PMID- 17070798
OWN - NLM
STAT- MEDLINE
DCOM- 20070124
LR  - 20231213
IS  - 0014-2999 (Print)
IS  - 0014-2999 (Linking)
VI  - 553
IP  - 1-3
DP  - 2006 Dec 28
TI  - Interactions between 3,4-methylenedioxymethamphetamine and sigma1 receptors.
PG  - 141-5
AB  - Methamphetamine and 3,4-methylenedioxymethamphetamine (MDMA) are structurally 
      similar and represent a serious and growing health threat. Earlier studies in our 
      laboratory have shown that methamphetamine interacts with sigma receptors and 
      that antagonism of these receptors can attenuate methamphetamine-induced 
      locomotor stimulation and neurotoxicity. However, no research exists which 
      characterizes the interaction between sigma receptors and MDMA. Therefore, the 
      goal of the present study was to determine whether sigma receptors are involved 
      in the actions of MDMA. In the first part of the study, competition and 
      saturation binding assays were performed to measure the interaction of MDMA with 
      sigma receptors. The receptor binding assays revealed that MDMA interacts 
      preferentially with the sigma(1) subtype, as compared to the sigma(2) subtype, 
      and that this interaction occurs in a competitive manner. The second part of the 
      study focused on behavioral measurements in male, Swiss Webster mice to determine 
      whether a selective sigma(1) receptor antagonist, BD1063 
      (1-[2-(3,4-dichlorophenyl)ethyl]-4-methylpiperazine, 0-30 mg/kg, i.p.) could 
      attenuate the locomotor stimulant actions of MDMA (0-50 mg/kg, i.p.). BD1063 
      alone had no effect on locomotor activity, but dose-dependently attenuated the 
      locomotor stimulant effects of MDMA and produced a significant shift to the right 
      in the MDMA dose response curve. Together, the data support the functional 
      relevance of the interaction of MDMA with sigma(1) receptors, and suggest that 
      these receptors are involved in the stimulant actions of MDMA.
FAU - Brammer, Matthew K
AU  - Brammer MK
AD  - Department of Pharmaceutical Sciences, College of Pharmacy, University of 
      Oklahoma Health Sciences Center, Oklahoma City, OK, 73190 USA.
FAU - Gilmore, Deborah L
AU  - Gilmore DL
FAU - Matsumoto, Rae R
AU  - Matsumoto RR
LA  - eng
GR  - R01 DA011979/DA/NIDA NIH HHS/United States
GR  - R01 DA013978/DA/NIDA NIH HHS/United States
GR  - DA11979/DA/NIDA NIH HHS/United States
GR  - DA13978/DA/NIDA NIH HHS/United States
PT  - Journal Article
PT  - Research Support, N.I.H., Extramural
PT  - Research Support, Non-U.S. Gov't
DEP - 20060928
PL  - Netherlands
TA  - Eur J Pharmacol
JT  - European journal of pharmacology
JID - 1254354
RN  - 0 (1-(2-(3,4-dichlorophenyl)ethyl)-4-methylpiperazine)
RN  - 0 (Central Nervous System Stimulants)
RN  - 0 (Dopamine Plasma Membrane Transport Proteins)
RN  - 0 (Hallucinogens)
RN  - 0 (Norepinephrine Plasma Membrane Transport Proteins)
RN  - 0 (Piperazines)
RN  - 0 (Receptors, sigma)
RN  - 0 (Serotonin Plasma Membrane Transport Proteins)
RN  - 0 (sigma-2 receptor)
RN  - KE1SEN21RM (N-Methyl-3,4-methylenedioxyamphetamine)
SB  - IM
MH  - Animals
MH  - Behavior, Animal/drug effects
MH  - Binding, Competitive/drug effects
MH  - Central Nervous System Stimulants/pharmacology
MH  - Dopamine Plasma Membrane Transport Proteins/metabolism
MH  - Dose-Response Relationship, Drug
MH  - Hallucinogens/*pharmacology
MH  - Male
MH  - Mice
MH  - Motor Activity/drug effects
MH  - N-Methyl-3,4-methylenedioxyamphetamine/*pharmacology
MH  - Norepinephrine Plasma Membrane Transport Proteins/metabolism
MH  - Piperazines/pharmacology
MH  - Protein Binding/drug effects
MH  - Radioligand Assay
MH  - Rats
MH  - Rats, Sprague-Dawley
MH  - Receptors, sigma/*drug effects
MH  - Serotonin Plasma Membrane Transport Proteins/metabolism
MH  - Sigma-1 Receptor
PMC - PMC1780037
MID - NIHMS14306
EDAT- 2006/10/31 09:00
MHDA- 2007/01/25 09:00
PMCR- 2007/12/28
CRDT- 2006/10/31 09:00
PHST- 2006/06/01 00:00 [received]
PHST- 2006/09/15 00:00 [revised]
PHST- 2006/09/19 00:00 [accepted]
PHST- 2006/10/31 09:00 [pubmed]
PHST- 2007/01/25 09:00 [medline]
PHST- 2006/10/31 09:00 [entrez]
PHST- 2007/12/28 00:00 [pmc-release]
AID - S0014-2999(06)01070-3 [pii]
AID - 10.1016/j.ejphar.2006.09.038 [doi]
PST - ppublish
SO  - Eur J Pharmacol. 2006 Dec 28;553(1-3):141-5. doi: 10.1016/j.ejphar.2006.09.038. 
      Epub 2006 Sep 28.