Potential Neuroleptic Agents. Part 4. Chemistry, Behavioral Pharmacology and Inhibition of [3H]Spiperone Binding of 3,5‐Disubstituted N‐[(1‐Ethyl‐2‐pyrrolidinyl)methyl]‐6‐methoxysalicylamides.

  title={Potential Neuroleptic Agents. Part 4. Chemistry, Behavioral Pharmacology and Inhibition of [3H]Spiperone Binding of 3,5‐Disubstituted N‐[(1‐Ethyl‐2‐pyrrolidinyl)methyl]‐6‐methoxysalicylamides.},
  author={Tomas de Paulis and Yatendra Kumar and Lars George Johansson and Sten Ingvar Raemsby and H. Hall and M. Saellemark and K. Aengeby‐Moeller and Sven Ove Oegren},
Die Carbonsauren (II) werden in die Amide (III) und (IV) umgewandelt, von denen (III) (R′, R2 = C1) auf Grund der Voruntersu-g chungsergebnisse klinisch gegen Schizophrenie untersucht werden soll. 
Carbon-11 labelling of eticlopride in two different positions--a selective high-affinity ligand for the study of dopamine D-2 receptors using PET.
A new highly selective high-affinity dopamine D-2 receptor antagonist, eticlopride, labelled with 11C in two different positions was injected in a Cynomolgus monkey and brain radioactivity was measured by positron emission tomography (PET). Expand
Synthesis and structure-activity relationships of 4-amino-5-chloro-N-(1,4-dialkylhexahydro-1,4-diazepin-6-yl)-2-methoxybenzamide derivatives, novel and potent serotonin 5-HT3 and dopamine D2 receptors dual antagonist.
In search of a dopamine D2 and serotonin 5-HT3 receptors dual antagonist as a potential broad antiemetic agent, a number of benzamides were prepared from 4-amino-5-chloro-2-methoxybenzoic acid derivatives and 6-aminos-1-4-dialkylhexahydro-1,4-diazepines and evaluated for their binding affinity using rat brain synaptic and rat cortical membranes. Expand
A Review of the Discovery, Pharmacological Characterization, and Behavioral Effects of the Dopamine D2‐Like Receptor Antagonist Eticlopride
This review highlights research utilizing this drug and compares it to typical and atypical antipsychotics used clinically and discusses the use of eticlopride in several behavioral models predictive of antipsychotic activity, extrapyramidal side effects (EPS), and learning and memory. Expand
Interaction of antipsychotic drugs with neurotransmitter receptor sites in vitro and in vivo in relation to pharmacological and clinical effects: role of 5HT2 receptors
Differentiation between the various D2 receptor mediated effects may be made more easily, allowing EPS-free maintenance therapy of schizophrenic patients, and it may be of prime importance to carefully titrate drug dosages. Expand
NCQ 298, a new selective iodinated salicylamide ligand for the labelling of dopamine D2 receptors
The specific properties of [123I]NCQ 298 suggest that this compound is a useful ligand for quantitative SPECT studies of dopamine D2 receptors in man. Expand
A comparative PET-study of five carbon-11 or fluorine-18 labelled salicylamides. Preparation and in vitro dopamine D-2 receptor binding.
  • C. Halldin, L. Farde, +4 authors O. Solin
  • Chemistry, Medicine
  • International journal of radiation applications and instrumentation. Part B, Nuclear medicine and biology
  • 1991
Five 11C- or 18F-labelled salicylamides prepared and examined in vitro and found that with both analogs I and II there was a high uptake in the striatum, a region with a high density of dopamine D-2 receptors, whereas the affinity of NCQ 135 was similar to that of eticlopride. Expand
Reversal of stress-induced anhedonia by the atypical antidepressants, fluoxetine and maprotiline
Previous reports of the efficacy of tricyclic antidepressants in this paradigm are extended, and support the hypothesis of a dopaminergic mechanism of antidepressant action. Expand
Stereospecific reversal of stress-induced anhedonia by mianserin and its (+)-enantiomer
The results suggest that (+)-mianserin is the active enantiomer in reversing chronic mild stress-induced anhedonia, and further support the hypothesis of a dopaminergic mechanism of antidepressant action in this paradigm. Expand
Apomorphine and pergolide induce hypothermia by stimulation of dopamine D-2 receptors.
D-2 dopamine receptors appear to play a decisive role in the mediation of the hypothermic response of apomorphine and pergolide in the rat and there may also exist an interaction between D-1 and D-2 receptors in the expression of DA-agonist-induced hypothermia. Expand
QSAR on Substituted Salicylamides Using with Implementation of 3D MEP Descriptors
A QSAR analysis of the [3H]spiperone binding affinity of 25 mono- and disubstituted salicylamides having F, Cl, Br, Me and Et substituents in the 3- and 5-positions have been done with PLS (partialExpand


Potential neuroleptic agents. 4. Chemistry, behavioral pharmacology, and inhibition of [3H]spiperone binding of 3,5-disubstituted N-[(1-ethyl-2-pyrrolidinyl)methyl]-6-methoxysalicylamides.
One compound, S-(-)-3,5-dichloro-N-[(1-ethyl-2-pyrrolidinyl) methyl]-6-methoxysalicylamide (raclopride, FLA 870) (13) had a stereotypy--hyperactivity separation more than twice that of sulpiride while being 100 times more potent in blocking the apomorphine effects. Expand