Interactions of isamoltane (CGP 361A), an anxiolytic phenoxypropanolamine derivative, with 5-HT1, receptor subtypes in the rat brain

@article{Waldmeier2004InteractionsOI,
  title={Interactions of isamoltane (CGP 361A), an anxiolytic phenoxypropanolamine derivative, with 5-HT1, receptor subtypes in the rat brain},
  author={Peter C. Waldmeier and Michael J.A. Williams and Peter A. Baumann and Serge François Bischoff and Matthew A. Sills and Robert F. Neale},
  journal={Naunyn-Schmiedeberg's Archives of Pharmacology},
  year={2004},
  volume={337},
  pages={609-620}
}
SummaryIsamoltane (CGP 361A; (1-(2-(1-pyrrolyl)phenoxy)-3-isopropylamino-2-propanol hydrochloride), β-adrenoceptor ligand (IC50 = 8.4 nmol/l) which has reported activity as an anxiolytic in man was found to be a reasonably active inhibitor of the binding of [125I]ICYP to 5-HT1B recognition sites in rat brain membranes with 27-fold selectivity (IC50 = 39 nmol/l) as compared to the inhibition of binding of [3H]8-OH-DPAT to 5-HT1A receptors (IC50 = 1070 nmol/l). This selectivity was considerably… 
Interaction of arylpiperazines with 5-HT1A, 5-HT1B, 5-HT1C and 5-HT1D receptors: do discriminatory 5-HT1B receptor ligands exist?
TLDR
Five putative 5-HT1 receptorsubtype selective ligands have different pharmacological profiles as predicted from radioligand binding studies, and despite claims to the contrary, none of the tested compounds had actual selectivity for a given 5- HT1 receptor subtype.
Biochemical and behavioural effects of isamoltane, a β-adrenoceptor antagonist with affinity for the 5-HT1B receptor of rat brain
TLDR
Observations indicate that isamoltane, by inhibiting the terminal 5HT autoreceptors, increased the synaptic concentration of 5-HT to a level that induced a behavioural response.
5-Hydroxytryptamine 5-HT1B and 5-HT1D receptors mediating inhibition of adenylate cyclase activity
TLDR
The results strengthen the identity between 5-HT receptors mediating inhibition of adenylate cyclase activity in rat and calf substantia nigra and 5- HT1B and5-HT1D binding sites, respectively and underline the differences between these receptors in terms of intrinsic activities and potencies of drugs.
CGP 28014, a new inhibitor of cerebral catechol-O-methylation with a non-catechol structure
TLDR
The in vivo effect of CGP 28014 held a potential to improve the efficacy of L-DOPA in the treatment of parkinsonism and to be equipotent or nearly so with tropolone, and also showed a similar duration of action.
Contribution of 5-Hydroxytryptamine1B Receptors and 20-Hydroxyeiscosatetraenoic Acid to Fall in Cerebral Blood Flow After Subarachnoid Hemorrhage
TLDR
The results suggest that the release of 5-HT after SAH activates5-HT1B receptors and the synthesis of 20- HETE and that 20-HETE contributes to the acute fall in rCBF by potentiating the vasoconstrictor response of cerebral vessels to 5- HT.
Contribution of 5-Hydroxytryptamine 1 B Receptors and 20-Hydroxyeiscosatetraenoic Acid to Fall in Cerebral Blood Flow After Subarachnoid Hemorrhage
TLDR
The results suggest that the release of 5-HT after SAH activates5-HT1B receptors and the synthesis of 20-HETE and that 20- HETE contributes to the acute fall in rCBF by potentiating the vasoconstrictor response of cerebral vessels to 5- HT.
Effects of the putative P-type calcium channel blocker, R,R-(−)-daurisoline on neurotransmitter release
TLDR
It is thought that the R,R-(−)-daurisoline compound is suitable to test whether blockade of glutamate release via voltage-sensitive Ca2+ channels is a viable concept to obtain novel neuroprotective and/or anticonvulsant compounds.
Effects of CGP 28014 on the in vivo release and metabolism of dopamine in the rat striatum assessed by brain microdialysis
TLDR
The inhibition of COMT is likely to be due to the action of a metabolite of CGP 28014 formed in the periphery and not in the brain, as well as a concentration-dependent, several-fold increase in extracellular DA.
The effects of the dopamine stabilizer (−)-OSU6162 on aggressive and sexual behavior in rodents
The dopamine stabilizer (−)-OSU61612 dampens locomotion in rodents rendered hyperactive by exposure to a novel environment or treatment with amphetamine, but stimulates locomotion in habituated
...
...

References

SHOWING 1-10 OF 102 REFERENCES
Biochemical and pharmacological characterization of CGS 12066B, a selective serotonin-1B agonist.
Selective interaction of novel anxiolytics with 5-hydroxytryptamine1A receptors
Characterization of a novel 3H-5-hydroxytryptamine binding site subtype in bovine brain membranes
  • R. E. Heuring, S. Peroutka
  • Biology, Chemistry
    The Journal of neuroscience : the official journal of the Society for Neuroscience
  • 1987
TLDR
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.
Evaluation of the binding of the A-1 selective adenosine radioligand, cyclopentyladenosine (CPA), to rat brain tissue
TLDR
It was found that CHA, S-PIA and the antagonist, PACPX were more active in displacing CHA than CPA, in general however, CPA has a binding profile very similar to that observed with CHA.
Serotonin autoreceptor in rat hippocampus: Pharmacological characterization as a subtype of the 5-HT1 receptor
TLDR
5-HT nerve terminals of rat hippocampus possess autoreceptors which appear to belong to the 5-HT1B subtype, which is characterized pharmacologically in terms of 5- HT receptor subtype by using superfused synaptosomes depolarized with 15 mM KCl.
Characterization of the A2 adenosine receptor labeled by [3H]NECA in rat striatal membranes.
TLDR
The regional distribution of [3H]NECA binding and the affinities of adenosine agonists and antagonists for inhibition of binding indicate that the site labeled by [3NECA belongs to the high affinity, or A2a, subclass of A2 receptor.
...
...