An M1 muscarinic receptor antagonist
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Drofenine (hydrochloride)

Item No. 43153

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
α-cyclohexyl-benzeneacetic acid, 2-(diethylamino)ethyl ester, monohydrochloride
CAS Number
548-66-3
Synonyms
  • Hexahydroadiphenine
  • NSC 42559
Molecular Formula
C20H31NO2 • HCl
Formula Weight
353.9
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥10 mg/mlEthanol: Soluble: ≥10 mg/ml
SMILES
O=C(C(C1CCCCC1)C2=CC=CC=C2)OCCN(CC)CC.Cl
InChi Code
InChI=1S/C20H31NO2.ClH/c1-3-21(4-2)15-16-23-20(22)19(17-11-7-5-8-12-17)18-13-9-6-10-14-18;/h5,7-8,11-12,18-19H,3-4,6,9-10,13-16H2,1-2H3;1H
InChi Key
WIELVDXKOYPANK-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    10 mg

    $98

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    25 mg

    $208

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    50 mg

    $258

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    100 mg

    $686

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    Product Description

    Drofenine is an antagonist of M1 muscarinic acetylcholine receptors (mAChRs).1 It inhibits carbachol-induced inositol phosphate accumulation in isolated guinea pig cortical slices, which endogenously express M1 muscarinic receptors (pA2 = 8.15). Drofenine also inhibits butyrylcholinesterase (BChE) isolated from human serum (Ki = 3 µM).2 It induces inward currents in whole-cell patch-clamp assays using HEK293 cells overexpressing transient receptor potential vanilloid 3 (TRPV3; EC50 = 205 µM).3 Drofenine (5 mg/kg twice per week) increases hepatic levels of α-smooth muscle actin (α-Sma) and collagen I in a mouse model of hepatic fibrosis induced by carbon tetrachloride (CCl4).4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Kunysz, E.L., Michel, A.D., and Whiting, R.L. Functional and direct binding studies using subtype selective muscarinic receptor antagonists. Br. J. Pharmacol. 93(3), 491-500 (1988).

    2. Bodur, E., Cokuğraş, A.N., and Tezcan, E.F. Inhibition effects of benactyzine and drofenine on human serum butyrylcholinesterase. Arch. Biochem. and Biophys. 386(1), 25-29 (2001).

    3. Deering-Rice, C.E., Mitchell, V.K., Romero, E.G., et al. Drofenine: A 2-APB analogue with greater selectivity for human TRPV3. Pharmacol. Res. Perspect. 2(5), e00062 (2014).

    4. Yan, L., Zhang, X., Fu, J., et al. Inhibition of the transient receptor potential vanilloid 3 channel attenuates carbon tetrachloride-induced hepatic fibrosis. Biochem. Biophys. Res. Commun. 558, 86-93 (2021).