Biochemical and behavioural effects of isamoltane, a β-adrenoceptor antagonist with affinity for the 5-HT1B receptor of rat brain

  title={Biochemical and behavioural effects of isamoltane, a $\beta$-adrenoceptor antagonist with affinity for the 5-HT1B receptor of rat brain},
  author={Lucy R{\'e}nyi and Lars-Gunnar Larsson and Stefan von Berg and B. E. Svensson and Gun Thorell and Svante B. Ross},
  journal={Naunyn-Schmiedeberg's Archives of Pharmacology},
SummaryThe biochemical and behavioural effects of isamoltane, a \-adrenoceptor and 5-HT1B receptor antagonist that has higher affinity for 5-HT1B receptors than for 5-HTIA receptors, on 5-HT neurotransmission in the rat brain were examined. In binding experiments isamoltane was found to be about five times more potent as a ligand for the 5-HT1B receptor than for the 5-HT1A receptor (Ki values 21 and 112 nmol/l, respectively). Isamoltane increased the K+-evoked overflow of 3H from 3H-5-HT loaded… 
Serotonin (5-HT) activation of immortalized hypothalamic neuronal cells through the 5-HT1B serotonin receptor.
Findings support the model wherein 5-HT action through the 1B receptor subtype occurs directly on PVN neurons, leading to potential modification of neuronal transcriptional and secretory machinery.
New Findings on the Sensitivity of Free-Operant Timing Behaviour to 5-Hydroxytryptamine Receptor Stimulation
The results suggest that mCPP’s effect on timing is mediated by an agonistic action at 5-HT1A and 4-HT2A, but not 5- HT1B, receptors, while Ro-600175 had no effect on T50.
Return of the lysergamides. Part IV: Analytical and pharmacological characterization of lysergic acid morpholide (LSM-775).
Findings suggest that 5-HT1A activation by L SM-775 masks its ability to induce the head twitch response, which is potentially consistent with reports in the literature indicating that LSM-775 is only capable of producing weak LSD-like effects in humans.
Reversal of inflammatory and noninflammatory visceral pain by central or peripheral actions of sumatriptan.
The findings suggest that sumatriptan suppresses either inflammatory or noninflammatory visceral pain, most likely through peripheral 5HT1(B)/(D) receptors.
N-Pyrrylarylsulfones with High Therapeutic Potential
The literature reviewed here may provide useful information on the potential of N-pyrrylarylsulfone pharmacophore as well as suggest concepts for the design and synthesis of new N-tetracyclic, tricyclic and non-cyclic compounds.
Cascade Synthesis of Pyrroles from Nitroarenes with Benign Reductants Using a Heterogeneous Cobalt Catalyst
The general synthetic utility of this methodology was demonstrated on a variety of functionalized substrates including the preparation of biologically active and pharmaceutically relevant compounds, for example, (+)‐Isamoltane.


Serotonin autoreceptor in rat hippocampus: Pharmacological characterization as a subtype of the 5-HT1 receptor
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.
Interactions of isamoltane (CGP 361A), an anxiolytic phenoxypropanolamine derivative, with 5-HT1, receptor subtypes in the rat brain
In vivo, isamoltane increased 5-HTP accumulation in rat cortex following central decarboxylase inhibition at doses of 1 and 3 mg/kg i.
Identity of inhibitory presynaptic 5-hydroxytryptamine (5-HT) autoreceptors in the rat brain cortex with 5-HT1B binding sites
In rat brain cortex slices preincubated with [3H]5-HT, the evidence indicates that the presynaptic 5- HT autoreceptor belongs to the 5-HT1B receptor subtype.
Pharmacological characterization of release-regulating serotonin autoreceptors in rat cerebellum.
Antagonistic properties of quipazine at presynaptic serotonin receptors and α-adrenoceptors in rat brain cortex slices
It is concluded that quipazine blocks presynaptic inhibitory serotonin receptors and α-adrenoceptors on monoaminergic neurones of the rat brain cortex.
Characterization of 5‐hydroxytryptaminergic autoreceptors in the rat hypothalamus
The 5‐HT autoreceptor in the rat hypothalamus is characterized using a classical pharmacological approach and it is found that it has more in common with the Autoreceptor which has been previously identified in the raphe nuclei of the rat than it has with the 5‐ HT receptor located on dopamine neuroterminals in the striatum.
Characterization of the 5-HT1B recognition site in rat brain: binding studies with (-)[125I]iodocyanopindolol.