A 5-HT1A and α2-AR antagonist
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Spiroxatrine

Item No. 33415

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
8-[(2,3-dihydro-1,4-benzodioxin-2-yl)methyl]-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one
CAS Number
1054-88-2
Synonyms
  • R-5188
Molecular Formula
C22H25N3O3
Formula Weight
379.5
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Acetontrile: Slightly soluble: 0.1-1 mg/mlDMSO: Slightly soluble: 0.1-1 mg/ml
SMILES
O=C(NCN1C2=CC=CC=C2)C31CCN(CC4OC5=C(OC4)C=CC=C5)CC3
InChi Code
InChI=1S/C22H25N3O3/c26-21-22(25(16-23-21)17-6-2-1-3-7-17)10-12-24(13-11-22)14-18-15-27-19-8-4-5-9-20(19)28-18/h1-9,18H,10-16H2,(H,23,26)
InChi Key
JVGBTTIJPBFLTE-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $87

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    10 mg

    $139

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    25 mg

    $283

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    50 mg

    $435

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    Product Description

    Spiroxatrine is an antagonist of the serotonin (5-HT) receptor subtype 5-HT1A (Ki = 3 nM) and α2-adrenergic receptors (α2-ARs; Kis = 28, 1.3, and 1.8 nM for α2A, α2B, and α2C, respectively).1 It is selective for these receptors over 5-HT1D (Ki = 2 µM) and 5-HT1B at 10 µM. Spiroxatrine also induces calcium mobilization in CHO cells expressing the human nociception opioid peptide (NOP) receptor (EC50 = 323 nM).2 It inhibits decreases in mean arterial pressure induced by urapidil in anesthetized normotensive cats when administered at doses of 3 or 10 nmol/kg.3 Spiroxatrine (2.5 and 5 mg/kg) induces catalepsy and catatonia in rats.4 It enhances reductions in ethanol intake induced by fluoxetine in alcohol-preferring rats.5

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Sorbi, C., Tait, A., Battisti, U.M., et al. Spiroxatrine derivatives towards 5-HT1A receptor selectivity. Pharmacol. Rep. 72(2), 427-434 (2020).

    2. Corrado, S., Battisti, U.M., Sorbi, C., et al. Synthesis and structure-activity relationships of triazaspirodecanone derivatives as nociceptin/orphanin FQ receptor ligands. Chem. Biol. Drug Des. 86(4), 447-458 (2015).

    3. Kolassa, N., Beller, K.D., and Sanders, K.H. Involvement of brain 5-HT1A receptors in the hypotensive response to urapidil. Am. J. Cardiol. 64(7), 7D-10D (1989).

    4. Costall, B., and Naylor, R.J. On catalepsy and catatonia and the predictability of the catalepsy test for neuroleptic activity. Psychopharmacologia 34(3), 233-241 (1974).

    5. McBride, W.J., Murphy, J.M., Lumeng, L., et al. Spiroxatrine augments fluoxetine-induced reduction of ethanol intake by the P line of rats. Pharmacol. Biochem. Behav. 34(2), 381-386 (1989).