PMID- 10528135
OWN - NLM
STAT- MEDLINE
DCOM- 19991209
LR  - 20190624
IS  - 0014-2999 (Print)
IS  - 0014-2999 (Linking)
VI  - 381
IP  - 1
DP  - 1999 Sep 17
TI  - Inhibition of plasma membrane monoamine transporters by beta-ketoamphetamines.
PG  - 63-9
AB  - Methcathinone and methylone, the beta-ketone analogues of methamphetamine and 
      3,4-methylenedioxymethamphetamine (MDMA), respectively, were tested for 
      neurotransmitter uptake inhibition in vitro. The beta-ketones were threefold less 
      potent than the nonketo drugs at inhibiting platelet serotonin accumulation, with 
      IC(50)'s of 34.6+/-4.8 microM and 5.8+/-0.7 microM, respectively. Methcathinone 
      and methylone were similar in potency to methamphetamine and MDMA at 
      catecholamine transporters individually expressed in transfected glial cells. For 
      dopamine uptake, IC(50)'s were 0.36+/-0.06 microM and 0.82+/-0.17 microM, 
      respectively; for noradrenaline uptake, IC(50) values were 0.51+/-0.10 microM and 
      1. 2+/-0.1 microM, respectively. In chromaffin granules, IC(50)'s for serotonin 
      accumulation were 112+/-8.0 microM for methcathinone and 166+/-12 microM for 
      methylone, 10-fold higher than the respective values for methamphetamine and 
      MDMA. Our results indicate that methcathinone and methylone potently inhibit 
      plasma membrane catecholamine transporters but only weakly inhibit the vesicle 
      transporter.
FAU - Cozzi, N V
AU  - Cozzi NV
AD  - Department of Pharmacology, East Carolina University School of Medicine, 
      Greenville, NC 27858, USA. ncozzi@brody.med.ecu.edu
FAU - Sievert, M K
AU  - Sievert MK
FAU - Shulgin, A T
AU  - Shulgin AT
FAU - Jacob, P 3rd
AU  - Jacob P 3rd
FAU - Ruoho, A E
AU  - Ruoho AE
LA  - eng
GR  - NS33650/NS/NINDS NIH HHS/United States
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
PT  - Research Support, U.S. Gov't, P.H.S.
PL  - Netherlands
TA  - Eur J Pharmacol
JT  - European journal of pharmacology
JID - 1254354
RN  - 0 (Dopamine Uptake Inhibitors)
RN  - 0 (Membrane Glycoproteins)
RN  - 0 (Membrane Transport Proteins)
RN  - 0 (Neuropeptides)
RN  - 0 (Propiophenones)
RN  - 0 (Vesicular Biogenic Amine Transport Proteins)
RN  - 10028-17-8 (Tritium)
RN  - 333DO1RDJY (Serotonin)
RN  - 386QA522QG (monomethylpropion)
RN  - 44RAL3456C (Methamphetamine)
RN  - 4764-17-4 (3,4-Methylenedioxyamphetamine)
RN  - L4I4B1R01F (methylone)
RN  - VTD58H1Z2X (Dopamine)
RN  - X4W3ENH1CV (Norepinephrine)
SB  - IM
MH  - 3,4-Methylenedioxyamphetamine/pharmacology
MH  - Animals
MH  - Cattle
MH  - Cell Membrane/*drug effects/metabolism
MH  - Chromaffin Cells/drug effects/metabolism
MH  - Dopamine/pharmacokinetics
MH  - Dopamine Uptake Inhibitors/*pharmacology
MH  - Humans
MH  - Membrane Glycoproteins/*drug effects
MH  - *Membrane Transport Proteins
MH  - Methamphetamine/analogs & derivatives/*pharmacology
MH  - *Neuropeptides
MH  - Norepinephrine/pharmacokinetics
MH  - Propiophenones/pharmacology
MH  - Serotonin/pharmacokinetics
MH  - Tritium
MH  - Tumor Cells, Cultured
MH  - Vesicular Biogenic Amine Transport Proteins
EDAT- 1999/10/21 09:00
MHDA- 2001/03/28 10:01
CRDT- 1999/10/21 09:00
PHST- 1999/10/21 09:00 [pubmed]
PHST- 2001/03/28 10:01 [medline]
PHST- 1999/10/21 09:00 [entrez]
AID - S0014-2999(99)00538-5 [pii]
AID - 10.1016/s0014-2999(99)00538-5 [doi]
PST - ppublish
SO  - Eur J Pharmacol. 1999 Sep 17;381(1):63-9. doi: 10.1016/s0014-2999(99)00538-5.