A μ- and κ1-opioid receptor antagonist
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β-Funaltrexamine (hydrochloride)

Item No. 39901

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[[(5α,6β)-17-(cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxymorphinan-6-yl]amino]-4-oxo-2-butenoic acid, methyl ester, monohydrochloride
CAS Number
72786-10-8
Synonyms
  • β-FNA
  • Naltrexone fumarate methyl ester
Molecular Formula
C25H30N2O6 • HCl
Formula Weight
491.0
Purity
≥95%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly Soluble: 1-10 mg/ml
SMILES
O[C@]12[C@@]34C5=C(C[C@@]2([H])N(CC4)CC6CC6)C=CC(O)=C5O[C@@]3([H])[C@@H](CC1)NC(/C=C/C(OC)=O)=O.Cl
InChi Code
InChI=1S/C25H30N2O6.ClH/c1-32-20(30)7-6-19(29)26-16-8-9-25(31)18-12-15-4-5-17(28)22-21(15)24(25,23(16)33-22)10-11-27(18)13-14-2-3-14;/h4-7,14,16,18,23,28,31H,2-3,8-13H2,1H3,(H,26,29);1H/b7-6+;/t16-,18-,23+,24+,25-;/m1./s1
InChi Key
BIPHUOBUKMPSQR-NQGXHZAGSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

    $116

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    5 mg

    $549

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    Product Description

    β-Funaltrexamine is an irreversible μ- and κ1-opioid receptor antagonist (Kis = 0.3 and 0.2 nM, respectively).1,2 It is selective for μ- and κ1-opioid receptors over the δ-opioid receptor (Ki = 12.8 nM).1 β-Funaltrexamine also reversibly inhibits electricity-induced twitches of isolated guinea pig ileal longitudinal muscle strips (IC50 = 48 nM), indicating opioid agonist activity.2 In vivo, β-funaltrexamine (0.3 µg/animal, i.c.v.) inhibits conditioned place preference induced by the μ-opioid receptor agonist endomorphin 1 (Item No. 23280) in mice.3 It prevents decreases in urine output induced by the opioid agonists fentanyl, D-propoxyphene, buprenorphine, profadol, or bromadoline in water-loaded rats when administered at a dose of 40 mg/kg.4 β-Funaltrexamine also reduces hemokinin 1-induced increases in the latency to withdrawal in the tail-flick test in mice.5

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Toll, L., Berzetei-Gurske, I.P., Polgar, W.E., et al. Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications. NIDA Res. Monogr. 178, 440-466 (1998).

    2. Takemori, A.E., Larson, D.L., and Portoghese, P.S. The irreversible narcotic antagonistic and reversible agonistic properties of the fumaramate methyl ester derivative of naltrexone. Eur. J. Pharmacol. 70(4), 445-451 (1981).

    3. Wu, H.-e., MacDougall, R.S., Clithero, A.D., et al. Opposite conditioned place preference responses to endomorphin-1 and endomorphin-2 in the mouse. Neurosci. Lett. 365(3), 157-161 (2004).

    4. Hayes, A.G., Skingle, M., and Tyers, M.B. Evaluation of the receptor selectivities of opioid drugs by investigating the block of their effect on urine output by beta-funaltrexamine. J. Pharmacol. Exp. Ther. 240(3), 984-988 (1987).

    5. Fu, C.Y., Zhao, Y.L., Dong, L., et al. In vivo characterization of the effects of human hemokinin-1 and human hemokinin-1(4-11), mammalian tachykinin peptides, on the modulation of pain in mice. Brain Behav. Immun. 22(6), 850-860 (2008).