Pindolol binding to 5-HT1A receptors in the human brain confirmed with positron emission tomography.

Abstract:

:The augmentation effect of (-)pindolol as used in combination with SSRI to treat major depression has been ascribed to blocking of dorsal raphe nucleus cell body 5-HT autoreceptors. In this study, the radioligand [carbonyl-11C]WAY-100635 and positron emission tomography were used to establish whether pindolol at a clinical dose level (10 mg s.o.d.) occupies 5-HT1A receptors in the human brain in vivo. Three healthy males were recruited and each subject was used as his own control. The 5-HT1A receptor occupancy was calculated for the frontal and temporal cortex and the raphe nuclei, using and a ratio analysis with the cerebellar cortex as the reference region. Maximal pindolol plasma concentration was reached within 3 h after drug administration. Two hours after pindolol administration, the regional 5-HT1A receptor occupancy was within the range 7-21% in the three subjects. The study confirms that the 5-HT1A-receptor may be a clinically significant target for pindolol.

journal_title

Psychopharmacology

authors

Andrée B,Thorberg SO,Halldin C,Farde L

doi

10.1007/s002130051009

subject

Has Abstract

pub_date

1999-06-01 00:00:00

pages

303-5

issue

3

eissn

0033-3158

issn

1432-2072

journal_volume

144

pub_type

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