Novel aza-analogous ergoline derived scaffolds as potent serotonin 5-HT6 and dopamine D2 receptor ligands

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

Standard

Novel aza-analogous ergoline derived scaffolds as potent serotonin 5-HT6 and dopamine D2 receptor ligands. / Krogsgaard-Larsen, Niels; Jensen, Anders A.; Schrøder, T.J.; Christoffersen, C.T.; Kehler, Jan.

In: Journal of Medicinal Chemistry, Vol. 57, No. 13, 2014, p. 5823-5828.

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

Harvard

Krogsgaard-Larsen, N, Jensen, AA, Schrøder, TJ, Christoffersen, CT & Kehler, J 2014, 'Novel aza-analogous ergoline derived scaffolds as potent serotonin 5-HT6 and dopamine D2 receptor ligands', Journal of Medicinal Chemistry, vol. 57, no. 13, pp. 5823-5828. https://doi.org/10.1021/jm5003759

APA

Krogsgaard-Larsen, N., Jensen, A. A., Schrøder, T. J., Christoffersen, C. T., & Kehler, J. (2014). Novel aza-analogous ergoline derived scaffolds as potent serotonin 5-HT6 and dopamine D2 receptor ligands. Journal of Medicinal Chemistry, 57(13), 5823-5828. https://doi.org/10.1021/jm5003759

Vancouver

Krogsgaard-Larsen N, Jensen AA, Schrøder TJ, Christoffersen CT, Kehler J. Novel aza-analogous ergoline derived scaffolds as potent serotonin 5-HT6 and dopamine D2 receptor ligands. Journal of Medicinal Chemistry. 2014;57(13):5823-5828. https://doi.org/10.1021/jm5003759

Author

Krogsgaard-Larsen, Niels ; Jensen, Anders A. ; Schrøder, T.J. ; Christoffersen, C.T. ; Kehler, Jan. / Novel aza-analogous ergoline derived scaffolds as potent serotonin 5-HT6 and dopamine D2 receptor ligands. In: Journal of Medicinal Chemistry. 2014 ; Vol. 57, No. 13. pp. 5823-5828.

Bibtex

@article{bc1bb4d8f3204e4fb858f185313e8fc9,
title = "Novel aza-analogous ergoline derived scaffolds as potent serotonin 5-HT6 and dopamine D2 receptor ligands",
abstract = "By introducing distal substituents on a tetracyclic scaffold resembling the ergoline structure, two series of analogues were achieved exhibiting subnanomolar receptor binding affinities for the dopamine D2 and serotonin 5-HT6 receptor subtype, respectively. While the 5-HT6 ligands were antagonists, the D2 ligands displayed intrinsic activities ranging from full agonism to partial agonism with low intrinsic activity. These structures could potentially be interesting for treatment of neurological diseases such as schizophrenia, Parkinson{\textquoteright}s disease, and cognitive deficits.",
author = "Niels Krogsgaard-Larsen and Jensen, {Anders A.} and T.J. Schr{\o}der and C.T. Christoffersen and Jan Kehler",
year = "2014",
doi = "10.1021/jm5003759",
language = "English",
volume = "57",
pages = "5823--5828",
journal = "Journal of Medicinal Chemistry",
issn = "0022-2623",
publisher = "American Chemical Society",
number = "13",

}

RIS

TY - JOUR

T1 - Novel aza-analogous ergoline derived scaffolds as potent serotonin 5-HT6 and dopamine D2 receptor ligands

AU - Krogsgaard-Larsen, Niels

AU - Jensen, Anders A.

AU - Schrøder, T.J.

AU - Christoffersen, C.T.

AU - Kehler, Jan

PY - 2014

Y1 - 2014

N2 - By introducing distal substituents on a tetracyclic scaffold resembling the ergoline structure, two series of analogues were achieved exhibiting subnanomolar receptor binding affinities for the dopamine D2 and serotonin 5-HT6 receptor subtype, respectively. While the 5-HT6 ligands were antagonists, the D2 ligands displayed intrinsic activities ranging from full agonism to partial agonism with low intrinsic activity. These structures could potentially be interesting for treatment of neurological diseases such as schizophrenia, Parkinson’s disease, and cognitive deficits.

AB - By introducing distal substituents on a tetracyclic scaffold resembling the ergoline structure, two series of analogues were achieved exhibiting subnanomolar receptor binding affinities for the dopamine D2 and serotonin 5-HT6 receptor subtype, respectively. While the 5-HT6 ligands were antagonists, the D2 ligands displayed intrinsic activities ranging from full agonism to partial agonism with low intrinsic activity. These structures could potentially be interesting for treatment of neurological diseases such as schizophrenia, Parkinson’s disease, and cognitive deficits.

U2 - 10.1021/jm5003759

DO - 10.1021/jm5003759

M3 - Journal article

VL - 57

SP - 5823

EP - 5828

JO - Journal of Medicinal Chemistry

JF - Journal of Medicinal Chemistry

SN - 0022-2623

IS - 13

ER -

ID: 101352572