4-Bromo-α-pyrrolidinopentiophenone, also known as 4Br-alpha-PVP, 4Br-α-PVP, or 4-bromo-α-pyrrolidinvalerophenone, is a stimulant drug belonging to the family of substituted cathinones and α-propylphenethylamines (and the related class of pyrrolidinophenones). It, along with other closely related compounds, was designated by the code ‘O-’ and is known as O-2419.
Pharmacology
Pharmacodynamics 4-Bromo-α-PVP is a serotonin–norepinephrine–dopamine reuptake inhibitor; its affinity value (Ki) for the serotonin, norepinephrine and dopamine transporters is 830 ± 190, 386 ± 53 and 51.0 ± 6.7 nM respectively; the IC50 values for the three transporters were 39.5 ± 7.5 nM for DAT, 1050 ± 90 nM for SERT and 83.0 ± 30 nM for NET.
It is interesting to note that 4-bromo-α-PVP did not induce anxiety-like behaviour in mice, in contrast to other known para- and meta-halogen-substituted (i.e. at the 3- and 4-positions of the benzene ring of cathinones) compounds such as 3-Cl-α-PVP, 4-F-α-PVP; this may be due to a serotonin background that is significantly higher than that of other halo- or other cathinone derivatives, although this requires further investigation. In a study of horizontal motor activity at a moderate dose (10 mg/kg): The effect of 4-bromo-α-PVP on mice wore off the quickest — the increased activity subsided completely in less than 60 minutes; at a high dose (25 mg/kg), a severe, prolonged effect set in, causing the animals to run frantically for over an hour. A conditioned place preference test was also conducted; 4-bromo-α-PVP, like other cathinone derivatives, caused severe dependence even at low doses (2.5 mg/kg); at the maximum dose (25 mg/kg), the findings indicative of addiction were exacerbated.
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