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Featured Research Papers

Two authors from this month's paper, Oluyomi M. Okunola-Bakare, and Jianjing Cao.
Two authors from this month's paper, Oluyomi M. Okunola-Bakare, and Jianjing Cao.

Featured Paper Archives
Featured paper of the Month!

July's Featured Paper!

Elucidation of Structural Elements for Selectivity across Monoamine Transporters: Novel 2-[(Diphenylmethyl)sulfinyl]acetamide (Modafinil) Analogues

J Med Chem 2014, 57, 1000-1013

Oluyomi M. Okunola-Bakare, Jianjing Cao, Theresa Kopajtic, Jonathan L. Katz, Claus J. Loland, Lei Shi, and Amy Hauck Newman.

2-[(Diphenylmethyl)sulfinyl]acetamide (modafinil, (±)-1) is a unique dopamine uptake inhibitor that binds the dopamine transporter (DAT) differently than cocaine and may have potential for the treatment of psychostimulant abuse. To further investigate structural requirements for this divergent binding mode, novel thio- and sulfinylacetamide and ethanamine analogues of (±)-1 were synthesized wherein (1) the diphenyl rings were substituted with methyl, trifluoromethyl, and halogen substituents and (2) substituents were added to the terminal amide/amine nitrogen. Halogen substitution of the diphenyl rings of (±)-1 gave several amide analogues with improved binding affinity for DAT and robust selectivity over the serotonin transporter (SERT), whereas affinity improved at SERT over DAT for the p-halo-substituted amine analogues. Molecular docking studies, using a subset of analogues with DAT and SERT homology models, and functional data obtained with DAT (A480T) and SERT (T497A) mutants defined a role for TM10 in the substrate/inhibitor S1 binding sites of DAT and SERT.

You can read more about this paper at the website for PubMed.

June's Featured Paper!

Similar Roles of Substantia Nigra and Ventral Tegmental Dopamine Neurons in Reward and Aversion

J Neurosci. 2014 Jan 15;34(3):817-22. doi: 10.1523/JNEUROSCI.1703-13.2014

Anton Ilango, Andrew J. Kesner, Kristine L. Keller, Garret D. Stuber, Antonello Bonci, Satoshi Ikemoto.

You can read more about this paper at the website for PubMed.

May's Featured Paper!

Real-time tracking of neighborhood surroundings and mood in urban drug misusers: Application of a new method to study behavior in its geographical context

Drug and Alcohol Dependence 134 (2014) 22– 29

David H. Epstein, Matthew Tyburski, Ian M. Craig, Karran A. Phillips, Michelle L. Jobes, Massoud Vahabzadeh, Mustapha Mezghanni, Jia-Ling Lin, C. Debra M. Furr-Holden, Kenzie L. Preston

You can read more about this paper at the website for PubMed.

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A figure from this month's paper.
A figure from this month's paper.

Hot off the Press Archives
Featured paper of the Month!

Critical Role of Peripheral Vasoconstriction in Fatal Brain Hyperthermia Induced by MDMA (Ecstasy) under Conditions That Mimic Human Drug Use

J. Neurosci June 4, 2014 - 34(23):7754–7762

Eugene A. Kiyatkin, Albert H. Kim, Ken T. Wakabayashi, Michael H. Baumann, and Yavin Shaham

MDMA(Ecstasy) is an illicit drug used by young adults at hot, crowed “rave” parties, yet the data on potential health hazards of its abuse remain controversial. Here, we examined the effect of MDMA on temperature homeostasis in male rats under standard laboratory conditions and under conditions that simulate drug use in humans.Wechronically implanted thermocouple microsensors in the nucleus accumbens (a brain reward area), temporal muscle, and facial skin to measure temperature continuously from freely moving rats. While focusing on brain hyperthermia, temperature monitoring from the two peripheral locations allowed us to evaluate the physiological mechanisms (i.e., intracerebral heat production and heat loss via skin surfaces) that underlie MDMA-induced brain temperature responses.

Our data confirm previous reports on high individual variability and relatively weak brain hyperthermic effects of MDMA under standard control conditions (quiet rest, 2223°C), but demonstrate dramatic enhancements of drug-induced brain hyperthermia during social interaction (exposure to male conspecific) and in warm environments (29°C). Importantly, we identified peripheral vasoconstriction as a critical mechanism underlying the activity- and state-dependent potentiation of MDMA-induced brain hyperthermia. Through this mechanism, which prevents proper heat dissipation to the external environment, MDMA at a moderate nontoxic dose (9 mg/kg or 1/5 of LD50 in rats) can cause fatal hyperthermia under environmental conditions commonly encountered by humans. Our results demonstrate that doses of MDMA that are nontoxic under cool, quiet conditions can become highly dangerous under conditions that mimic recreational use of MDMA at rave parties or other hot, crowded venues.

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Large-Scale Brain Network Coupling Predicts Acute Nicotine Abstinence Effects on Craving and Cognitive Function

JAMA Psychiatry 2014;():. doi:10.1001/jamapsychiatry.2013.4109.

Caryn Lerman, Hong Gu, James Loughead, Kosha Ruparel, Yihong Yang, & Elliot A. Stein

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Presynaptic glycine receptors as a potential therapeutic target for hyperekplexia disease

Nature Neuroscience 17, 232–239 (2014)

Wei Xiong, Shao-Rui Chen, Liming He, Kejun Cheng, Yi-Lin Zhao, Hong Chen, De-Pei Li, Gregg E Homanics, John Peever, Kenner C Rice, Ling-gang Wu, Hui-Lin Pan & Li Zhang

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The National Institute on Drug Abuse (NIDA), is part of the National Institutes of Health (NIH), the principal biomedical and behavioral research agency of the United States Government. NIH is a component of the U.S. Department of Health and Human Services.

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