[11C]phenytoin revisited: synthesis by [11C]CO carbonylation and first evaluation as a P-gp tracer in rats

UNLABELLED BACKGROUND At present, several positron emission tomography (PET) tracers are in use for imaging P-glycoprotein (P-gp) function in man. At baseline, substrate tracers such as R-[11C]verapamil display low brain concentrations with a distribution volume of around 1. [11C]phenytoin is supposed to be a weaker P-gp substrate, which may lead to higher brain concentrations at baseline. T...

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Synthesis and Biological Evaluation of New 1, 4-Dihydropyridines as Antihypertensives Agents in Rats

New analogues of nifedipine, as a known calcium channel blocker, were synthesized by replacing the orthonitrophenyl group on position 4 with 1-(4-Nitrobenzyl)-5-imidazolyl or 2-methylthio-1-(4-Nitrobenzyl)-5-imidazolyl substituent. Effects of the new synthesized compounds on blood pressure were studied at 15, 30 and 60 min after administration by indirect tail-cuff method and compared with nife...

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Synthesis and Biological Evaluation of New 1, 4-Dihydropyridines as Antihypertensives Agents in Rats

New analogues of nifedipine, as a known calcium channel blocker, were synthesized by replacing the orthonitrophenyl group on position 4 with 1-(4-Nitrobenzyl)-5-imidazolyl or 2-methylthio-1-(4-Nitrobenzyl)-5-imidazolyl substituent. Effects of the new synthesized compounds on blood pressure were studied at 15, 30 and 60 min after administration by indirect tail-cuff method and compared with nife...

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Synthesis and Preliminary Evaluation of a New 99mTc Labeled Substance P Analogue as a Potential Tumor Imaging Agent

Neurokinin 1 receptors (NK1R) are overexpressed on several types of important human cancer cells. Substance P (SP) is the most specific endogenous ligand known for NK1Rs. Accordingly, a new SP analogue was synthesized and evaluated for detection of NK1R positive tumors. [6-hydrazinopyridine-3-carboxylic acid (HYNIC)-Tyr8-Met(O)11-SP] was synthesized and radiolabeled with 99mTc using ethylenedia...

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Synthesis and Preliminary Evaluation of a New 99mTc Labeled Substance P Analogue as a Potential Tumor Imaging Agent

Neurokinin 1 receptors (NK1R) are overexpressed on several types of important human cancer cells. Substance P (SP) is the most specific endogenous ligand known for NK1Rs. Accordingly, a new SP analogue was synthesized and evaluated for detection of NK1R positive tumors. [6-hydrazinopyridine-3-carboxylic acid (HYNIC)-Tyr8-Met(O)11-SP] was synthesized and radiolabeled with 99mTc using ethylenedia...

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[11C]phenytoin revisited: synthesis by [11C]CO carbonylation and first evaluation as a P-gp tracer in rats

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