Results 81 to 90 of about 957 (180)
A chemometric study of the 5-HT1A receptor affinities presented by arylpiperazine compounds
Arylpiperazine compounds are promising 5-HT1A receptor ligands that can contribute for accelerating the onset of therapeutic effect of selective serotonin reuptake inhibitors. In the present work, the chemometric methods HCA, PCA, KNN, SIMCA and PLS were
WEBER, Karen C. +1 more
core +1 more source
This research was focused on in silico characterization and in vitro biological testing of the series of the compounds carrying a N-arylpiperazine moiety.
Ivan Malík +9 more
doaj +1 more source
Synthesis, computational and pharmacological evaluation of novel N-{4-[2-(4-aryl-piperazin-1-yl)ethyl]phenyl}-arylamides [PDF]
Serotonin, or 5-hydroxytryptamine (5-HT), is a biogenic amine most noted as a neurotransmitter, an activator of the utmost subtype family of G-protein- coupled receptors (GPCR). Drugs targeting 5-HT1A and other 5-HT receptors treat central nervous system
Andrić Deana B. +6 more
doaj +1 more source
In our endeavour towards the development of effective anticancer therapeutics, a novel series of isoxazole-piperazine hybrids were synthesized and evaluated for their cytotoxic activities against human liver (Huh7 and Mahlavu) and breast (MCF-7) cancer ...
Burcu Çalışkan +5 more
doaj +1 more source
New Imide 5-HT1A Receptor Ligands – Modification of Terminal Fragment Geometry
Two sets of new o-methoxyphenylpiperazine (MPP; series a) and 1,2,3,4-tetrahydroisoquinoline (THIQ; series b) derivatives, containing various imide moietiesderived from NAN190, were synthesized and evaluated in vitro for their ability to bind tothe ...
Ryszard Bugno +4 more
doaj +1 more source
A series of arylpiperazine- and 1,2,3,4-tetrahydroisoquinoline-based arylsulfonamides was synthesized and evaluated for their interactions with the constitutively active 5-HT7 receptor.
Schmidt, A.W. +10 more
core +1 more source
Background: Protease activated receptor-1 (PAR1) is a G-coupled receptor activated by α-thrombin and other proteases. Several reports have demonstrated the PAR1 involvement in tumorigenesis and tumor progression.
CORVINO, ANGELA +14 more
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Modeling interactions of α1a adrenergic receptor and different arylpiperazine ligands
Molecular modelling studies were undertaken in order to identify key interactions of selected ligands with α1A adrenergic receptor, responsible for their binding and presumably receptor activation. The previously made model of α1A adrenergic receptor was
Senćanski, Milan V. +9 more
core
Since it was known that 5HT properties (5HT(1A) agonism or 5HT(2A) antagonism) combined with D-2 antagonism may lead to atypical antipsychotic drugs, a series of 19 benzothiazolin-2-one and benzoxazin-3-one derivatives possessing the arylpiperazine ...
Rettori, MC +9 more
core +1 more source

