Bifeprunox is a potent partial agonist of dopamine D2-like and 5-HT1A receptor (pEC50: 6.37 for hippocampus 5-HT1A; pKis: 7.19 and 8.83 for cortex 5-HT1A and striatum D2). It is an antipsychotic for the research of schizophrenia.
PK14105 has been evaluated biologically as a potential radioligand for positron emission tomography (PET) studies targeting peripheral benzodiazepine binding sites (PBBS) receptors. When administered to rats with unilaterally lesioned striata, PK14105 was observed to quickly cross the blood-brain barrier, displaying significant radioactivity retention in the lesioned striatum, in contrast to the unlesioned striatum or cerebellar vermis. Additionally, PK14105 has the capability to inhibit receptor ligands, calcium channel ligands, and co-transporters in all salivary glands.
ADCI is an inhibitor of voltage-activated sodium channels and N-methyl-D-aspartate (NMDA)-receptor-gated channels. Inhibition of sodium channels by ADCI was voltage dependent. High doses of ADCI increased dopamine metabolism in the prefrontal cortex and o
CGP 56999A is an antagonist of GABA(B) receptor, it enhances expression of brain-derived neurotrophic factor and attenuates dopamine depletion in the rat corpus striatum.
GSK-215083 is a PET radioligand for the 5-HT6 receptor. GSK 215083 is a quinoline based compounds and acts by antagonising the 5-HT6 receptor. GSK-215083 binds to receptors 5-hydroxytrypamine-6 (5HT6) in the striatum and 5-hydroxytryptamine-2A (5HT2A) in
PD 142505-0028, a functionally M1-selective muscarinic agonist, rapidly increases glutamate but not aspartate concentrations in the striatum of anesthetized rats. Additionally, it inhibited production of amyloidogenic A beta and increased secretion of sol
Trazium esilate is an adrenergic receptor antagonist. Trazium esilate is a weak displacer on a1-, a2- and D2-receptors, however, it induced a2-receptor desenzitization after repeated treatment. It had no influence on rat brain cortical noradrenaline and s