PMID- 23026265
OWN - NLM
STAT- MEDLINE
DCOM- 20130108
LR  - 20191210
IS  - 1879-3169 (Electronic)
IS  - 0378-4274 (Linking)
VI  - 214
IP  - 3
DP  - 2012 Nov 15
TI  - Estrogenic effects and their action mechanism of the major active components of 
      party pill drugs.
PG  - 339-47
LID - S0378-4274(12)01310-0 [pii]
LID - 10.1016/j.toxlet.2012.09.014 [doi]
AB  - Benzylpiperazine (BZP) and trifluoromethylphenylpiperazine (TFMPP) are commonly 
      used constituents of party pill drugs. They are reported to induce psychoactive 
      effects such as euphoria and provide effects similar with other illicit drugs 
      such as methylenedioxymethamphetamine (MDMA). A great deal of evidence has proven 
      that party pills, as alternatives for MDMA, exert harmful effects on users. 
      However, their toxicological effects have not been fully understood and endocrine 
      disruptive effects are still unknown. In this study, we identified estrogenic 
      effects of BZP and TFMPP by using in vitro and in vivo assays. BZP and TFMPP 
      stimulated cell proliferation in a dose-dependent manner, while co-treatment with 
      tamoxifen and BZP or TFMPP showed a decrease of E(2)-induced cell proliferation. 
      In an estrogen sensitive reporter gene assay, BZP and TFMPP significantly 
      increased transcriptional activities of party pill drugs. In addition, ER-related 
      genes, PR and pS2, were significantly stimulated by BZP and TFMPP. These results 
      indicated that BZP and TFMPP could have estrogenic activities related to the 
      ER-mediated pathway. Unlike the in vitro assay results, BZP and TFMPP did not 
      show significant effects on weight increase in a rodent uterotrophic assay. 
      However, further studies would be necessary to verify the estrogenic activities 
      of BZP and TFMPP by a chronic exposure animal study.
CI  - Copyright (c) 2012 Elsevier Ireland Ltd. All rights reserved.
FAU - Min, Cho Rong
AU  - Min CR
AD  - School of Pharmacy, Sungkyunkwan University, 300 Cheoncheon dong, Jangan-gu, 
      Suwon, Kyeonggi-do 440-746, South Korea.
FAU - Kim, Mi Jie
AU  - Kim MJ
FAU - Park, Yong Joo
AU  - Park YJ
FAU - Kim, Ha Ryong
AU  - Kim HR
FAU - Lee, Soo Yeun
AU  - Lee SY
FAU - Chung, Kyu Hyuck
AU  - Chung KH
FAU - Oh, Seung Min
AU  - Oh SM
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
DEP - 20120928
PL  - Netherlands
TA  - Toxicol Lett
JT  - Toxicology letters
JID - 7709027
RN  - 0 (Central Nervous System Stimulants)
RN  - 0 (Estrogen Receptor Modulators)
RN  - 0 (Estrogens)
RN  - 0 (Illicit Drugs)
RN  - 0 (Piperazines)
RN  - 0 (Serotonin Receptor Agonists)
RN  - 094ZI81Y45 (Tamoxifen)
RN  - 25R3ONU51C (1-(3-trifluoromethylphenyl)piperazine)
RN  - 3UG152ZU0E (1-benzylpiperazine)
SB  - IM
MH  - Breast Neoplasms/drug therapy/genetics/metabolism
MH  - Cell Line, Tumor
MH  - Cell Proliferation/drug effects
MH  - Cell Survival/drug effects
MH  - Central Nervous System Stimulants/*toxicity
MH  - Dose-Response Relationship, Drug
MH  - Drug Antagonism
MH  - Estrogen Receptor Modulators/pharmacology
MH  - Estrogens/metabolism/pharmacology
MH  - Female
MH  - Gene Expression/drug effects
MH  - Gene Expression Regulation/drug effects
MH  - Genes, Reporter/drug effects/genetics
MH  - Humans
MH  - Illicit Drugs/*toxicity
MH  - Organ Size/drug effects
MH  - Piperazines/*toxicity
MH  - Serotonin Receptor Agonists/*toxicity
MH  - Tamoxifen/pharmacology
MH  - Uterus/drug effects/growth & development
EDAT- 2012/10/03 06:00
MHDA- 2013/01/09 06:00
CRDT- 2012/10/03 06:00
PHST- 2012/05/23 00:00 [received]
PHST- 2012/09/17 00:00 [revised]
PHST- 2012/09/19 00:00 [accepted]
PHST- 2012/10/03 06:00 [entrez]
PHST- 2012/10/03 06:00 [pubmed]
PHST- 2013/01/09 06:00 [medline]
AID - S0378-4274(12)01310-0 [pii]
AID - 10.1016/j.toxlet.2012.09.014 [doi]
PST - ppublish
SO  - Toxicol Lett. 2012 Nov 15;214(3):339-47. doi: 10.1016/j.toxlet.2012.09.014. Epub 
      2012 Sep 28.