Application of the PET ligand [11C]ORM-13070 to examine receptor occupancy by the α2C-adrenoceptor antagonist ORM-12741: translational validation of target engagement in rat and human brain

Mohammed Shahid; Juha O. Rinne; Mika Scheinin; Jere Virta; Päivi Marjamäki; Olof Solin; Eveliina Arponen; Jukka Sallinen; Katja Kuokkanen; Juha Rouru

doi:10.1186/s13550-020-00741-y

Application of the PET ligand [11C]ORM-13070 to examine receptor occupancy by the α2C-adrenoceptor antagonist ORM-12741: translational validation of target engagement in rat and human brain

Mohammed Shahid, Juha O. Rinne, Mika Scheinin, Jere Virta, Päivi Marjamäki, Olof Solin, Eveliina Arponen, Jukka Sallinen, Katja Kuokkanen, Juha Rouru

Turku PET Centre

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

6 Citations (Scopus)

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Abstract

Availability of the α2C-adrenoceptor (α2C-AR) positron emission tomography (PET) tracer, [11C]ORM-13070, and the α2C-AR antagonist ORM-12741 allows probing of the roles of this G-protein coupled receptor subtype in brain function, both in healthy humans and in patients with various brain disorders. This translational study employed [11C]ORM-13070 autoradiography and PET to determine α2C-AR occupancy by ORM-12741 in rat and human brain, respectively.

Original language	English
Journal	EJNMMI Research
Volume	10
Issue number	1
DOIs	https://doi.org/10.1186/s13550-020-00741-y
Publication status	Published - 2020
MoE publication type	A1 Journal article-refereed

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10.1186/s13550-020-00741-y

s13550-020-00741-yFinal published version, 1.29 MBLicence: CC BY

https://urn.fi/URN:NBN:fi-fe202201148171

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Shahid, M., Rinne, J. O., Scheinin, M., Virta, J., Marjamäki, P., Solin, O., Arponen, E., Sallinen, J., Kuokkanen, K., & Rouru, J. (2020). Application of the PET ligand [11C]ORM-13070 to examine receptor occupancy by the α2C-adrenoceptor antagonist ORM-12741: translational validation of target engagement in rat and human brain. EJNMMI Research, 10(1). https://doi.org/10.1186/s13550-020-00741-y

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title = "Application of the PET ligand [11C]ORM-13070 to examine receptor occupancy by the α2C-adrenoceptor antagonist ORM-12741: translational validation of target engagement in rat and human brain",

abstract = "Availability of the α2C-adrenoceptor (α2C-AR) positron emission tomography (PET) tracer, [11C]ORM-13070, and the α2C-AR antagonist ORM-12741 allows probing of the roles of this G-protein coupled receptor subtype in brain function, both in healthy humans and in patients with various brain disorders. This translational study employed [11C]ORM-13070 autoradiography and PET to determine α2C-AR occupancy by ORM-12741 in rat and human brain, respectively.",

author = "Mohammed Shahid and Rinne, {Juha O.} and Mika Scheinin and Jere Virta and P{\"a}ivi Marjam{\"a}ki and Olof Solin and Eveliina Arponen and Jukka Sallinen and Katja Kuokkanen and Juha Rouru",

year = "2020",

doi = "10.1186/s13550-020-00741-y",

language = "English",

volume = "10",

journal = "EJNMMI Research",

issn = "2191-219X",

publisher = "Biomed central",

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}

Shahid, M, Rinne, JO, Scheinin, M, Virta, J, Marjamäki, P, Solin, O, Arponen, E, Sallinen, J, Kuokkanen, K & Rouru, J 2020, 'Application of the PET ligand [11C]ORM-13070 to examine receptor occupancy by the α2C-adrenoceptor antagonist ORM-12741: translational validation of target engagement in rat and human brain', EJNMMI Research, vol. 10, no. 1. https://doi.org/10.1186/s13550-020-00741-y

Application of the PET ligand [11C]ORM-13070 to examine receptor occupancy by the α2C-adrenoceptor antagonist ORM-12741: translational validation of target engagement in rat and human brain. / Shahid, Mohammed; Rinne, Juha O.; Scheinin, Mika et al.
In: EJNMMI Research, Vol. 10, No. 1, 2020.

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

TY - JOUR

T1 - Application of the PET ligand [11C]ORM-13070 to examine receptor occupancy by the α2C-adrenoceptor antagonist ORM-12741: translational validation of target engagement in rat and human brain

AU - Shahid, Mohammed

AU - Rinne, Juha O.

AU - Scheinin, Mika

AU - Virta, Jere

AU - Marjamäki, Päivi

AU - Solin, Olof

AU - Arponen, Eveliina

AU - Sallinen, Jukka

AU - Kuokkanen, Katja

AU - Rouru, Juha

PY - 2020

Y1 - 2020

N2 - Availability of the α2C-adrenoceptor (α2C-AR) positron emission tomography (PET) tracer, [11C]ORM-13070, and the α2C-AR antagonist ORM-12741 allows probing of the roles of this G-protein coupled receptor subtype in brain function, both in healthy humans and in patients with various brain disorders. This translational study employed [11C]ORM-13070 autoradiography and PET to determine α2C-AR occupancy by ORM-12741 in rat and human brain, respectively.

AB - Availability of the α2C-adrenoceptor (α2C-AR) positron emission tomography (PET) tracer, [11C]ORM-13070, and the α2C-AR antagonist ORM-12741 allows probing of the roles of this G-protein coupled receptor subtype in brain function, both in healthy humans and in patients with various brain disorders. This translational study employed [11C]ORM-13070 autoradiography and PET to determine α2C-AR occupancy by ORM-12741 in rat and human brain, respectively.

U2 - 10.1186/s13550-020-00741-y

DO - 10.1186/s13550-020-00741-y

M3 - Article

SN - 2191-219X

VL - 10

JO - EJNMMI Research

JF - EJNMMI Research

IS - 1

ER -

Application of the PET ligand [11C]ORM-13070 to examine receptor occupancy by the α2C-adrenoceptor antagonist ORM-12741: translational validation of target engagement in rat and human brain

Abstract

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