Date published: 2026-2-27

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Bicifadine Hydrochloride (CAS 66504-75-4)

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Alternate Names:
1-(4-Methylphenyl)-3-azabicyclo[3.1.0]hexane Hydrochloride
Application:
Bicifadine Hydrochloride is an inhibitor of SLC5A2, 5-HT, and dopamine
CAS Number:
66504-75-4
Molecular Weight:
209.72
Molecular Formula:
C12H15N•HCl
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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Bicifadine Hydrochloride (BHCL) is a derivative of the amino acid tryptophan and a member of the phenylpiperidine class of compounds. It acts as an agonist at serotonin and dopamine receptors, as well as an antagonist at norepinephrine receptors. It is a potent inhibitor of SLC6A2 (noradrenalin transporter) (IC50 = 55 nM). Moreover, it may act to inhibit the activity of several enzymes, including monoamine oxidase and acetylcholinesterase. Bicifadine also displays inhibition of the 5-HT and dopamine transporters (IC50 values are 117 nM and 910 nM respectively) and exhibits antinociceptive and antiallodynic activity in rodent models of acute, persistent, and chronic pain.


Bicifadine Hydrochloride (CAS 66504-75-4) References

  1. Determination of the polymorphic forms of bicifadine hydrochloride by differential scanning calorimetry-thermogravimetric analysis, X-ray powder diffraction, attenuated total reflectance-infrared spectroscopy, and attenuated total reflectance-near-infrared spectroscopy.  |  McArdle, P., et al. 2005. Appl Spectrosc. 59: 1365-71. PMID: 16316514
  2. Near infrared spectroscopy in the development of solid dosage forms.  |  Räsänen, E. and Sandler, N. 2007. J Pharm Pharmacol. 59: 147-59. PMID: 17270069
  3. Preclinical compounds for the treatment of overactive bladder.  |  Giannitsas, K., et al. 2009. Expert Opin Ther Pat. 19: 107-17. PMID: 19441912
  4. Quantitative analysis of sulfathiazole polymorphs in ternary mixtures by attenuated total reflectance infrared, near-infrared and Raman spectroscopy.  |  Hu, Y., et al. 2010. J Pharm Biomed Anal. 53: 412-20. PMID: 20605386
  5. Crystal structures and Hirshfeld surface analyses of the di- and tri-hydrates of (5α,17E)-17-hydrazonoandrostan-3-ol: Significant differences in the hydrogen bonding patterns and supramolecular arrangements.  |  Gomes, LR., et al. 2018. Steroids. 140: 92-103. PMID: 30273694
  6. The oral analgesic efficacy of bicifadine hydrochloride in postoperative pain.  |  Wang, RI., et al. 1982. J Clin Pharmacol. 22: 160-4. PMID: 7096604
  7. Vaporization enthalpy and liquid vapor pressure of bicifadine using correlation gas chromatography  |  Umnahanant, P. 2020. The Journal of Chemical Thermodynamics. 150: 106204.
  8. Crystal structures, Hirshfeld surface analysis and PIXEL calculations of two chalcone derivatives, containing isopropoxy substituents: Importance of dispersion energy  |  Gomes, L. R., Low, J. N., & Wardell, J. L. 2021. Journal of Molecular Structure. 1237: 130354.

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

Bicifadine Hydrochloride, 10 mg

sc-210918
10 mg
$383.00