An α2-AR antagonist
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SKF 86466 (hydrochloride)

Item No. 11953

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6-chloro-2,3,4,5-tetrahydro-3-methyl-1H-3-benzazepine, monohydrochloride
CAS Number
86129-54-6
Molecular Formula
C11H14ClN • HCl
Formula Weight
232.2
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: 20 mg/mlWater: 20 mg/ml
λmax
217, 223 nm
SMILES
ClC1=C2C(CCN(C)CC2)=CC=C1.Cl
InChi Code
InChI=1S/C11H14ClN.ClH/c1-13-7-5-9-3-2-4-11(12)10(9)6-8-13;/h2-4H,5-8H2,1H3;1H
InChi Key
JKQKVNMNAIFCFS-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $120

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    10 mg

    $169

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    25 mg

    $378

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    Product Description

    SKF 86466 is an antagonist of α2-adrenergic receptors (α2-ARs; Kis = 9.4, 16, and 20 nM for α2A, α2B, and α2C receptors, respectively).1 It is selective for α2-ARs over α1-ARs (Kis = 449, 485, and 126 nM for α1A, α1B, and α1D receptors, respectively). SKF 86466 inhibits contractions in rabbit aorta and canine saphenous vein induced by norepinephrine or B-HT 920 (Item No. 14177), respectively (KBs = 600 and 42 nM, respectively). It decreases diastolic blood pressure in DOCA-salt hypertensive, spontaneously hypertensive, and two kidney-one clip (2K-1C) renal hypertensive rats when administered at a dose of 2 mg/kg, i.v.2 SKF 86466 (1 mg/kg) reduces muscle rigidity induced by reserpine (Item No. 19474) in a mouse model of Parkinson’s disease.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ruffolo, R.R., Jr., Bondinell, W., and Hieble, J.P. α- and β-adrenoceptors: From the gene to the clinic. 2. Structure-activity relationships and therapeutic applications. J. Med. Chem. 38(19), 3681-3716 (1995).

    2. Roesler, J.M., McCafferty, J.P., DeMarinis, R.M., et al. Characterization of the antihypertensive activity of SK&F 86466, a selective alpha-2 antagonist, in the rat. J. Pharmacol. Exp. Ther. 236(1), 1-7 (1986).

    3. Tanabe, M., Hashimoto, M., and Ono, H. Imidazoline I1 receptor-mediated reduction of muscle rigidity in the reserpine-treated murine model of Parkinson’s disease. Eur. J. Pharmacol. 589(1-3), 102-105 (2008).