Results 111 to 120 of about 605 (157)

In-vivo metabolism of 4-substituted arylpiperazines to pharmacologically active 1-arylpiperazines.

Bollettino chimico farmaceutico, 1991
A common metabolic process of 4-substituted arylpiperazine pharmacological agents is cleavage of the side-chain to yield 1-arylpiperazines. These metabolites are a well-known class of centrally active compounds and their formation may therefore be a pharmacologically significant pathway, at least in certain species, for derivates that undergo extensive
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Arylpiperazine Derivatives Acting at 5-HT1A Receptors

Current Medicinal Chemistry, 2002
Serotonin (5-hydroxytryptamine, 5-HT) is one of the most attractive targets for medicinal chemists. Among 5-HTRs, the 5-HT(1A) subtype is the best studied and it is generally accepted that it is involved in psychiatric disorders such as anxiety and depression. Several structurally different compounds are known to bind 5-HT(1A)R sites.
M L, López-Rodríguez, D, Ayala, B, Benhamú, M J, Morcillo, A, Viso   +4 more
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Soluble polymer-supported synthesis of arylpiperazines

Tetrahedron Letters, 1998
Abstract A method for soluble, inexpensive polymer-supported synthesis of piperazine and piperidine libraries on the basis of nucleophilic aryl substitution (S n Ar) and N-acylation is reported. Asymmetric N, N′-disubstituted piperazine and piperidine derivatives, that are potential drug candidates, can be synthesized in quantitative yields and ...
Pi-Chi Pan, Chung-Ming Sun
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Spatial structure in the N-arylpiperazine series

Bulletin of the Academy of Sciences of the USSR Division of Chemical Science, 1987
In the compounds examined, the angle of rotation of the plane of the aromatic ring relative to the unshared electron pair of the nitrogen atom is close to orthogonal, but in the o-fluoro-compound it is smaller.
I. Yu. Strobykina, V. E. Kataev, A. N. Vereshchagin, I. V. Galyametdinova, V. D. Akamsin   +4 more
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Novel arylpiperazines as selective α1-adrenergic receptor antagonists

Bioorganic & Medicinal Chemistry Letters, 2000
A novel series of arylpiperazines has been synthesized and identified as antagonists of alpha1a adrenergic receptor (alpha1a-AR) implicated in benign prostatic hyperplasia. These compounds selectively bind to membrane bound alpha1a-AR with K(i)s as low as 0.66 nM.
X, Li, W V, Murray, L, Jolliffe, V, Pulito   +3 more
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Intraocular Pressure Lowering Effects of Novel Arylpiperazine Derivatives

Journal of Ocular Pharmacology and Therapeutics, 1998
Arylpiperazine derivatives were synthesized and investigated in this study. Two animal models, including an intraocular pressure (IOP) recovery method and an alpha-chymotrypsin-induced glaucoma model, were used to determine the ocular pharmacological effects of the arylpiperazine derivatives.
C H, Chiang, T J, Chang, D W, Lu, A R, Lee   +3 more
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Modeling of the D₂ Dopamine Receptor Arylpiperazine Binding Site for 1‐{2‐[5‐(1H‐Benzimidazole‐2‐thione)]ethyl}‐4‐arylpiperazines.

ChemInform, 2004
AbstractFor Abstract see ChemInform Abstract in Full Text.
Šukalović, Vladimir, Zlatović, Mario, Andrić, Deana, Roglić, Goran, Kostić Rajačić, Slađana, Šoškić, Vukić   +5 more
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The Interactions of the 5-HT3 Receptor with Arylpiperazine, Tropane, and Quinuclidine Ligands

Current Topics in Medicinal Chemistry, 2002
The serotonin 5-HT(3) receptor subtype is unique among the receptors for this neurotransmitter because it has been demonstrated to be a ligand-gated ion channel capable of mediating rapid intercellular communication. This review covers the authors work performed during more than a decade in the development of 5-HT(3) receptor ligands belonging to the ...
Cappelli, Andrea, Anzini, Maurizio, Vomero, Salvatore, Mennuni, L., Makovec, F., Hamon, M., De Benedetti, P. G., Menziani, M. C.   +7 more
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Arylpiperazine derivatives as serotoninergic ligands

2009
Serotonin is a neuromediator well known for its implication in mood regulation, anxiety, depression,insomnia as well as in normal human function such as sleep, sexual activity and appetite and recently it was demonstrated its involvement in the proliferation of human tumor cells.
FIORINO F, DE ANGELIS F, SEVERINO B, PERISSUTTI E, FRECENTESE F, ESPOSITO A, MASSARELLI, PAOLA, RENNER C, SANTAGADA V, CALIENDO G.   +9 more
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Antihypertensive activity of 1-dimethylphosphinylmethyl-4-arylpiperazines

Journal of Medicinal Chemistry, 1974
E J, Glamkowski, J, Strupczewski, E, Wolf, D L, Woodward   +3 more
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