More Binding More Fun 151 Using Beta Blockers

We subsequently published evidence (Hoyer et al. 1985a) that brain 5-HT1/ [3H]5-HT binding could be displaced in a triphasic manner by a beta-blocker (SDZ 21-009), which was characterized by high affinity for 5-HT1B sites, intermediate for 5-HT1A sites, and very low affinity for 5-HT1C sites. Our autoradiographic data had also demonstrated the ability of this compound to selectively bind to 5-HT1B sites in specific brain areas (Hoyer et al. 1985a, b). Some further indole beta-blockers turned out to be very important tools for the delineation of 5-HT1 receptor subtypes. Indeed, we noticed that ICYP, [125I]iodocyanopindolol, a very potent antagonist at b-adrenoceptors, which is still the most popular radioligand for labeling these receptors (Engel et al. 1981; Hoyer et al. 1982), was also binding in the brain to sites sensitive to 5-HT and other serotoninergic ligands. Although the radioligand was initially described (in 1981) as highly specific for beta-receptors, we had to admit that it was perfectly suitable to label 5-HT1B receptors in rodents but not in other species.

Defeat Drugs and Live Free

Defeat Drugs and Live Free

Being addicted to drugs is a complicated matter condition that's been specified as a disorder that evidences in the obsessional thinking about and utilization of drugs. It's a matter that might continue to get worse and become disastrous and deadly if left untreated.

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