Pharmaceutical Chemistry Journal

, volume 50 , issue 8 , pages 501-504

Novel Pyrrolo[1,2-a]Pyrazines (TSPO Ligands) with Anxiolytic Activity Dependent on Neurosteroid Biosynthesis

M. A. Yarkova ¹

G V Mokrov ¹

T. A. Gudasheva ¹

S. B. Seredenin ¹

Hide authors affiliations Show authors affiliations: 1 affiliation

Zakusov State Institute of Pharmacology, Russian Academy of Medical Sciences, Moscow, Russia |

Publication type: Journal Article

Publication date: 2016-11-17

Springer Nature

Pharmaceutical Chemistry Journal

scimago Q4

wos Q4

SJR: 0.219

CiteScore: 1.4

Impact factor: 1.0

ISSN: 0091150X, 15739031

DOI: 10.1007/s11094-016-1476-0

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Drug Discovery

Pharmacology

Abstract

A series of novel pyrrolo[1,2-a]pyrazines that were ligands of 18 kDa translocator protein (TSPO) were synthesized at Zakusov SIP. The compounds N-benzyl-N-methyl-1-phenylpyrrolo[1,2-a]pyrazine-3-carboxamide (GML-1) and N-butyl-N-methyl-1-phenylpyrrolo[1,2-a]pyrazine-3-carboxamide (GML-3) were found to possess high TSPO affinity and pronounced anxiolytic activity. The anxiolytic effects of GML-1 and GML-3 in elevated plus-maze tests were completely blocked by the neurosteroidogenic-enzyme inhibitors trilostane and finasteride.

Found

3 citations

Mokrov Grigory

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North Caucasus Federal University

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GOST |

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GOST Copy

Yarkova M. A. et al. Novel Pyrrolo[1,2-a]Pyrazines (TSPO Ligands) with Anxiolytic Activity Dependent on Neurosteroid Biosynthesis // Pharmaceutical Chemistry Journal. 2016. Vol. 50. No. 8. pp. 501-504.

GOST all authors (up to 50) Copy

Yarkova M. A., Mokrov G. V., Gudasheva T. A., Seredenin S. B. Novel Pyrrolo[1,2-a]Pyrazines (TSPO Ligands) with Anxiolytic Activity Dependent on Neurosteroid Biosynthesis // Pharmaceutical Chemistry Journal. 2016. Vol. 50. No. 8. pp. 501-504.

RIS |

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RIS Copy

TY - JOUR

DO - 10.1007/s11094-016-1476-0

UR - https://doi.org/10.1007/s11094-016-1476-0

TI - Novel Pyrrolo[1,2-a]Pyrazines (TSPO Ligands) with Anxiolytic Activity Dependent on Neurosteroid Biosynthesis

T2 - Pharmaceutical Chemistry Journal

AU - Yarkova, M. A.

AU - Mokrov, G V

AU - Gudasheva, T. A.

AU - Seredenin, S. B.

PY - 2016

DA - 2016/11/17

PB - Springer Nature

SP - 501-504

IS - 8

VL - 50

SN - 0091-150X

SN - 1573-9031

ER -

BibTex |

Cite this

BibTex (up to 50 authors) Copy

@article{2016_Yarkova,

author = {M. A. Yarkova and G V Mokrov and T. A. Gudasheva and S. B. Seredenin},

title = {Novel Pyrrolo[1,2-a]Pyrazines (TSPO Ligands) with Anxiolytic Activity Dependent on Neurosteroid Biosynthesis},

journal = {Pharmaceutical Chemistry Journal},

year = {2016},

volume = {50},

publisher = {Springer Nature},

month = {nov},

url = {https://doi.org/10.1007/s11094-016-1476-0},

number = {8},

pages = {501--504},

doi = {10.1007/s11094-016-1476-0}

}

MLA

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MLA Copy

Yarkova, M. A., et al. “Novel Pyrrolo[1,2-a]Pyrazines (TSPO Ligands) with Anxiolytic Activity Dependent on Neurosteroid Biosynthesis.” Pharmaceutical Chemistry Journal, vol. 50, no. 8, Nov. 2016, pp. 501-504. https://doi.org/10.1007/s11094-016-1476-0.

Publisher

Springer Nature

Journal

Pharmaceutical Chemistry Journal

scimago Q4

wos Q4

SJR

0.219

CiteScore

1.4

Impact factor

1.0

ISSN

0091150X (Print)

15739031 (Electronic)

Profiles

Grigory Vladimirovich Mokrov