A series of novel compounds having a benzothiazoline skeleton was studied for their structure-activity relationship (SAR) with respect to Ca2+ antagonistic activity. As test compounds, analogues of 3-acyl-2-arylbenzothiazolines (3) were synthesized. Benzothiazoline derivatives (3) exerted higher Ca2+ antagonistic activity than the corresponding thiazolidine derivatives (2). Effects of substituents R1-R4, the substitution position of the aminoalkoxy group and R2, and the length of the methylene chain on biological activities were examined. Compound 4 [3-acetyl-2-[5-methoxy-2-[4-[N-methyl-N-(3,4,5-trimethoxyphenethyl ) amino]butoxy]phenyl]benzothiazoline hydrochloride] showed a potent Ca2+ antagonistic activity in vitro and dual inhibition on the fast Na+ inward channel and the slow Ca2+ inward channel in Langendorff perfused rabbit hearts. Compound 4 also showed a long-acting hypotensive effect in spontaneously hypertensive rats and prevented acute pulmonary thrombotic death in mice.
The inclusive production rate of neutral pions in the rapidity range greater than y = 8.9 has been measured by the Large Hadron Collider forward (LHCf) experiment during √ s = 7 TeV protonproton collision operation in early 2010. This paper presents the transverse momentum spectra of the neutral pions. The spectra from two independent LHCf detectors are consistent with each other and serve as a cross-check of the data. The transverse momentum spectra are also compared with the predictions of several hadronic interaction models that are often used for high-energy particle physics and for modeling ultra-high-energy cosmic-ray showers.
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