An α1- and α2-adrenergic receptor antagonist
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Tolazoline (hydrochloride)

Item No. 18865

Technical Information
Formal Name
4,5-dihydro-2-(phenylmethyl)-1H-imidazole, monohydrochloride
CAS Number
59-97-2
Molecular Formula
C10H12N2 • HCl
Formula Weight
Purity
≥95%
Formulation
A crystalline solid
DMF: 20 mg/mlDMSO: 25 mg/mlEthanol: 25 mg/mlPBS (pH 7.2): 10 mg/ml
SMILES
C1(CC2=NCCN2)=CC=CC=C1.Cl
InChi Code
InChI=1S/C10H12N2.ClH/c1-2-4-9(5-3-1)8-10-11-6-7-12-10;/h1-5H,6-8H2,(H,11,12);1H
InChi Key
RHTNTTODYGNRSP-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Tolazoline is an α1-adrenergic receptor (α1-AR; IC50 = 3,200 nM) and α2-AR antagonist (Kis = 112, 1,230, 354, and 173 nM for α2A, α2B-, α2C-, and α2D-ARs, respectively).1,2 Tolazoline inhibits α-AR agonist-induced contractions in isolated human corpus cavernosum smooth muscle (IC50 = 0.1 µM).3 It also lowers vascular resistance in isolated perfused porcine skin flaps (IPPSFs) preconstricted by norepinephrine with an EC50 value of 288 nM.4 Formulations containing tolazoline have been used in veterinary medicine to reverse the analgesia and sedation induced by xylazine in horses.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Megens, A.A.H.P., Leysen, J.E., Awouters, F.H.L., et alFurther validation of in vivo and in vitro pharmacological procedures for assessing the ɑ2/ɑ1-selectivity of test compounds: (1) ɑ-adrenoceptor antagonists. Eur. J. Pharmacol. 129(1-2), 49-55 (1986).

    2. Schwartz, D.D., and Clark, T.P. Selectivity of atipamezole, yohimbine and tolazoline for alpha-2 adrenergic receptor subtypes: Implications for clinical reversal of alpha-2 adrenergic receptor mediated sedation in sheep. J. Vet. Pharmacol. Ther. 21(5), 342-347 (1998).

    3. Costa, P., Soulie-Vassal, M.L., Sarrazin, B., et alAdrenergic receptors on smooth muscle cells isolated from human penile corpus cavernosum. J. Urol. 150(3), 859-863 (1993).

    4. Rogers, R.A., and Riviere, J.E. Pharmacologic modulation of the cutaneous vasculature in the isolated perfused porcine skin flap. J. Pharm. Sci. 83(12), 1682-1689 (1994).