[(1R,2S)-1-hydroxy-2-[(1-methylethyl)amino]butyl]-2(1H)-quinolinone, monohydrochloride
CAS Number
62929-91-3
Molecular Formula
C16H22N2O3 • HCl
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
DMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:4): 0.20 mg/ml
λmax
237, 262, 297 nm
SMILES
O=C1C=CC2=C([C@@H]([C@H](NC(C)C)CC)O)C=CC(O)=C2N1.Cl
InChi Code
InChI=1S/C16H22N2O3.ClH/c1-4-12(17-9(2)3)16(21)11-5-7-13(19)15-10(11)6-8-14(20)18-15;/h5-9,12,16-17,19,21H,4H2,1-3H3,(H,18,20);1H/t12-,16+;/m1./s1
InChi Key
AEQDBKHAAWUCMT-KKJWGQAZSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Procaterol is an agonist of β2-adrenergic receptors (β2-ARs).1 It binds to (Kd = 46 pM), and is selective for, β2-ARs over β1-ARs (Kd = 4,000 pM). Procaterol binds more potently to β2-ARs in isolated guinea pig lung than to β1-ARs in isolated guinea pig cardiac ventricle in the presence (IC50s = 175 and 1,660 nM, respectively) and absence of GTP (Item No. 16060; IC50s = 55.1 and 1,660 nM, respectively).2 It inhibits contractions induced by acetylcholine (Item No. 23829) in isolated guinea pig trachea (EC50 = 10.5 nM).3 In vivo, procaterol inhibits histamine-induced airflow obstruction in a guinea pig model of ovalbumin-sensitized asthma when administered via inhalation at a dose of 10 µg/ml.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Marullo, S., Emorine, L.J., Strosberg, A.D., et alSelective binding of ligands to β1, β2 or chimeric β1/β2-adrenergic receptors involves multiple subsites. EMBO J. 9(5), 1471-1476 (1990).

    2. Kikkawa, H., Naito, K., and Ikezawa, K. Tracheal relaxing effects and β2-selectivity of TA-2005, a newly developed bronchodilating agent, in isolated guinea pig tissues. Jpn. J. Pharmacol. 57(2), 175-185 (1991).

    3. Yoshizaki, S., Tanimura, K., Tamada, S., et alSympathomimetic amines having a carbostyril nucleus. J. Med. Chem. 19(9), 1138-1142 (1976).

    4. Mirza, Z.N., Tokuyama, K., Arakawa, H., et alInhaled procaterol inhibits histamine-induced airflow obstruction and microvascular leakage in guinea-pig airways with allergic inflammation. Clin. Exp. Allergy 28(5), 644-652 (1998).