Molecular pharmacology of 5-HT1D recognition sites: Radioligand binding studies in human, pig and calf brain membranes

  title={Molecular pharmacology of 5-HT1D recognition sites: Radioligand binding studies in human, pig and calf brain membranes},
  author={Christian Waeber and Philippe Schoeffter and Jos{\'e} Mar{\'i}a Palacios and Daniel Hoyer},
  journal={Naunyn-Schmiedeberg's Archives of Pharmacology},
Summary1)The binding characteristics of [3H]5-HT (5-hydroxytryptamine, serotonin) were investigated in membrane preparations of several regions from calf, pig and human brain in the presence of 100 nmol/l 8-OH-DPAT (8-hydroxy-2[di-n-dipropylamino]tetralin) and 100 nmol/l mesulergine in order to mask 5-HT1A and 5-HT1C sites.2)[3H]5-HT bound rapidly, reversibly and stereo-selectively to a population of high affinity recognition sites in membranes from pig caudate, calf caudate and human cortex… 

5-HT1D receptors in guinea-pig and pigeon brain

It is suggested that 5-HT1D sites may be present in the brain of the majority of vertebrate species located higher than the sauropside-mammalian divergence in the phylogenic tree, whereas 5- HT1B sites are only found in some rodents.

5.HT1 receptors in the vertebrate brain

The regional distribution of high affinity [33H]5-HT recognition sites in the brain of several vertebrates (pigeon, rat, mouse, guinea-pig, cat, dog, monkey and human) was analyzed using in vitro autoradiography and suggested that the majority of 5-HT1 sites belong to the 5- HT1D subtype in the pigeon brain.

“5-HT1R” or 5-HT1D sites? Evidence for 5-HT 1D binding sites in rabbit brain

The present data strongly suggest that rabbit brain has recognition sites with the pharmacological profile and distribution characteristic of the 5-HT1D recognition site and are in agreement with results obtained by Limberger et al. (1991).

[3H]sumatriptan labels both 5-HT1D and 5-HT1F receptor binding sites in the guinea pig brain: an autoradiographic study

In vitro autoradiography data show that [3H]sumatriptan, in the presence of 10 nM 5-carboxamidotryptamine, is a more suitable radioligand to study the distribution of 5-HT1F binding sites.

5-HT1D binding sites in various species: similar pharmacological profile in dog, monkey, calf, guinea-pig and human brain membranes

The pharmacological profile of 5-HT1D sites in dog and monkey brain is established for the first time and shows that the pharmacological characteristics of these sites is indeed very similar in the brain of a variety of species including man, and demonstrates the advantageous features of [1251]GTI as an iodinated 5- HT1D radioligand which can be used without the need to mask the binding to other5-HT receptor subtypes.

Metitepine distinguishes two receptors mediating inhibition of [3H]-5-hydroxytryptamine release in guinea pig hippocampus

Heterogeneity in the receptor mediating inhibition of [3H]-5-HT release in guinea pig hippocampus is suggested, as well as the ability of metitepine to antagonise the effects of sumatriptan or 5-CT in this model.

Evidence for presynaptic location of inhibitory 5-HT1D\-like autoreceptors in the guinea-pig brain cortex

The potencies of the agonists in inhibiting tritium overflow from slices correlated with those in synaptosomes, suggesting that the same site of action is involved in both preparations, and the 5-HT receptors mediating inhibition in the guinea-pig cortex are located on the serotoninergic axon terminals and represent presynaptic inhibitory autoreceptors.

Autoradiographic characterisation and localisation of 5-HT1D compared to 5-HT1B binding sites in rat brain

The regional distribution and the pharmacology of the binding sites labelled with the novel 5-hydroxytryptamine (serotonin) 5-HT1B/1D selective radioligand serotonin-O-carboxy-methyl-glycyl-[125I]tyrosinamide (abbreviated [ 125I]GTI) was determined using quantitative autoradiography in rat brain.



Characterization of a novel 3H-5-hydroxytryptamine binding site subtype in bovine brain membranes

  • R. E. HeuringS. Peroutka
  • Biology, Chemistry
    The Journal of neuroscience : the official journal of the Society for Neuroscience
  • 1987
The data demonstrate the presence of a homogeneous class of 5- HT1 binding sites in bovine caudate that is pharmacologically distinct from previously defined 5-HT1A, 5-ht1B, 5 - HT1C, 4-HT2, 3-HT3 receptor subtypes.

Characterization of the 5-HT1B recognition site in rat brain: binding studies with (-)[125I]iodocyanopindolol.

The binding of serotonergic ligands to the porcine choroid plexus: characterization of a new type of serotonin recognition site.

5-HT1A-receptors mediate stimulation of adenylate cyclase in rat hippocampus

Data support the concept that 5-HT stimulated adenylate cyclase activity in rat hippocampus is mediated by a5-HT1A receptor, as pharmacologically characterised with a series of agonists and antagonists of various structural classes.

Identification of serotonin 5-HT3 recognition sites in membranes of N1E-115 neuroblastoma cells by radioligand binding.

Competitive in nature, as demonstrated by saturation experiments carried out with [3H]ICS 205-930 in the presence and the absence of unlabeled compounds: apparent Bmax values were not reduced, whereas apparent KD values were increased inThe presence of competing ligands.