Citation
Baumann, Michael H., et al. "Powerful Cocaine-like Actions of 3,4-methylenedioxypyrovalerone (MDPV), a Principal Constituent of Psychoactive 'bath Salts' Products." Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology, vol. 38, no. 4, 2013, pp. 552-62.
Baumann MH, Partilla JS, Lehner KR, et al. Powerful cocaine-like actions of 3,4-methylenedioxypyrovalerone (MDPV), a principal constituent of psychoactive 'bath salts' products. Neuropsychopharmacology. 2013;38(4):552-62.
Baumann, M. H., Partilla, J. S., Lehner, K. R., Thorndike, E. B., Hoffman, A. F., Holy, M., Rothman, R. B., Goldberg, S. R., Lupica, C. R., Sitte, H. H., Brandt, S. D., Tella, S. R., Cozzi, N. V., & Schindler, C. W. (2013). Powerful cocaine-like actions of 3,4-methylenedioxypyrovalerone (MDPV), a principal constituent of psychoactive 'bath salts' products. Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology, 38(4), 552-62. https://doi.org/10.1038/npp.2012.204
Baumann MH, et al. Powerful Cocaine-like Actions of 3,4-methylenedioxypyrovalerone (MDPV), a Principal Constituent of Psychoactive 'bath Salts' Products. Neuropsychopharmacology. 2013;38(4):552-62. PubMed PMID: 23072836.
TY - JOUR
T1 - Powerful cocaine-like actions of 3,4-methylenedioxypyrovalerone (MDPV), a principal constituent of psychoactive 'bath salts' products.
AU - Baumann,Michael H,
AU - Partilla,John S,
AU - Lehner,Kurt R,
AU - Thorndike,Eric B,
AU - Hoffman,Alexander F,
AU - Holy,Marion,
AU - Rothman,Richard B,
AU - Goldberg,Steven R,
AU - Lupica,Carl R,
AU - Sitte,Harald H,
AU - Brandt,Simon D,
AU - Tella,Srihari R,
AU - Cozzi,Nicholas V,
AU - Schindler,Charles W,
Y1 - 2012/10/17/
PY - 2012/10/18/entrez
PY - 2012/10/18/pubmed
PY - 2013/10/30/medline
SP - 552
EP - 62
JF - Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology
JO - Neuropsychopharmacology
VL - 38
IS - 4
N2 - The abuse of psychoactive 'bath salts' containing cathinones such as 3,4-methylenedioxypyrovalerone (MDPV) is a growing public health concern, yet little is known about their pharmacology. Here, we evaluated the effects of MDPV and related drugs using molecular, cellular, and whole-animal methods. In vitro transporter assays were performed in rat brain synaptosomes and in cells expressing human transporters, while clearance of endogenous dopamine was measured by fast-scan cyclic voltammetry in mouse striatal slices. Assessments of in vivo neurochemistry, locomotor activity, and cardiovascular parameters were carried out in rats. We found that MDPV blocks uptake of [(3)H]dopamine (IC(50)=4.1 nM) and [(3)H]norepinephrine (IC(50)=26 nM) with high potency but has weak effects on uptake of [(3)H]serotonin (IC(50)=3349 nM). In contrast to other psychoactive cathinones (eg, mephedrone), MDPV is not a transporter substrate. The clearance of endogenous dopamine is inhibited by MDPV and cocaine in a similar manner, but MDPV displays greater potency and efficacy. Consistent with in vitro findings, MDPV (0.1-0.3 mg/kg, intravenous) increases extracellular concentrations of dopamine in the nucleus accumbens. Additionally, MDPV (0.1-3.0 mg/kg, subcutaneous) is at least 10 times more potent than cocaine at producing locomotor activation, tachycardia, and hypertension in rats. Our data show that MDPV is a monoamine transporter blocker with increased potency and selectivity for catecholamines when compared with cocaine. The robust stimulation of dopamine transmission by MDPV predicts serious potential for abuse and may provide a mechanism to explain the adverse effects observed in humans taking high doses of 'bath salts' preparations.
SN - 1740-634X
UR - https://www.unboundmedicine.com/medline/citation/23072836/Powerful_cocaine_like_actions_of_34_methylenedioxypyrovalerone__MDPV__a_principal_constituent_of_psychoactive_'bath_salts'_products_
L2 - https://www.ncbi.nlm.nih.gov/pmc/articles/pmid/23072836/
DB - PRIME
DP - Unbound Medicine
ER -