The psychoactive aminoalkylbenzofuran derivatives, 5-APB and 6-APB, mimic the effects of 3,4-methylenedioxyamphetamine (MDA) on monoamine transmission in male rats.
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| Title: | The psychoactive aminoalkylbenzofuran derivatives, 5-APB and 6-APB, mimic the effects of 3,4-methylenedioxyamphetamine (MDA) on monoamine transmission in male rats. |
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| Authors: | Brandt, Simon D. (AUTHOR), Walters, Hailey M. (AUTHOR), Partilla, John S. (AUTHOR), Blough, Bruce E. (AUTHOR), Kavanagh, Pierce V. (AUTHOR), Baumann, Michael H. (AUTHOR) |
| Source: | Psychopharmacology. 2020, Vol. 237 Issue 12, p3703-3714. 12p. 1 Diagram, 1 Chart, 5 Graphs. |
| Subjects: | Monoamine transporters, Serotonin, Serotonin transporters, Serotonin receptors, Benzofurans, Cell receptors, Nucleus accumbens |
| Abstract: | Rationale: The nonmedical use of new psychoactive substances (NPS) is a worldwide public health concern. The so-called "benzofury" compounds, 5-(2-aminopropyl)benzofuran (5-APB) and 6-(2-aminopropyl)benzofuran (6-APB), are NPS with stimulant-like properties in human users. These substances are known to interact with monoamine transporters and 5-HT receptors in transfected cells, but less is known about their effects in animal models. Methods: Here, we used in vitro monoamine transporter assays in rat brain synaptosomes to characterize the effects of 5-APB and 6-APB, together with their N-methyl derivatives 5-MAPB and 6-MAPB, in comparison with 3,4-methylenedioxyamphetamine (MDA) and 3,4-methylenedioxymethamphetamine (MDMA). In vivo neurochemical and behavioral effects of 5-APB (0.3 and 1.0 mg/kg, i.v.) and 6-APB (0.3 and 1.0 mg/kg, i.v.) were assessed in comparison with MDA (1.0 and 3.0 mg/kg, i.v.) using microdialysis sampling in the nucleus accumbens of conscious male rats. Results: All four benzofuran derivatives were substrate-type releasers at dopamine transporters (DAT), norepinephrine transporters (NET), and serotonin transporters (SERT) with nanomolar potencies, similar to the profile of effects produced by MDA and MDMA. However, the benzofurans were at least threefold more potent than MDA and MDMA at evoking transporter-mediated release. Like MDA, both benzofurans induced dose-related elevations in extracellular dopamine and serotonin in the brain, but benzofurans were more potent than MDA. The benzofuran derivatives also induced profound behavioral activation characterized by forward locomotion which lasted for at least 2 h post-injection. Conclusions: Overall, benzofurans are more potent than MDA in vitro and in vivo, producing sustained stimulant-like effects in rats. These data suggest that benzofuran-type compounds may have abuse liability and could pose risks for adverse effects, especially if used in conjunction with abused drugs or medications which enhance monoamine transmission in the brain. [ABSTRACT FROM AUTHOR] |
| Copyright of Psychopharmacology is the property of Springer Nature and its content may not be copied or emailed to multiple sites without the copyright holder's express written permission. Additionally, content may not be used with any artificial intelligence tools or machine learning technologies. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.) | |
| Database: | Psychology and Behavioral Sciences Collection |
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| Header | DbId: pbh DbLabel: Psychology and Behavioral Sciences Collection An: 147157244 AccessLevel: 6 PubType: Academic Journal PubTypeId: academicJournal PreciseRelevancyScore: 0 |
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| Items | – Name: Title Label: Title Group: Ti Data: The psychoactive aminoalkylbenzofuran derivatives, 5-APB and 6-APB, mimic the effects of 3,4-methylenedioxyamphetamine (MDA) on monoamine transmission in male rats. – Name: Author Label: Authors Group: Au Data: <searchLink fieldCode="AR" term="%22Brandt%2C+Simon+D%2E%22">Brandt, Simon D.</searchLink> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Walters%2C+Hailey+M%2E%22">Walters, Hailey M.</searchLink> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Partilla%2C+John+S%2E%22">Partilla, John S.</searchLink> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Blough%2C+Bruce+E%2E%22">Blough, Bruce E.</searchLink> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Kavanagh%2C+Pierce+V%2E%22">Kavanagh, Pierce V.</searchLink> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Baumann%2C+Michael+H%2E%22">Baumann, Michael H.</searchLink> (AUTHOR) – Name: TitleSource Label: Source Group: Src Data: <searchLink fieldCode="JN" term="%22Psychopharmacology%22">Psychopharmacology</searchLink>. 2020, Vol. 237 Issue 12, p3703-3714. 