A δ2-opioid receptor inverse agonist
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Naltriben (mesylate)

Item No. 38979

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(4bS,8R,8aS,14bR)-7-(cyclopropylmethyl)-5,6,7,8,9,14b-hexahydro-4,8-methano-8aH-bisbenzofuro[3,2-e:2′,3′-g]isoquinoline-1,8a-diol, methanesulfonate
CAS Number
122517-78-6
Synonyms
  • NIH 10924
  • NTB
Molecular Formula
C26H25NO4 • CH3SO3H
Formula Weight
511.6
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble
SMILES
O[C@@]12[C@@]([C@](O3)([H])C(OC4=CC=CC=C54)=C5C2)(CC6)C(C3=C7O)=C(C=C7)C[C@@]1([H])N6CC8CC8.C[S](=O)(O)=O
InChi Code
InChI=1S/C26H25NO4.CH4O3S/c28-18-8-7-15-11-20-26(29)12-17-16-3-1-2-4-19(16)30-22(17)24-25(26,21(15)23(18)31-24)9-10-27(20)13-14-5-6-14;1-5(2,3)4/h1-4,7-8,14,20,24,28-29H,5-6,9-13H2;1H3,(H,2,3,4)/t20-,24+,25+,26-;/m1./s1
InChi Key
XRRFZOCDAWPIBB-IDRHMUJXSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Certificates of Analysis & Batch Specific Data

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    1 mg

    $52

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    5 mg

    $195

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    10 mg

    $362

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    25 mg

    $646

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    Product Description

    Naltriben is an inverse agonist of δ2-opioid receptors (Ki = 0.013 nM in CHO-DG44 cells expressing the mouse receptor).1,2 It is selective for δ2-opioid receptors over κ- and μ-opioid receptors (Kis = 13 and 12 nM in PC12 and COS-7 cells expressing the mouse and rat receptors, respectively). Naltriben (1 and 10 µM) induces axonal retraction in primary mouse hippocampal neurons under both normoxic and hypoxic conditions.3 It is also an activator of transient receptor potential melastatin 7 (TRPM7) and induces calcium influx in HEK293 cells expressing mouse TRPM7 (EC50 = 20.7 µM).4 It reduces self-administration of alcohol or alcohol mixed with saccharin or quinine in alcohol-preferring rats when administered at a dose of 6 mg/kg.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Raynor, K., Kong, H., Chen, Y., et al. Pharmacological characterization of the cloned κ-, δ-, and μ-opioid receptors. Mol. Pharm. 45(2), 330-334 (1994).

    2. Krishnan-Sarin, S., Portoghese, P.S., Li, T.K., et al. The delta2-opioid receptor antagonist naltriben selectively attenuates alcohol intake in rats bred for alcohol preference. Pharmacol. Biochem. Behav. 52(1), 153-159 (1995).

    3. Turlova, E., Ji, D., Deurloo, M., et al. Hypoxia-induced neurite outgrowth involves regulation through TRPM7. Mol. Neurobiol. 60(2), 836-850 (2023).

    4. Hofmann, T., Schäfer, S., Linseisen, M., et al. Activation of TRPM7 channels by small molecules under physiological conditions. Pflugers Arch. 466(12), 2177-2189 (2014).