Discriminative Stimulus Effect of the Serenic Eltoprazine

Ybema, Caroline E.; Olivier, Berend; Slangen, Jef L.

doi:10.1097/00008877-199204001-00118

Cited by 2 publications

(5 citation statements)

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“…Training is proceeding very slowly, and even after more than 60 sessions it has not yet reached a satisfactory level. Our experience contrasts with that with 5-HT agonists, such as flesinoxan and eltoprazine, which are learned quite rapidly (Ybema et al, 1990(Ybema et al, , 1992. in the number of ß-receptors in certain cortical layers.…”

Section: Subchronic Effectsmentioning

confidence: 71%

Preclinical Evidence on the Psychotropic Profile of Fluvoxamine

Olivier¹,

Bosch²,

Hest³

et al. 1993

Pharmacopsychiatry

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Serotonin (5-HT) reuptake inhibitors (SSRIs) such as fluvoxamine are interesting compounds. Initially launched as antidepressants, they have been found to be active in various psychiatric disorders besides depression, including obsessive-compulsive disorder, panic disorder, and eating disturbances. Preliminary data suggest their efficacy in alcohol and drug abuse, aggression, and posttraumatic stress disorder as well. Along with those clinical findings, new preclinical data have emerged. For example, fluvoxamine has demonstrated activity in various models of anxiety in rodents. Its anxiolytic activity can be clearly discriminated from that of the benzodiazepines. In the DRL 72-sec paradigm, fluvoxamine exhibits a good antidepressant profile, similar to those of imipramine and flesinoxan. Studies have shown that fluvoxamine does not down-regulate beta-adrenoceptors; apparently, that property is not a conditio sine qua non for antidepressant activity. Results of studies of the mechanism of action of fluvoxamine in which drug discrimination tests were performed with rats and pigeons suggest that the fluvoxamine stimulus is not (or is only to a very limited degree) dependent on activation of 5-HT1A receptors or 5-HT1B/1D receptors, or both. Experimentation is ongoing in those animal models.

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Section: Subchronic Effectsmentioning

confidence: 71%

Preclinical Evidence on the Psychotropic Profile of Fluvoxamine

Olivier¹,

Bosch²,

Hest³

et al. 1993

Pharmacopsychiatry

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“…The results of the in vitro binding studies in rat frontal cortex homogenates of the target compounds [7][8][9][10][11][12][13][14][15][16][17][18] are summarized in Table 2. Succinimidyl compound 7 has only a moderate affinity for the 5-HTia receptor (pX¡ = 6.96).…”

Section: Resultsmentioning

confidence: 99%

“…2-[2-[4-(2,3-Dihydro-l,4-benzodioxin-5-yl)-l-piperazinyl]ethyl]-3a,4,7,7a-tetrahydro-LH-isoindole-l,3(2fl)-dione, Dihydrochloride (10). Compound 10 was prepared using cis-1.2.3.6-tetrahydrophthalic anhydride and the piperazineethanamine 20.…”

Section: Methodsmentioning

confidence: 99%

“…[3][4][5][6] The discovery of other heteroarylpiperazines as potent 5-HTia ligands such as N4substituted derivatives of eltoprazine (3) and 4, e.g., the phenylbutyl derivative 5, and flesinoxan (6) has resulted in the pharmacological evaluation of these drugs as potential central nervous system (CNS) drugs. [7][8][9][10] In this paper the synthesis of a new series of N4imidoethyl derivatives (7)(8)(9)(10)(11)(12)(13)(14)(15)(16)(17)(18) of eltoprazine (3) and their affinity for the 5-HTia receptor are described. The correlation of the inhibition constant pif, or the local inhibition constant pKi+ with the pKa and clogP was investigated.…”

Section: Introduction Chart 1 Structures Of 5-htia Ligandsmentioning

confidence: 99%

“…Displacement of [3H]-2-(Di-n-propylamino)-8hydroxytetralin: Binding to 5-HTia Recognition Sites in Rat Frontal Cortex Homogenates of Compounds[7][8][9][10][11][12][13][14][15][16][17][18] …”

mentioning

confidence: 99%

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A Series of N4-Imidoethyl Derivatives of 1-(2,3-Dihydro-1,4-benzodioxin-5-yl)piperazine as 5-HT1A Receptor Ligands: Synthesis and Structure-Affinity Relationships

Wijngaarden²,

Mt³

et al. 1995

J. Med. Chem.

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A series of unsubstituted and substituted succinimido, maleimido, and glutarimidoethyl derivatives of eltoprazine (3) was synthesized and tested for affinity for the 5-HT1A receptor in rat brain homogenates. The unsubstituted compounds have a moderate affinity for the receptor, while the affinity considerably increases by substitution at or enlargement of these cyclic ring systems. A good correlation was found between the inhibition constant Ki (expressed as pKi) and the lipophilicity (clogP). No correlation was observed between the pKi or pKi+ (local inhibition constant) and the basicity of the N4-nitrogen atom.

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Discriminative Stimulus Effect of the Serenic Eltoprazine

Cited by 2 publications

References 0 publications

Preclinical Evidence on the Psychotropic Profile of Fluvoxamine

Preclinical Evidence on the Psychotropic Profile of Fluvoxamine

A Series of N4-Imidoethyl Derivatives of 1-(2,3-Dihydro-1,4-benzodioxin-5-yl)piperazine as 5-HT1A Receptor Ligands: Synthesis and Structure-Affinity Relationships

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