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논문 기본 정보

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학술저널
저자정보
Abiero, Arvie (Uimyung Research Institute for Neuroscience, Department of Pharmacy, Sahmyook University) Ryu, In Soo (Center for Safety Pharmacology, Korea Institute of Toxicology) Botanas, Chrislean Jun (Uimyung Research Institute for Neuroscience, Department of Pharmacy, Sahmyook University) Custodio, Raly James Perez (Uimyung Research Institute for Neuroscience, Department of Pharmacy, Sahmyook University) Sayson, Leandro Val (Uimyung Research Institute for Neuroscience, Department of Pharmacy, Sahmyook University) Kim, Mikyung (Uimyung Research Institute for Neuroscience, Department of Pharmacy, Sahmyook University) Lee, Hyun Jun (Uimyung Research Institute for Neuroscience, Department of Pharmacy, Sahmyook University) Kim, Hee Jin (Uimyung Research Institute for Neuroscience, Department of Pharmacy, Sahmyook University) Seo, Joung-Wook (Center for Safety Pharmacology, Korea Institute of Toxicology) Cho, Min Chang (Medicinal Chemistry Laboratory, Department of Pharmacy & Department of Life and Nanopharmaceutical Sciences, College of Pharmacy, Kyung Hee University) Lee, Kun Won (Medicinal Chemistry Laboratory, Department of Pharmacy & Department of Life and Na) Yoo, Sung Yeun Jang, Choon-Gon Lee, Yong Sup Cheong, Jae Hoon
저널정보
한국응용약물학회 Biomolecules & Therapeutics(구 응용약물학회지) Biomolecules & therapeutics 제28권 제1호
발행연도
2020.1
수록면
83 - 91 (9page)

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Tryptamines are monoamine alkaloids with hallucinogenic properties and are widely abused worldwide. To hasten the regulations of novel substances and predict their abuse potential, we designed and synthesized four novel synthetic tryptamine analogs: Pyrrolidino tryptamine hydrochloride (PYT HCl), Piperidino tryptamine hydrochloride (PIT HCl), N,N-dibutyl tryptamine hydrochloride (DBT HCl), and 2-Methyl tryptamine hydrochloride (2-MT HCl). Then, we evaluated their rewarding and reinforcing effects using the conditioned place preference (CPP) and self-administration (SA) paradigms. We conducted an open field test (OFT) to determine the effects of the novel compounds on locomotor activity. A head-twitch response (HTR) was also performed to characterize their hallucinogenic properties. Lastly, we examined the effects of the compounds on 5-HTR1a and 5-HTR2a in the prefrontal cortex using a quantitative real-time polymerase chain reaction (qRT-PCR) assay. None of the compounds induced CPP in mice or initiated SA in rats. PYT HCl and PIT HCl reduced the locomotor activity and elevated the 5-HTR1a mRNA levels in mice. Acute and repeated treatment with the novel tryptamines elicited HTR in mice. Furthermore, a drug challenge involving a 7-day abstinence from drug use produced higher HTR than acute and repeated treatments. Both the acute treatment and drug challenge increased the 5-HTR2a mRNA levels. Ketanserin blocked the induced HTR. Taken together, the findings suggest that PYT HCl, PIT HCl, DBT HCl, and 2-MT HCl produce hallucinogenic effects via 5-HTR2a stimulation, but may have low abuse potential.
#Novel synthetic tryptamine analogs #Abuse potential #Conditioned place preference #Self-administration #Head-twitch response #$5-HT_2$ receptors

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참고문헌 (44)

참고문헌 신청
Abiero, A. / 2019 / 5-Methoxy-α-methyltryptamine (5-MeO-AMT), a tryptamine derivative, induces head-twitch responses in mice through the activation of serotonin receptor 2a in the prefrontal cortex / Behav. Brain Res 359:828~835 google schola Anji, A. / 2000 / Regulation of 5-HT2A receptor mRNA levels and binding sites in rat frontal cortex by the agonist DOI and the antagonist mianserin / Neuropharmacology 39:1996~2005 google schola Araújo, A. M. / 2015 / The hallucinogenic world of tryptamines : an updated review / Arch. Toxicol 89:1151~1173 google schola Berry, J. N. / 2012 / Reinstatement of methamphetamine conditioned place preference in nicotine-sensitized rats / Behav. Brain Res 235:158~165 google schola Botanas, C. J. / 2017 / Methoxetamine produces rapid and sustained antidepressant effects probably via glutamatergic and serotonergic mechanisms / Neuropharmacology 126:121~127 google schola

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