receptor antagonist (pKi
= 8.2). Displays > 60-fold selectivity over 5-HT1D
receptors in radioligand binding and functional assays. Centrally active following oral administration in vivo
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Stimulation of 5-HT1B receptors causes hypothermia in the guinea-pig.
Hagan et al.
The selective 5-HT1B receptor inverse agonist 1'-methyl-5-[[2'-methyl-4'-(5-methyl-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]carbonyl]-2,3,6,7-tetrahydrospiro[furo[2,3-f]indole-3,4'-piperidine (SB-224289) potently blocks terminal 5-HT
Gaster et al.
Differential effects of 5-HT1B/1D receptor antagonists in dorsal and median raphe innervated brain regions.
Roberts et al.
SB-224289 - a novel selective (human) 5-HT1B receptor antagonist with negative intrinsic activity.
Selkirk et al.
The citations listed below are publications that use Tocris products. Selected citations for SB 224289 hydrochloride include:
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