New analogues of ACPD with selective activity for group II metabotropic glutamate receptors

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New analogues of ACPD with selective activity for group II metabotropic glutamate receptors. / Bräuner-Osborne, Hans; Madsen, U; Mikiciuk-Olasik, E; Curry, K.

In: European Journal of Pharmacology, Vol. 332, No. 3, 13.08.1997, p. 327-31.

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

Harvard

Bräuner-Osborne, H, Madsen, U, Mikiciuk-Olasik, E & Curry, K 1997, 'New analogues of ACPD with selective activity for group II metabotropic glutamate receptors', European Journal of Pharmacology, vol. 332, no. 3, pp. 327-31.

APA

Bräuner-Osborne, H., Madsen, U., Mikiciuk-Olasik, E., & Curry, K. (1997). New analogues of ACPD with selective activity for group II metabotropic glutamate receptors. European Journal of Pharmacology, 332(3), 327-31.

Vancouver

Bräuner-Osborne H, Madsen U, Mikiciuk-Olasik E, Curry K. New analogues of ACPD with selective activity for group II metabotropic glutamate receptors. European Journal of Pharmacology. 1997 Aug 13;332(3):327-31.

Author

Bräuner-Osborne, Hans ; Madsen, U ; Mikiciuk-Olasik, E ; Curry, K. / New analogues of ACPD with selective activity for group II metabotropic glutamate receptors. In: European Journal of Pharmacology. 1997 ; Vol. 332, No. 3. pp. 327-31.

Bibtex

@article{a13bc5ff1ea147219869276b5f5dc348,
title = "New analogues of ACPD with selective activity for group II metabotropic glutamate receptors",
abstract = "In this study we have determined the pharmacology of a series of 1-aminocyclopentane-1,3-dicarboxylic acid (1,3-ACPD) analogues at cloned metabotropic glutamic acid (mGlu) receptors. The new analogues comprise the four possible stereoisomers of 1-amino-1-carboxycyclopentane-3-acetic acid (1,3-homo-ACPD) and the racemic mixture of (1RS,2RS)-1-amino-1-carboxycyclopentane-2-acetic acid (1RS,2RS-homo-ACPD), (1RS,2RS)-Homo-ACPD was shown to be a competitive mGlu2 receptor antagonist with a KB of 391 microM. (1S,3R)-Homo-ACPD and (1R,3R)-homo-ACPD were both shown to be mGlu2 receptor agonists with EC50 values of 122 and 105 microM, respectively. Compared to (S)-Glu both compounds displayed partial agonism with intrinsic activities of 79% and 47%, respectively. (1S,3S)-Homo-ACPD was also found to be a partial mGlu2 receptor agonist with an intrinsic activity of 27% compared to (S)-Glu. None of the compounds tested showed any activity at mGlu1a or mGlu4a receptors. These homo-ACPD's show a higher degree of subtype selectivity than the parent compound (1SR,3RS)-ACPD. In addition none of the compounds demonstrated any activity at ionotropic Glu receptors.",
keywords = "Animals, CHO Cells, Cricetinae, Cycloleucine, Glutamic Acid, Receptors, Metabotropic Glutamate, Second Messenger Systems, Stereoisomerism, Structure-Activity Relationship",
author = "Hans Br{\"a}uner-Osborne and U Madsen and E Mikiciuk-Olasik and K Curry",
year = "1997",
month = aug,
day = "13",
language = "English",
volume = "332",
pages = "327--31",
journal = "European Journal of Pharmacology",
issn = "0014-2999",
publisher = "Elsevier",
number = "3",

}

RIS

TY - JOUR

T1 - New analogues of ACPD with selective activity for group II metabotropic glutamate receptors

AU - Bräuner-Osborne, Hans

AU - Madsen, U

AU - Mikiciuk-Olasik, E

AU - Curry, K

PY - 1997/8/13

Y1 - 1997/8/13

N2 - In this study we have determined the pharmacology of a series of 1-aminocyclopentane-1,3-dicarboxylic acid (1,3-ACPD) analogues at cloned metabotropic glutamic acid (mGlu) receptors. The new analogues comprise the four possible stereoisomers of 1-amino-1-carboxycyclopentane-3-acetic acid (1,3-homo-ACPD) and the racemic mixture of (1RS,2RS)-1-amino-1-carboxycyclopentane-2-acetic acid (1RS,2RS-homo-ACPD), (1RS,2RS)-Homo-ACPD was shown to be a competitive mGlu2 receptor antagonist with a KB of 391 microM. (1S,3R)-Homo-ACPD and (1R,3R)-homo-ACPD were both shown to be mGlu2 receptor agonists with EC50 values of 122 and 105 microM, respectively. Compared to (S)-Glu both compounds displayed partial agonism with intrinsic activities of 79% and 47%, respectively. (1S,3S)-Homo-ACPD was also found to be a partial mGlu2 receptor agonist with an intrinsic activity of 27% compared to (S)-Glu. None of the compounds tested showed any activity at mGlu1a or mGlu4a receptors. These homo-ACPD's show a higher degree of subtype selectivity than the parent compound (1SR,3RS)-ACPD. In addition none of the compounds demonstrated any activity at ionotropic Glu receptors.

AB - In this study we have determined the pharmacology of a series of 1-aminocyclopentane-1,3-dicarboxylic acid (1,3-ACPD) analogues at cloned metabotropic glutamic acid (mGlu) receptors. The new analogues comprise the four possible stereoisomers of 1-amino-1-carboxycyclopentane-3-acetic acid (1,3-homo-ACPD) and the racemic mixture of (1RS,2RS)-1-amino-1-carboxycyclopentane-2-acetic acid (1RS,2RS-homo-ACPD), (1RS,2RS)-Homo-ACPD was shown to be a competitive mGlu2 receptor antagonist with a KB of 391 microM. (1S,3R)-Homo-ACPD and (1R,3R)-homo-ACPD were both shown to be mGlu2 receptor agonists with EC50 values of 122 and 105 microM, respectively. Compared to (S)-Glu both compounds displayed partial agonism with intrinsic activities of 79% and 47%, respectively. (1S,3S)-Homo-ACPD was also found to be a partial mGlu2 receptor agonist with an intrinsic activity of 27% compared to (S)-Glu. None of the compounds tested showed any activity at mGlu1a or mGlu4a receptors. These homo-ACPD's show a higher degree of subtype selectivity than the parent compound (1SR,3RS)-ACPD. In addition none of the compounds demonstrated any activity at ionotropic Glu receptors.

KW - Animals

KW - CHO Cells

KW - Cricetinae

KW - Cycloleucine

KW - Glutamic Acid

KW - Receptors, Metabotropic Glutamate

KW - Second Messenger Systems

KW - Stereoisomerism

KW - Structure-Activity Relationship

M3 - Journal article

C2 - 9300268

VL - 332

SP - 327

EP - 331

JO - European Journal of Pharmacology

JF - European Journal of Pharmacology

SN - 0014-2999

IS - 3

ER -

ID: 45614086