Re-evaluation of lisuride pharmacology: 5-hydroxytryptamine1A receptor-mediated behavioral effects overlap its other properties in rats

  title={Re-evaluation of lisuride pharmacology: 5-hydroxytryptamine1A receptor-mediated behavioral effects overlap its other properties in rats},
  author={Danuta Marona-Lewicka and Deborah M. Kurrasch-Orbaugh and Jennifer R. Selken and Medhane G. Cumbay and Joshua G. Lisnicchia and David E. Nichols},
Abstract Rationale. There is substantial evidence that lisuride can produce effects linked to 5-HT1A receptor occupancy. Nevertheless, this action has generally been ignored in the mechanism of action of lisuride, in favor of an exclusive role for dopamine receptors in considering its antiparkinsonian effects, or an exclusive role of 5-HT2A/2C receptor activation in hallucinogenesis. These conclusions are surprising when one considers that the potent interaction of lisuride with 5-HT1A… 

LSD but not lisuride disrupts prepulse inhibition in rats by activating the 5-HT2A receptor

It is demonstrated that lisuride and LSD disrupt PPI via distinct receptor mechanisms and provide additional support for the classification of l isuride as a non-hallucinogenic 5-HT2A agonist.

ecent advances in the neuropsychopharmacology of serotonergic allucinogens

The evidence demonstrating the serotonin 5-HT2A receptor is the primary site of hallucinogen action is reviewed, showing it to be responsible for mediating the effects of hallucinationsinogens in human subjects and in animal behavioral paradigms.

Multiple receptors contribute to the behavioral effects of indoleamine hallucinogens

8R-lisuride is a potent stereospecific histamine H1-receptor partial agonist.

8R-lisuride is the most potent stereospecific partial agonist for the human H1R yet reported, and provides a valuable tool to further characterize this important therapeutic target in vitro.

Towards a biophysical understanding of hallucinogen action

This work describes a qualitative use of the h5-HT2A receptor homology model to provide a molecular basis for the pharmacological characterization of psychoactive phenylalkylamine hallucinogens and a systematic iterative approach to explore several of the receptor-binding interactions observed in virtual docking simulations to the model.

Recent advances in the neuropsychopharmacology of serotonergic hallucinogens

Aripiprazole (OPC-14597) fully substitutes for the 5-HT1A receptor agonist LY293284 in the drug discrimination assay in rats

Although the efficacy of aripiprazole against the positive symptoms of schizophrenia may be related to its dopamine receptor interactions, it seems possible that its atypical profile may derive, at least in part, from its 5-HT1A agonist effect, rather than from unusual D2 receptor properties.

Hallucinogens and Serotonin 5-HT2A Receptor-Mediated Signaling Pathways.

Recent advances in understanding hallucinogen drug action are reviewed through characterization of structure, neuroanatomical location, and function of the 5-HT2A receptor.



Dopaminergic and serotonergic mediation of the discriminable effects of ergot alkaloids.

(+)Lysergic acid diethylamide, but not its nonhallucinogenic congeners, is a potent serotonin 5HT1C receptor agonist.

The present finding that (+)LSD, but not its nonhallucinogenic congeners, is a 5HT1C receptor agonist suggests a possible role for these receptors in mediating the psychoactive effects of LSD.

Locomotor effects of lisuride: A consequence of dopaminergic and serotonergic actions

The open-field test was used to study the involvement of serotonergic and dopaminergic mechanisms in the action of lisuride on locomotor activity in the rat and concluded that the locomotor stimulant effect of higher doses of l isuride may depend on stimulation of postsynaptic dopamine receptors and a scrotonergic action.

Comparative effects of LSD and lisuride: Clues to specific hallucinogenic drug actions

  • F. J. White
  • Biology, Psychology
    Pharmacology Biochemistry and Behavior
  • 1986

Dual activation by lisuride of central serotonin 5-HT(1A) and dopamine D(2) receptor sites: drug discrimination and receptor binding studies.

Results indicate that discriminative stimulus properties of lisuride are mediated by the dual activation of 5-HT(1A) and D(2) receptor sites in brain.

Direct dopaminergic action of lisuride hydrogen maleate, an ergot derivative, in mice.

The interaction of lisuride, an ergot derivative, with serotonergic and dopaminergic receptors in rabbit brain.

Lisuride is a very potent stimulator of serotonin-sensitive adenylate cyclase in rabbit frontal cortex and can interact with serotonin and dopamine receptor binding sites in rabbit cortex and caudate nucleus.

Activity of a non-hallucinogenic ergoline derivative, lisuride, in an animal behavior model for hallucinogens

Results indicate that lisuride, a non-hallucinogenic iso-lysergic acid derivative, is a false positive in the animal behavior model for hallucinogens.