High impact information on Lopac-S-003

• In vitro affinity for vascular 5HT2 and alpha receptors was determined for several compounds (spiperone, ketanserin, mianserin, trazodone, mepiprazole, benzoctamine, m-trifluoro-methylphenylpiperazine, m-chlorophenylpiperazine, and 1-(1-naphthyl)piperazine) known to interact with serotonin receptors [1].
• 5-HT1B receptor antagonist properties of novel arylpiperazide derivatives of 1-naphthylpiperazine [2].
• A structurally related compound, 1-naphthylpiperazine (1-NP), possesses a high affinity for 5-HT1 (Ki = 5 nM) and 5-HT2 (Ki = 18 nM) sites [3].
• Guinea pig tracheal contraction to 5-HT, 5-MT and DP-5-CT was inhibited by 1-(1-naphthyl)piperazine (1-NP, 30 nM) [4].
• However, contractions to serotonin in the fundus but not in the ileum were blocked by certain antagonists [metergoline and 1-(1-naphthyl)piperazine] demonstrating that the receptors involved in serotonin-induced contractions in the fundus are different from the ileum [5].

Anatomical context of Lopac-S-003

• The present in vitro studies using the 5-HT2 receptor antagonists ketanserin, LY53857 and 1-(1-naphthyl)piperazine show that serotonin-induced contractions in the rat uterus and guinea-pig trachea are also mediated by interaction with 5-HT2 receptors [5].
• 5-HT, alpha Me-5-HT and sumatriptan contracted both coronary artery and saphenous vein and the non-selective 5-HT receptor antagonist 1-naphthylpiperazine (100nM) blocked 5-HT- and sumatriptan-induced contraction in both tissues [6].

Associations of Lopac-S-003 with other chemical compounds

• Serotonin-antagonist effects of 1-(1-naphthyl)piperazine on operant behavior of squirrel monkeys [7].
• The agonists 1-(1-naphthyl)piperazine and buspirone (both serotonin receptor 1A agonists) were similarly effective in reducing K(Ca) [8].

Gene context of Lopac-S-003

• 4-Sulfonyl analogs of 1-(1-naphthyl)piperazine bind at human 5-HT6 receptors and represent a novel class of human 5-HT6 receptor ligands [9].

Analytical, diagnostic and therapeutic context of Lopac-S-003

• The enhancing effect of non-selective serotonergic autoreceptor antagonists, methiothepin (100 microM) or 1-(1-naphthyl)piperazine (NP) (10 microM), administered through the microdialysis probe, after 24 h washout, was similar in both control and chronically treated groups [10].

References