2-Chloro-2-phenylethylamine

β-Chlorophenethylamine
Names
IUPAC name
2-chloro-2-phenylethanamine
Other names
  • β-Chlorophenylethylamine
  • 2'-Chlorophenethylamine
Identifiers
3D model (JSmol)
ChemSpider
  • InChI=1S/C8H10ClN/c9-8(6-10)7-4-2-1-3-5-7/h1-5,8H,6,10H2
    Key: IUAYUYABWKLCER-UHFFFAOYSA-N
  • C1=CC=C(C=C1)C(CN)Cl
Properties
C8H10ClN
Molar mass 155.63 g·mol−1
Density 1.106
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
Infobox references

2-Chloro-2-phenylethylamine, also known as β-chlorophenethylamine, is an irreversible inhibitor or suicidal inhibitor of the enzyme dopamine-beta-monooxygenase,[1] a derivative of phenylethylamine in which the hydrogen atom in the β-position of the ethyl chain is replaced by a chlorine atom. This is a substituted phenylethylamine,[2][3][4] does not exhibit pronounced psychoactivity.

It is a related compound to N,N-dimethyl-2-chloro-2-phenylethylamine (DMEA), a precursor in organic synthesis.

Pharmacology

Inhibition of dopamine β-hydroxylase

2-Chloro-2-phenylethylamine is a suicide inhibitor of dopamine β-hydroxylase, which irreversibly inactivates them via covalent modification of the active site: a bound alpha-aminoacetophenone is formed, followed by an intramolecular redox reaction to form a ketone-derived radical cation as an inhibitory substance.[4][5]

See also

References

  1. ^ Bossard, M. J.; Klinman, J. P. (1990-04-05). "Use of isotope effects to characterize intermediates in mechanism-based inactivation of dopamine beta-monooxygenase by beta-chlorophenethylamine". The Journal of Biological Chemistry. 265 (10): 5640–5647. ISSN 0021-9258. PMID 2318829.
  2. ^ Weyler, W. "2-Chloro-2-phenylethylamine as a mechanistic probe and active site-directed inhibitor of monoamine oxidase from bovine liver mitochondria". Archives of Biochemistry and Biophysics. 255 (2): 400–408. doi:10.1016/0003-9861(87)90408-5. ISSN 0003-9861. PMID 3592682.
  3. ^ PubChem. "2'-Chlorophenethylamine". pubchem.ncbi.nlm.nih.gov. Retrieved 2026-02-07.
  4. ^ a b Mangold, J. B.; Klinman, J. P. (1984-06-25). "Mechanism-based inactivation of dopamine beta-monooxygenase by beta-chlorophenethylamine". The Journal of Biological Chemistry. 259 (12): 7772–7779. ISSN 0021-9258. PMID 6547439.
  5. ^ Bossard, M J; Klinman, J P (1990-04-05). "Use of isotope effects to characterize intermediates in mechanism-based inactivation of dopamine beta-monooxygenase by beta-chlorophenethylamine". Journal of Biological Chemistry. 265 (10): 5640–5647. doi:10.1016/S0021-9258(19)39410-4. ISSN 0021-9258.