Category: 337972-47-1

Lanig, Harald published the artcileComparative molecular field analysis of dopamine D4 receptor antagonists including 3-[4-(4-Chlorophenyl)piperazin-1-ylmethyl]pyrazolo[1,5-a]pyridine (FAUC 113), 3-[4-(4-Chlorophenyl)piperazin-1-ylmethyl]-1H-pyrrolo[2,3-b]pyridine (L-745,870), and clozapine, Product Details of C18H19ClN4, the publication is Journal of Medicinal Chemistry (2001), 44(8), 1151-1157, database is CAplus and MEDLINE.

A CoMFA study was undertaken to elucidate the correlation of biol. activity and structural parameters of 25 dopamine D4 antagonists. A special point of interest is that we have included the atypical D4 antagonist clozapine as a structural template for all other compounds After comparing potential protonation sites at semiempirical (AM1) and ab initio (6-31G(d)) levels of theory, possible conformations of the lead compound 3-[4-(4-chlorophenyl)piperazin-1-ylmethyl]pyrazolo[1,5-a]pyridine (FAUC 113) were investigated by systematic semiempirical conformational anal. The final conformation of FAUC 113, which was used as a template for the other compounds in the dataset, was chosen by clustering and rigid body alignment of all conformations to clozapine. The CoMFA applied on the final alignment resulted in a q²_cv of 0.739. To elucidate the influence of the absolute orientation of the mols. within the grid space, the entire dataset was systematically rotated (1296 steps) within the lattice. The Gaussian-shaped distribution of the q²_cv values spanned the range of 0.699-0.794 and therefore supports the significance of the anal.

Journal of Medicinal Chemistry published new progress about 337972-47-1. 337972-47-1 belongs to piperazines, auxiliary class Inhibitor, name is 2-((4-(4-Chlorophenyl)piperazin-1-yl)methyl)pyrazolo[1,5-a]pyridine, and the molecular formula is C18H19ClN4, Product Details of C18H19ClN4.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Itsumi, Momoe published the artcileProfile of androgen receptor activators identified using high-throughput screen, Recommanded Product: 2-((4-(4-Chlorophenyl)piperazin-1-yl)methyl)pyrazolo[1,5-a]pyridine, the publication is Andrologia (2021), 53(1), e13856, database is CAplus and MEDLINE.

In this study using distinct system, effectors on dopamine signalling were identified as candidates that prominently increase AR activity. Then, this study suggested novel function on AR signalling in several compounds, which may be useful or harmful in organs where AR signalling play a role. In conclusion, various candidates for AR activation were identified using high-throughput screening.

Andrologia published new progress about 337972-47-1. 337972-47-1 belongs to piperazines, auxiliary class Inhibitor, name is 2-((4-(4-Chlorophenyl)piperazin-1-yl)methyl)pyrazolo[1,5-a]pyridine, and the molecular formula is C18H19ClN4, Recommanded Product: 2-((4-(4-Chlorophenyl)piperazin-1-yl)methyl)pyrazolo[1,5-a]pyridine.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Boeckler, Frank published the artcileFAUC 213, a highly selective dopamine D₄ receptor full antagonist, exhibits atypical antipsychotic properties in behavioural and neurochemical models of schizophrenia, SDS of cas: 337972-47-1, the publication is Psychopharmacology (Berlin, Germany) (2004), 175(1), 7-17, database is CAplus and MEDLINE.

2-[4-(4-Chlorophenyl)piperazin-1-ylmethyl]pyrazolo[1,5-a]pyridine (FAUC 213) is a highly selective antagonist at the dopamine D₄ receptor subtype. It was designed as a derivative of two partial antagonists and has been proven to be a complete antagonist in mitogenesis assay. In the present study, FAUC 213 was examined for antipsychotic properties in animal models of behavioral neurobiol. and neurochem. Different concentrations of FAUC 213 were screened for effects on spontaneous, as well as amphetamine-induced, locomotor activity and apomorphine-induced prepulse disruption. The liability of causing extrapyramidal side effects was investigated in models of catalepsy and by high-performance liquid chromatog. (HPLC) detection of dopamine turnover in several brain regions. The application schedule was validated, and the bioavailability of the compound determined, by a HPLC-pharmacokinetic study. A significant effect in both the reduction of amphetamine-induced locomotor hyperactivity and the restoration of apomorphine-disrupted prepulse inhibition was found at 30 mg/kg. This dose proved not to be high enough to induce catalepsy or to increase dopamine turnover in the dorsal striatum, nucleus accumbens and medial prefrontal cortex. The selective D₄ antagonist FAUC 213, therefore, is not believed to mediate the above-mentioned effects via D₂ receptor antagonism, but a partial involvement of 5-HT₂– and α₁-receptors cannot be ruled out at present. We have gathered evidence that FAUC 213 exhibits atypical antipsychotic characteristics.

Psychopharmacology (Berlin, Germany) published new progress about 337972-47-1. 337972-47-1 belongs to piperazines, auxiliary class Inhibitor, name is 2-((4-(4-Chlorophenyl)piperazin-1-yl)methyl)pyrazolo[1,5-a]pyridine, and the molecular formula is C18H19ClN4, SDS of cas: 337972-47-1.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics