Affinities and intrinsic activities of dopamine receptor agonists for the hD21 and hD4.4 receptors

Robert A. Lahti; Alex Mutin; Erika V. Cochrane; Pieter G. Tepper; Durk Dijkstra; Håkan Wikström; Carol A. Tamminga

doi:10.1016/0014-2999(96)00127-6

Affinities and intrinsic activities of dopamine receptor agonists for the hD₂₁ and hD_4.4 receptors

Robert A. Lahti, Alex Mutin, Erika V. Cochrane, Pieter G. Tepper, Durk Dijkstra, Håkan Wikström, Carol A. Tamminga

Research output: Contribution to journal › Article › peer-review

14 Scopus citations

Abstract

The affinity and intrinsic activity of dopamine receptor agonists were determined at the human dopamine hD₂₁ and hD_4.4 receptors. (-)-3-Hydroxy-N-n-propylpiperidine ((-)3-PPP) had an intrinsic activity of 46% and 83%, whereas (+)-N-propylnorapomorphine ((+)-NPA) had intrinsic activities of 61% and 58% at the dopamine hD₂₁ and hD_4.4 receptors, respectively. Affinities also varied. A single, or multiple, dopamine D₂-type receptor(s) may be involved in schizophrenia and agonists are being tested as therapy. Understanding their properties at the individual dopamine D₂-family receptors is important.

Original language	English (US)
Pages (from-to)	R11-R13
Journal	European Journal of Pharmacology
Volume	301
Issue number	1-3
DOIs	https://doi.org/10.1016/0014-2999(96)00127-6
State	Published - Apr 22 1996

Keywords

Dopamine hD receptor
Dopamine hD receptor
Intrinsic activity

ASJC Scopus subject areas

Pharmacology

Access to Document

10.1016/0014-2999(96)00127-6

Cite this

@article{d319b7fe592e4387940375810acfa039,

title = "Affinities and intrinsic activities of dopamine receptor agonists for the hD21 and hD4.4 receptors",

abstract = "The affinity and intrinsic activity of dopamine receptor agonists were determined at the human dopamine hD21 and hD4.4 receptors. (-)-3-Hydroxy-N-n-propylpiperidine ((-)3-PPP) had an intrinsic activity of 46% and 83%, whereas (+)-N-propylnorapomorphine ((+)-NPA) had intrinsic activities of 61% and 58% at the dopamine hD21 and hD4.4 receptors, respectively. Affinities also varied. A single, or multiple, dopamine D2-type receptor(s) may be involved in schizophrenia and agonists are being tested as therapy. Understanding their properties at the individual dopamine D2-family receptors is important.",

keywords = "Dopamine hD receptor, Dopamine hD receptor, Intrinsic activity",

author = "Lahti, {Robert A.} and Alex Mutin and Cochrane, {Erika V.} and Tepper, {Pieter G.} and Durk Dijkstra and H{\aa}kan Wikstr{\"o}m and Tamminga, {Carol A.}",

note = "Funding Information: We acknowledge Hubert H.M. Van Tol (Clarke Institute) for CHO-hD4. 4 cells, Marc Caron (Duke University) for CHO-hDzl cells, and Richard Hsi (Upjohn Labs) for \[3H\]U-86170. This work was supported by National Institute of Mental Health Grant 5 ROI MH49667-03.",

year = "1996",

month = apr,

day = "22",

doi = "10.1016/0014-2999(96)00127-6",

language = "English (US)",

volume = "301",

pages = "R11--R13",

journal = "European Journal of Pharmacology",

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TY - JOUR

T1 - Affinities and intrinsic activities of dopamine receptor agonists for the hD21 and hD4.4 receptors

AU - Lahti, Robert A.

AU - Mutin, Alex

AU - Cochrane, Erika V.

AU - Tepper, Pieter G.

AU - Dijkstra, Durk

AU - Wikström, Håkan

AU - Tamminga, Carol A.

N1 - Funding Information: We acknowledge Hubert H.M. Van Tol (Clarke Institute) for CHO-hD4. 4 cells, Marc Caron (Duke University) for CHO-hDzl cells, and Richard Hsi (Upjohn Labs) for \[3H\]U-86170. This work was supported by National Institute of Mental Health Grant 5 ROI MH49667-03.

PY - 1996/4/22

Y1 - 1996/4/22

N2 - The affinity and intrinsic activity of dopamine receptor agonists were determined at the human dopamine hD21 and hD4.4 receptors. (-)-3-Hydroxy-N-n-propylpiperidine ((-)3-PPP) had an intrinsic activity of 46% and 83%, whereas (+)-N-propylnorapomorphine ((+)-NPA) had intrinsic activities of 61% and 58% at the dopamine hD21 and hD4.4 receptors, respectively. Affinities also varied. A single, or multiple, dopamine D2-type receptor(s) may be involved in schizophrenia and agonists are being tested as therapy. Understanding their properties at the individual dopamine D2-family receptors is important.

AB - The affinity and intrinsic activity of dopamine receptor agonists were determined at the human dopamine hD21 and hD4.4 receptors. (-)-3-Hydroxy-N-n-propylpiperidine ((-)3-PPP) had an intrinsic activity of 46% and 83%, whereas (+)-N-propylnorapomorphine ((+)-NPA) had intrinsic activities of 61% and 58% at the dopamine hD21 and hD4.4 receptors, respectively. Affinities also varied. A single, or multiple, dopamine D2-type receptor(s) may be involved in schizophrenia and agonists are being tested as therapy. Understanding their properties at the individual dopamine D2-family receptors is important.

KW - Dopamine hD receptor

KW - Intrinsic activity

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