Preclinical pharmacology of ropinirole (SK&F 101468-A) a novel dopamine D2 agonist

  title={Preclinical pharmacology of ropinirole (SK\&F 101468-A) a novel dopamine D2 agonist},
  author={Rebecca Eden and Brenda Costall and Annette M. Domeney and Philip A. Gerrard and Carol A. Harvey and M. Elizabeth Kelly and Robert J. Naylor and David A. A. Owen and A Wright},
  journal={Pharmacology Biochemistry and Behavior},

Anxiolytic profile of ropinirole in the rat, mouse and common marmoset

Ropinirole did not compromise the effect of amitriptyline in the Porsolt test of depression and in itself produced antidepressant-like effects and may predict an action of ropinirole in man that would provide a superior profile of action over other presently available anti-parkinsonian agents.

S32504, a Novel Naphtoxazine Agonist at Dopamine D3/D2 Receptors: II. Actions in Rodent, Primate, and Cellular Models of Antiparkinsonian Activity in Comparison to Ropinirole

S32504 displays potent and stereospecific activity in rodent, primate, and cellular models of antiparkinsonian properties and engagement of D3 receptors contributes to its neuroprotective properties.

D(2), but not D(1) dopamine receptor agonists potentiate cannabinoid-induced sedation in nonhuman primates.

Modulation of D(2) dopamine receptor activity by a nonsedating dose of a cannabinoid agonist has implications for the pathophysiology and treatment of dopamine-related neuropsychiatric disorders and drug addiction.

The Effects of a Selective Dopamine D2 Receptor Agonist on Behavioral and Pathological Outcome in 1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine-Treated Squirrel Monkeys

Results suggest that sumanirole can exert antiparkinsonian effects similar to l-DOPA without the behavioral and morphological consequences of the latter.

S32504, a Novel Naphtoxazine Agonist at Dopamine D3/D2 Receptors: I. Cellular, Electrophysiological, and Neurochemical Profile in Comparison with Ropinirole

D3/D2 agonist and antiparkinsonian agent ropinirole mimicked the profile of S32504, which is a potent and selective agonist at dopamine D3 and D2 receptors.

Ligands for the dopamine D 2-like receptors

This study synthesized a series of substituted N-(1-benzyl-piperidin-4-yl)benzamides with varying degrees of DA D4 selectivity, and tested four of these benzamides for their ability to inhibit Damphetamine-induced hyperactivity in the rat.



MK 458, a selective and potent D2 receptor agonist in advanced Parkinson's disease.

While the reduction in signs of PD was comparable to those on levodopa, MK 458 did not induce dyskinesias or dystonias, and it is postulated that MK 458 may be able to replace levodOPA as the primary treatment for PD.

Effects of chronic oral administration of the antidepressants, desmethylimipramine and zimelidine on rat cortical GABAB binding sites: a comparison with 5‐HT2 binding site changes

It may be concluded that the effects of antidepressant administration upon GABAB binding sites is a less consistent observation than their effects on 5‐HT2 binding sites.

Striatal dopamine release after amphetamine or nerve degeneration revealed by rotational behaviour.

  • U. Ungerstedt
  • Biology
    Acta physiologica Scandinavica. Supplementum
  • 1971
Amphetamine induced vigorous rotational behaviour in rats where the nigrostriatal dopamine system was unilaterally degenerated by an intracerebral injection of 6-hydroxydopamine (6-OH-DA) and evidence was obtained that the amphetamine induced release of DA was dependent upon nerve impulses.

Mouse locomotor activity: an in vivo test for dopamine autoreceptor activation.

A pharmacologic test is described for assessing selective dopamine (DA) autoreceptor activation using locomotor activity (LMA) of the mouse as the dependent variable. In this test, three criteria

Serotonin and lysergic acid diethylamide binding in rat brain membranes: relationship to postsynaptic serotonin receptors.

The ontogeny of 5- HT and LSD binding sites is nearly identical and does not appear to depend on functionally intact presynaptic 5-HT neuronal input.

Effect of apomorphine on motility in rats.