PMID- 27079619 OWN - NLM STAT- MEDLINE DCOM- 20170323 LR - 20221207 IS - 1879-3177 (Electronic) IS - 0887-2333 (Linking) VI - 34 DP - 2016 Aug TI - Contractile effects of 3,4-methylenedioxymethamphetamine on the human internal mammary artery. PG - 187-193 LID - S0887-2333(16)30069-8 [pii] LID - 10.1016/j.tiv.2016.04.002 [doi] AB - Since the late 1980s numerous reports have detailed adverse reactions to the use of 3,4-methylenedioxymethamphetamine (MDMA) associated with cardiovascular collapse and sudden death, following ventricular tachycardia and hypertension. For a better understanding of the effects of MDMA on the cardiovascular system, it is critical to determine their effects at the vasculature level, including the transporter or neurotransmitter systems that are most affected at the whole range of drug doses. With this purpose in mind, the aim of our study was to evaluate the contractile effect of MDMA in the human internal mammary artery, the contribution of SERT for this effect and the responsiveness of this artery to 5-HT in the presence of MDMA. We have also studied the possible involvement of 5-HT2 receptors on the MDMA contractile effect in this human blood vessel using ketanserin. Our results showed that MDMA contracted the studied human's internal mammary artery in a SERT-independent form, through activation of 5-HT2A receptors. Considering the high plasma concentrations achieved in heavy users or in situations of acute exposure to drugs, this effect is probably involved in the cardiovascular risk profile of this psychostimulant, especially in subjects with pre-existing cardiovascular disease. CI - Copyright (c) 2016 Elsevier Ltd. All rights reserved. FAU - Silva, Sonia AU - Silva S AD - Group of Pharmacology and Pharmaceutical Care, Faculty of Pharmacy, University of Coimbra, Portugal. Electronic address: sonias@ci.uc.pt. FAU - Carvalho, Felix AU - Carvalho F AD - UCIBIO-REQUIMTE, Laboratory of Toxicology, Department of Biological Sciences, Faculty of Pharmacy, University of Porto, Portugal. FAU - Fernandes, Eduarda AU - Fernandes E AD - UCIBIO-REQUIMTE, Laboratory of Applied Chemistry, Department of Chemistry, Faculty of Pharmacy, University of Porto, Portugal. FAU - Antunes, Manuel J AU - Antunes MJ AD - Cardiothoracic Surgery, University Hospital of Coimbra, Coimbra, Portugal. FAU - Cotrim, Maria Dulce AU - Cotrim MD AD - Group of Pharmacology and Pharmaceutical Care, Faculty of Pharmacy, University of Coimbra, Portugal. LA - eng PT - Journal Article DEP - 20160411 PL - England TA - Toxicol In Vitro JT - Toxicology in vitro : an international journal published in association with BIBRA JID - 8712158 RN - 0 (Hallucinogens) RN - 0 (Receptor, Serotonin, 5-HT2A) RN - 0 (Receptor, Serotonin, 5-HT2C) RN - 0 (SLC6A4 protein, human) RN - 0 (Serotonin Antagonists) RN - 0 (Serotonin Plasma Membrane Transport Proteins) RN - 0 (Serotonin Uptake Inhibitors) RN - 01K63SUP8D (Fluoxetine) RN - 333DO1RDJY (Serotonin) RN - 97F9DE4CT4 (Ketanserin) RN - KE1SEN21RM (N-Methyl-3,4-methylenedioxyamphetamine) SB - IM MH - Fluoxetine/pharmacology MH - Hallucinogens/*pharmacology MH - Humans MH - In Vitro Techniques MH - Isometric Contraction/drug effects MH - Ketanserin/pharmacology MH - Mammary Arteries/*drug effects/physiology MH - N-Methyl-3,4-methylenedioxyamphetamine/*pharmacology MH - Receptor, Serotonin, 5-HT2A/*physiology MH - Receptor, Serotonin, 5-HT2C/physiology MH - Serotonin/pharmacology MH - Serotonin Antagonists/pharmacology MH - Serotonin Plasma Membrane Transport Proteins/physiology MH - Selective Serotonin Reuptake Inhibitors/pharmacology OTO - NOTNLM OT - 5-HT OT - Fluoxetine OT - Human internal mammary artery OT - Ketanserin OT - MDMA (ecstasy) EDAT- 2016/04/16 06:00 MHDA- 2017/03/24 06:00 CRDT- 2016/04/16 06:00 PHST- 2015/09/29 00:00 [received] PHST- 2016/03/24 00:00 [revised] PHST- 2016/04/04 00:00 [accepted] PHST- 2016/04/16 06:00 [entrez] PHST- 2016/04/16 06:00 [pubmed] PHST- 2017/03/24 06:00 [medline] AID - S0887-2333(16)30069-8 [pii] AID - 10.1016/j.tiv.2016.04.002 [doi] PST - ppublish SO - Toxicol In Vitro. 2016 Aug;34:187-193. doi: 10.1016/j.tiv.2016.04.002. Epub 2016 Apr 11.