Percutaneous transluminal angioplasty: the treatment of choice for renovascular hypertension due to fibromuscular dysplasia

Twenty-three renal artery stenoses in 21 hypertensive patients, caused by fibromuscular dysplasia, were treated with percutaneous transluminal angioplasty (PTA). Follow-up over a period of 1 to 30 months, including angiography, renal vein renin assay, and radionuclide flow studies, was performed in 8 patients, each with one stenosis. Dilatation was initially successful in all cases and was successfully repeated in 1 case. The mean systolic pressure decreased by 61.81 mm Hg and the mean diastolic pressure by 36.28 mm Hg in response to treatment. Thirteen patients were cured, 8 were felt to have better control of blood pressure on medication, and there was no failures. This study demonstrates that PTA is a clinically effective method of treating renovascular hypertension due to fibromuscular dysplasia.     

2,4-二氨基-5-取代苄基嘧啶类化合物的合成及其抑酶活性

本文设计并合成了18个在苄基上带有不同体积取代基的2,4-二氨基-5-取代苄基嘧啶类化合物。测定了这些化合物对乳酪菌二氢叶酸还原酶及对鸡肝二氢叶酸还原酶的表观50%抑制作用。其中2,4-二氨基-5-(3′-羟基-4′-甲氧基)苄基、2,4-二氨基-5-(3′-甲氧基-4′-甲氧乙氧基)苄基嘧啶对上述二氢叶酸还原酶(DHFR)的选择性较好。     

Structure-activity relationship studies of CNS agents. Part 29. N-Methylpiperazino-substituted derivatives of quinazoline, phthalazine and quinoline as novel α1, 5-HT1A and 5-HT2A receptor ligands

New N-methylpiperazino-substituted quinazolines 8 and 9, phthalazine 13, and quinoline 19 have been synthesized. The receptor binding profiles (α₁, 5-HT_1A, 5-HT_2A) of these compounds and their analogs (7–22) have been determined. It has been demonstrated that orientation of a local dipole moment of the heteroaromatic ring system affects both the α₁ and 5-HT_2A affinity of the investigated class of ligands. Distortion of the coplanar unfused heteroaromatic ring system results in a decreased 5-HT_2A affinity. 4-(4-Methylpiperazino)-2-(2-thienyl)quinoline 18 is the most active and selective α₁ ligand (K_i = 4.9 nM) with a much lower affinity for 5-HT_1A (K_i = 3420 nM) and 5-HT_2A (K_i = 211 nM) receptors.