Brain histamine H₁ receptor occupancy after oral administration of desloratadine and loratadine.

ABSTRACT: Some histamine H₁ receptor (H₁R) antagonists induce adverse sedative reactions caused by blockade of histamine transmission in the brain. Desloratadine is a second-generation antihistamine for treatment of allergic disorders. Its binding to brain H₁Rs, which is the basis of sedative property of antihistamines, has not been examined previously in the human brain by positron emission tomography (PET). We examined brain H₁R binding potential ratio (BPR), H₁R occupancy (H₁RO), and subjective sleepiness after oral desloratadine administration in comparison to loratadine. Eight healthy male volunteers underwent PET imaging with [¹¹C]-doxepin, a PET tracer for H₁Rs, after a single oral administration of deslor

SUBMITTER: Nakamura T 

PROVIDER: S-EPMC6624455 | biostudies-literature | 2019 Aug

REPOSITORIES: biostudies-literature