12p. 1 Diagram, 1 Chart, 5 Graphs. – Name: Subject Label: Subjects Group: Su Data: <searchLink fieldCode="DE" term="%22Monoamine+transporters%22">Monoamine transporters</searchLink><br /><searchLink fieldCode="DE" term="%22Serotonin%22">Serotonin</searchLink><br /><searchLink fieldCode="DE" term="%22Serotonin+transporters%22">Serotonin transporters</searchLink><br /><searchLink fieldCode="DE" term="%22Serotonin+receptors%22">Serotonin receptors</searchLink><br /><searchLink fieldCode="DE" term="%22Benzofurans%22">Benzofurans</searchLink><br /><searchLink fieldCode="DE" term="%22Cell+receptors%22">Cell receptors</searchLink><br /><searchLink fieldCode="DE" term="%22Nucleus+accumbens%22">Nucleus accumbens</searchLink> – Name: Abstract Label: Abstract Group: Ab Data: Rationale: The nonmedical use of new psychoactive substances (NPS) is a worldwide public health concern. The so-called "benzofury" compounds, 5-(2-aminopropyl)benzofuran (5-APB) and 6-(2-aminopropyl)benzofuran (6-APB), are NPS with stimulant-like properties in human users. These substances are known to interact with monoamine transporters and 5-HT receptors in transfected cells, but less is known about their effects in animal models. Methods: Here, we used in vitro monoamine transporter assays in rat brain synaptosomes to characterize the effects of 5-APB and 6-APB, together with their N-methyl derivatives 5-MAPB and 6-MAPB, in comparison with 3,4-methylenedioxyamphetamine (MDA) and 3,4-methylenedioxymethamphetamine (MDMA). In vivo neurochemical and behavioral effects of 5-APB (0.3 and 1.0 mg/kg, i.v.) and 6-APB (0.3 and 1.0 mg/kg, i.v.) were assessed in comparison with MDA (1.0 and 3.0 mg/kg, i.v.) using microdialysis sampling in the nucleus accumbens of conscious male rats. Results: All four benzofuran derivatives were substrate-type releasers at dopamine transporters (DAT), norepinephrine transporters (NET), and serotonin transporters (SERT) with nanomolar potencies, similar to the profile of effects produced by MDA and MDMA. However, the benzofurans were at least threefold more potent than MDA and MDMA at evoking transporter-mediated release. Like MDA, both benzofurans induced dose-related elevations in extracellular dopamine and serotonin in the brain, but benzofurans were more potent than MDA. The benzofuran derivatives also induced profound behavioral activation characterized by forward locomotion which lasted for at least 2 h post-injection. Conclusions: Overall, benzofurans are more potent than MDA in vitro and in vivo, producing sustained stimulant-like effects in rats. These data suggest that benzofuran-type compounds may have abuse liability and could pose risks for adverse effects, especially if used in conjunction with abused drugs or medications which enhance monoamine transmission in the brain. [ABSTRACT FROM AUTHOR] – Name: AbstractSuppliedCopyright Label: Group: Ab Data: <i>Copyright of Psychopharmacology is the property of Springer Nature and its content may not be copied or emailed to multiple sites without the copyright holder's express written permission. Additionally, content may not be used with any artificial intelligence tools or machine learning technologies. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract.</i> (Copyright applies to all Abstracts.) |
| PLink | https://search.ebscohost.com/login.aspx?direct=true&site=eds-live&db=pbh&AN=147157244 |
| RecordInfo | BibRecord: BibEntity: Identifiers: – Type: doi Value: 10.1007/s00213-020-05648-z Languages: – Code: eng Text: English PhysicalDescription: Pagination: PageCount: 12 StartPage: 3703 Subjects: – SubjectFull: Monoamine transporters Type: general – SubjectFull: Serotonin Type: general – SubjectFull: Serotonin transporters Type: general – SubjectFull: Serotonin receptors Type: general – SubjectFull: Benzofurans Type: general – SubjectFull: Cell receptors Type: general – SubjectFull: Nucleus accumbens Type: general Titles: – TitleFull: The psychoactive aminoalkylbenzofuran derivatives, 5-APB and 6-APB, mimic the effects of 3,4-methylenedioxyamphetamine (MDA) on monoamine transmission in male rats. Type: main BibRelationships: HasContributorRelationships: – PersonEntity: Name: NameFull: Brandt, Simon D. – PersonEntity: Name: NameFull: Walters, Hailey M. – PersonEntity: Name: NameFull: Partilla, John S. – PersonEntity: Name: NameFull: Blough, Bruce E. – PersonEntity: Name: NameFull: Kavanagh, Pierce V. – PersonEntity: Name: NameFull: Baumann, Michael H. IsPartOfRelationships: – BibEntity: Dates: – D: 01 M: 12 Text: 2020 Type: published Y: 2020 Identifiers: – Type: issn-print Value: 00333158 Numbering: – Type: volume Value: 237 – Type: issue Value: 12 Titles: – TitleFull: Psychopharmacology Type: main |
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