PMID- 12969746
OWN - NLM
STAT- MEDLINE
DCOM- 20040806
LR  - 20190624
IS  - 0014-2999 (Print)
IS  - 0014-2999 (Linking)
VI  - 476
IP  - 1-2
DP  - 2003 Aug 22
TI  - Actions of amphetamine derivatives and cathinone at the noradrenaline 
      transporter.
PG  - 31-4
AB  - We have recently shown that methylenedioxymethamphetamine (MDMA), 
      methylenedioxyamphetamine (MDA), cathinone and methylenedioxyethylamphetamine 
      (MDEA) have a cocaine-like action to potentiate the contractile actions of 
      noradrenaline but not isoprenaline in the 1-Hz paced rat right ventricle. The 
      purpose of this study was to directly test the actions of these compounds at the 
      noradrenaline transporter. In rat left ventricular slices, potency (-log IC50) 
      values at inhibiting uptake of [3H]noradrenaline were: cocaine 6.16+/-0.15, 
      cathinone 6.03+/-0.16, MDMA 6.05+/-0.07, MDA 5.68+/-0.06 and MDEA 5.56+/-0.08. 
      MDEA and MDA were significantly less potent. In rat cerebral cortex membranes, 
      MDMA was significantly less potent at displacing [3H]nisoxetine binding; -log 
      EC50 values: cocaine 5.04+/-0.08, cathinone 5.40+/-0.14, MDA 4.66+/-0.11, MDEA 
      4.99+/-0.15, MDMA 4.22+/-0.07. The noradrenaline uptake studies showed that MDEA 
      was least potent: MDEA was also least potent functionally in the paced rat right 
      ventricle. The [3H]nisoxetine displacement studies did not compare with the 
      functional studies.
FAU - Cleary, Linda
AU  - Cleary L
AD  - Department of Physiology, Royal College of Surgeons in Ireland, 123 St. Stephen's 
      Green, Dublin 2, Ireland.
FAU - Docherty, James R
AU  - Docherty JR
LA  - eng
PT  - Comparative Study
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
PL  - Netherlands
TA  - Eur J Pharmacol
JT  - European journal of pharmacology
JID - 1254354
RN  - 0 (Adrenergic Uptake Inhibitors)
RN  - 0 (Alkaloids)
RN  - 0 (Amphetamines)
RN  - 0 (Norepinephrine Plasma Membrane Transport Proteins)
RN  - 0 (Slc6a2 protein, rat)
RN  - 0 (Symporters)
RN  - 01K63SUP8D (Fluoxetine)
RN  - 17NV064B2D (nisoxetine)
RN  - 4764-17-4 (3,4-Methylenedioxyamphetamine)
RN  - 540EI4406J (cathinone)
RN  - I5Y540LHVR (Cocaine)
RN  - KE1SEN21RM (N-Methyl-3,4-methylenedioxyamphetamine)
RN  - ML1I4KK67B (3,4-methylenedioxyethamphetamine)
SB  - IM
MH  - 3,4-Methylenedioxyamphetamine/*analogs & derivatives/pharmacology
MH  - Adrenergic Uptake Inhibitors/*pharmacology
MH  - Alkaloids/*pharmacology
MH  - Amphetamines/*pharmacology
MH  - Animals
MH  - Cerebral Cortex/metabolism
MH  - Cocaine/pharmacology
MH  - Competitive Bidding
MH  - Fluoxetine/*analogs & derivatives/pharmacology
MH  - In Vitro Techniques
MH  - Male
MH  - Myocardium/metabolism
MH  - N-Methyl-3,4-methylenedioxyamphetamine/pharmacology
MH  - Norepinephrine Plasma Membrane Transport Proteins
MH  - Rats
MH  - Rats, Wistar
MH  - Symporters/*metabolism
EDAT- 2003/09/13 05:00
MHDA- 2004/08/07 05:00
CRDT- 2003/09/13 05:00
PHST- 2003/09/13 05:00 [pubmed]
PHST- 2004/08/07 05:00 [medline]
PHST- 2003/09/13 05:00 [entrez]
AID - S0014299903021733 [pii]
AID - 10.1016/s0014-2999(03)02173-3 [doi]
PST - ppublish
SO  - Eur J Pharmacol. 2003 Aug 22;476(1-2):31-4. doi: 10.1016/s0014-2999(03)02173-3.