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

7 Citations (Scopus)

106 Downloads (Pure)

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

@article{3590af3d65de4866a8ba819d5cbd4b69,

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",

number = "1",

}

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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