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Upstream product

• 176639-73-9 C₁₅H₂₂N₂O₂S 
• 3308-94-9 4-chloro-1-(4-fluorophenyl)-1,1-(ethylenedioxy)butane 
• 5650-51-1 5,6-dihydro-<6H>-cyclopenta--thiophene-4-one 
• 176639-50-2 4-oxo-4H-5,6-dihydrocyclopentathiophene-5-ylacetic acid 
• 176639-49-9 (4-Oxo-5,6-dihydro-4H-cyclopenta[b]thiophen-5-yl)-acetic acid ethyl ester 
• 176639-68-2 N¹-<(4-oxo-4H-5,6-dihydrocyclopentathiophene-5-yl)acetyl>piperazine ethylene ketal 
• 176639-58-0 N¹-<(4-oxo-4H-5,6-dihydrocyclopentathiophene-5-yl)acetyl>-N⁴-(tert-butoxycarbonyl)piperazine 
• 240404-06-2 N¹-<(4-oxo-4H-5,6-dihydrocyclopentathiophene-5-yl)acetyl>piperazine 
• 176639-53-5 (4-Oxo-5,6-dihydro-4H-cyclopenta[b]thiophen-5-yl)-acetyl chloride 

Relevant academic research and scientific papers

Conformationally constrained butyrophenones with mixed dopaminergic (D2) and serotoninergic (5-HT2(A), 5-HT2(C)) affinities: Synthesis, pharmacology, 3D-QSAR, and molecular modeling of (aminoalkyl)benzo- and - thienocycloa

A series of novel conformationally restricted butyrophenones (2- (aminoethyl)- and 3-(aminomethyl)thieno- or benzocycloalkanones bearing (6- fluorobenzisoxazolyl)piperidine, (p-fluorobenzoyl)piperidine, (o- methoxyphenyl)piperazine, or linear butyrophenon

Synthesis and affinities for dopamine (D2) and 5-hydroxytryptamine (5-HT2A) receptors of 1-(benzoylpropyl)-4-(1-oxocycloalkyl-2-ethyl)-piperazines as cyclic butyrophenone derivatives

Starting from benzo- or thienocycloalkaneacetic acids, we have prepared a series of 1-(3-p-fluorobenzoylpropyl)-4-(1-oxo-benzo- or thienocycloalkyl-2-ethyl)piperazines 8a - e containing both semirigid and linear butyrophenones pharmacophores. The affinities of these compounds for dopamine (D2) and 5-hydroxytryptamine (5-HT2A) receptors were evaluated in vitro in receptor-binding assays and in functional experiments. The ratios of pKi's for 5-HT2A/D2 receptors may be useful for rapid screening of new compounds and assessing potential induction of extrapyramidal symptoms; ratio values >1.12 (Meltzer's ratio) are predictive of an atypical antipsychotic profile. The new molecules had a ratio in the range of 0.96-1.11 while haloperidol showed a ratio of 0.93. The 2-piperazinoethyl thiotetralone derivative 8d (QF 0506B) with a ratio of 1.11 was the most active compound.