5-HT2A/5-HT2C receptor pharmacology and intrinsic clearance of N-benzylphenethylamines modified at the primary site of metabolism

Research output: Contribution to journal › Journal article › Research › peer-review

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5-HT2A/5-HT2C receptor pharmacology and intrinsic clearance of N-benzylphenethylamines modified at the primary site of metabolism. / Leth-Petersen, Sebastian; Petersen, Ida Nymann; Jensen, Anders A; Bundgaard, Christoffer; Bæk, Mathias; Kehler, Jan; Kristensen, Jesper L.

In: A C S Chemical Neuroscience, 26.08.2016, p. 1-6.

Research output: Contribution to journal › Journal article › Research › peer-review

Harvard

Leth-Petersen, S, Petersen, IN, Jensen, AA, Bundgaard, C, Bæk, M, Kehler, J & Kristensen, JL 2016, '5-HT2A/5-HT2C receptor pharmacology and intrinsic clearance of N-benzylphenethylamines modified at the primary site of metabolism', A C S Chemical Neuroscience, pp. 1-6. https://doi.org/10.1021/acschemneuro.6b00265

APA

Leth-Petersen, S., Petersen, I. N., Jensen, A. A., Bundgaard, C., Bæk, M., Kehler, J., & Kristensen, J. L. (2016). 5-HT2A/5-HT2C receptor pharmacology and intrinsic clearance of N-benzylphenethylamines modified at the primary site of metabolism. A C S Chemical Neuroscience, 1-6. https://doi.org/10.1021/acschemneuro.6b00265

Vancouver

Leth-Petersen S, Petersen IN, Jensen AA, Bundgaard C, Bæk M, Kehler J et al. 5-HT2A/5-HT2C receptor pharmacology and intrinsic clearance of N-benzylphenethylamines modified at the primary site of metabolism. A C S Chemical Neuroscience. 2016 Aug 26;1-6. https://doi.org/10.1021/acschemneuro.6b00265

Author

Leth-Petersen, Sebastian ; Petersen, Ida Nymann ; Jensen, Anders A ; Bundgaard, Christoffer ; Bæk, Mathias ; Kehler, Jan ; Kristensen, Jesper L. / 5-HT2A/5-HT2C receptor pharmacology and intrinsic clearance of N-benzylphenethylamines modified at the primary site of metabolism. In: A C S Chemical Neuroscience. 2016 ; pp. 1-6.

Bibtex

@article{ba748a670b364f27b9086408a63b576d,
title = "5-HT2A/5-HT2C receptor pharmacology and intrinsic clearance of N-benzylphenethylamines modified at the primary site of metabolism",
abstract = "The toxic hallucinogen 25B-NBOMe is very rapidly degraded by human liver microsomes and has low oral bioavailability. Herein we report on the synthesis, microsomal stability and 5-HT2A/5-HT2C receptor profile of novel analogs of 25B-NBOMe modified at the primary site of metabolism. Although microsomal stability could be increased while maintaining potent 5-HT2 receptor agonist properties, all analogs had an intrinsic clearance above 1.3 L/kg/h predictive of high first-pass metabolism.",
author = "Sebastian Leth-Petersen and Petersen, {Ida Nymann} and Jensen, {Anders A} and Christoffer Bundgaard and Mathias B{\ae}k and Jan Kehler and Kristensen, {Jesper L}",
year = "2016",
month = aug,
day = "26",
doi = "10.1021/acschemneuro.6b00265",
language = "English",
pages = "1--6",
journal = "ACS Chemical Neuroscience",
issn = "1948-7193",
publisher = "American Chemical Society",

}

RIS

TY - JOUR

T1 - 5-HT2A/5-HT2C receptor pharmacology and intrinsic clearance of N-benzylphenethylamines modified at the primary site of metabolism

AU - Leth-Petersen, Sebastian

AU - Petersen, Ida Nymann

AU - Jensen, Anders A

AU - Bundgaard, Christoffer

AU - Bæk, Mathias

AU - Kehler, Jan

AU - Kristensen, Jesper L

PY - 2016/8/26

Y1 - 2016/8/26

N2 - The toxic hallucinogen 25B-NBOMe is very rapidly degraded by human liver microsomes and has low oral bioavailability. Herein we report on the synthesis, microsomal stability and 5-HT2A/5-HT2C receptor profile of novel analogs of 25B-NBOMe modified at the primary site of metabolism. Although microsomal stability could be increased while maintaining potent 5-HT2 receptor agonist properties, all analogs had an intrinsic clearance above 1.3 L/kg/h predictive of high first-pass metabolism.

AB - The toxic hallucinogen 25B-NBOMe is very rapidly degraded by human liver microsomes and has low oral bioavailability. Herein we report on the synthesis, microsomal stability and 5-HT2A/5-HT2C receptor profile of novel analogs of 25B-NBOMe modified at the primary site of metabolism. Although microsomal stability could be increased while maintaining potent 5-HT2 receptor agonist properties, all analogs had an intrinsic clearance above 1.3 L/kg/h predictive of high first-pass metabolism.

U2 - 10.1021/acschemneuro.6b00265

DO - 10.1021/acschemneuro.6b00265

M3 - Journal article

C2 - 27564969

SP - 1

EP - 6

JO - ACS Chemical Neuroscience

JF - ACS Chemical Neuroscience

SN - 1948-7193

ER -

ID: 164969052