Category: 316-81-4

Novel GABA_A receptor blockers: an attempt to find more potent clozapine-like selective GABA antagonists was written by Squires, Richard F.;Saederup, Else. And the article was included in Voprosy Meditsinskoi Khimii in 1997.Quality Control of N,N-Dimethyl-10-(3-(4-methylpiperazin-1-yl)propyl)-10H-phenothiazine-2-sulfonamide This article mentions the following:

Because clozapine and a number of other antipsychotic, as well as antidepressant drugs selectively block subsets of GABA_A receptors, we have routinely screened 1100 compounds since 1983 for GABA antagonists effects on ³⁵S-TBPS binding, with a view to finding more potent clozapine-like selective GABA_A receptor blockers. About 225 GABA antagonists were identified. Among compounds not previously published, four groups of tricyclic compounds (phenothiazines, phenoxazines, acridines and phenazines) contained GABA_A receptor blockers, with acridines and oxidized phenothiazines in general being the most potent. Other active groups include cocaine derivatives, xanthines, indoles and phenethylamine derivatives A large group of miscellaneous structures includes all known GABA_A receptor blockers, as well as some antihistamines, antitussives, antimalarial/antiprotozoals, potential antidepressant, and a large non-therapeutic category consisting of diverse chem. structures. The amidino steroid R5135 remains the most potent GABA_A receptor blocker by far (EC₅₀ = 5.7 nM, ΔB_opt = 130%), and is non-aromatic Pitrazepin, the next-most potent GABA_A receptor blocker (EC₅₀ = 360 nM), also fully reverses the inhibitory effect of 1 μM GABA on ³⁵S-TBPS binding, but is 63-fold less potent than R5135. Appropriately positioned amidino groups, ring (aromatic) nitrogen, ether and keto groups can contribute to the potency of GABA_A receptor blockade. Clozapine-like selective GABA_A receptor blockers with EC₅₀ values in the low nanomolar range remain to be identified. Such compounds may have potent antipsychotic effects. In the experiment, the researchers used many compounds, for example, N,N-Dimethyl-10-(3-(4-methylpiperazin-1-yl)propyl)-10H-phenothiazine-2-sulfonamide (cas: 316-81-4Quality Control of N,N-Dimethyl-10-(3-(4-methylpiperazin-1-yl)propyl)-10H-phenothiazine-2-sulfonamide).

N,N-Dimethyl-10-(3-(4-methylpiperazin-1-yl)propyl)-10H-phenothiazine-2-sulfonamide (cas: 316-81-4) belongs to piperazine derivatives. Piperazine causes primary dermal irritation and skin burns at high concentrations. Piperazine also causes eye irritation in humans. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines. The connecting property of all these chemicals is the presence of a piperazine functional group.Quality Control of N,N-Dimethyl-10-(3-(4-methylpiperazin-1-yl)propyl)-10H-phenothiazine-2-sulfonamide

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

QSAR and 3D-QSAR of phenothiazine type multidrug resistance modulators in P388/ADR cells was written by Tsakovska, Ivanka M.. And the article was included in Bioorganic & Medicinal Chemistry in 2003.Recommanded Product: N,N-Dimethyl-10-(3-(4-methylpiperazin-1-yl)propyl)-10H-phenothiazine-2-sulfonamide This article mentions the following:

A series of 25 phenothiazines and structurally related compounds was investigated by QSAR (quant. structure activity relationship) and 3D-QSAR methods with respect to their MDR (multidrug resistance) reversing activity in P388/ADR- murine leukemia cell line resistant to ADR (adriamycin). The objective was to outline structural properties important for the investigated activity. Different measures for MDR reversal were used and compared. Two 3D-QSAR approaches were applied-CoMFA (comparative mol. field anal.) and CoMSIA (comparative mol. similarity indexes anal.). Both, neutral and protonated forms of the compounds were investigated. Mol. models with good predictive power were derived using a hydrophobic field alone and a combination of steric, hydrophobic, and hydrogen bond acceptor fields of the compounds In the combined models highest contribution of the hydrogen bond acceptor field was noticed. Thus, the dominant role of the hydrophobic and hydrogen bond acceptor fields for MDR reversing activity of the investigated compounds was demonstrated. The structural regions responsible for the differences in anti-MDR activity were analyzed in respect to their hydrophobic, hydrogen bond acceptor and steric nature. The results may direct design of new phenothiazines and related compounds as MDR modulators. In the experiment, the researchers used many compounds, for example, N,N-Dimethyl-10-(3-(4-methylpiperazin-1-yl)propyl)-10H-phenothiazine-2-sulfonamide (cas: 316-81-4Recommanded Product: N,N-Dimethyl-10-(3-(4-methylpiperazin-1-yl)propyl)-10H-phenothiazine-2-sulfonamide).

N,N-Dimethyl-10-(3-(4-methylpiperazin-1-yl)propyl)-10H-phenothiazine-2-sulfonamide (cas: 316-81-4) belongs to piperazine derivatives. The piperazine scaffold is often found in biologically active compounds in different therapeutic areas. These therapeutic areas include antifungals, antidepressants, antivirals, and serotonin receptor (5-HT) antagonists/agonists. Piperazine and its salts did not induce point mutations in a bacterial test. A series of mutagenicity studies in cells, both in vitro and in vivo, has been completed and showed no evidence of mutagenic effect.Recommanded Product: N,N-Dimethyl-10-(3-(4-methylpiperazin-1-yl)propyl)-10H-phenothiazine-2-sulfonamide

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics