Topic
Propylthiouracil
About: Propylthiouracil is a research topic. Over the lifetime, 2181 publications have been published within this topic receiving 46996 citations. The topic is also known as: Thyreostat® & 2,3-dihydro-6-propyl-2-thioxo-4(1H)-pyrimidinone.
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TL;DR: In vitro conversion of T4 to T3, T3 to 3,3′-diiodothyronine (T2), and rT3 to T2 by canine thyroid, liver, and kidney homogenate was examined, and TSH markedly stimulated thyroidal inner and outer ring iodothyronines-monodeiodinating activities.
Abstract: To investigate the effect of TSH administration on thyroidal iodothyronine-deiodinating activity, in vitro conversion of T4 to T3, T3 to 3,3′-diiodothyronine (T2), and rT3 to T2 by canine thyroid, liver, and kidney homogenate was examined, comparing tissues from TSH-treated dogs (3 IU bovine TSH daily for 3 days) with tissues from sex- and weight-matched saline-treated controls. The in vitro conversion activities were studied in the presence of 4 mM dithiothreitol at pH 6.5 for outer ring (T4 to T3 and rT3 to T2) and at pH 7.8 for inner ring (T3 to T2) deiodination. Iodothyronine-monodeiodinating activity in dog thyroid is heat labile (inactivated at 56 C × 5 min) and pH dependent, inhibited by propylthiouracil (0.2 mM) and ipodate (0.2 mM), unaffected by methimazole (up to 4 mM), ascorbate (up to 0.1 M), or KI (up to 4 mM), and is localized in the microsomal fraction. TSH markedly stimulated thyroidal inner and outer ring iodothyronine-monodeiodinating activities. Baseline rates of T4 to T3, T3 to T2, an...
42 citations
TL;DR: Treatment with dronedarone results in cardioprotection by selectively mimicking hypothyroidism, accompanied by a reduction in body weight because of the suppression of food intake.
Abstract: Hypothyroid heart displays a phenotype of cardioprotection against ischemia and this study investigated whether administration of dronedarone, an amiodarone-like compound that has been shown to preferentially antagonize thyroid hormone binding to thyroid hormone receptor alpha1 (TRalpha1), results in a similar effect. Dronedarone was given in Wistar rats (90 mg/kg, once daily (od) for 2 weeks) (DRON), while untreated animals served as controls (CONT). Hypothyroidism (HYPO) was induced by propylthiouracil administration. Isolated rat hearts were perfused in Langendorff mode and subjected to 20 minutes of zero-flow global ischemia (I) followed by 45 minutes of reperfusion (R). 3,5,3' Triiodothyronine remained unchanged while body weight and food intake were reduced. alpha-Myosin heavy chain (alpha-MHC) decreased in DRON while beta-myosin heavy chain (beta-MHC) and sarcoplasmic reticulum Ca2+ adenosine triphosphatase (ATPase) expression (SERCA) was similar to CONT. In HYPO, alpha-MHC and SERCA were decreased while beta-MHC was increased. Myocardial glycogen content was increased in both DRON and HYPO. In DRON, resting heart rate and contractility were reduced and ischemic contracture was significantly suppressed while postischemic left ventricular end-diastolic pressure and lactate dehydrogenase release (IU/L min) after I/R were significantly decreased. In conclusion, dronedarone treatment results in cardioprotection by selectively mimicking hypothyroidism. This is accompanied by a reduction in body weight because of the suppression of food intake. TRs might prove novel pharmacologic targets for the treatment of cardiovascular illnesses.
42 citations
TL;DR: It is concluded that p75NGFR and NGF are independently regulated by thyroid hormone during critical periods of cerebellar development and the effect of thyroid hormone deficiency on p75 NGFR content in Purkinje cells may involve complex mechanisms such as impaired efficiency of axonal transport.
41 citations
TL;DR: It appears that the effects of chemical thyroidectomy on mature and immature rat brain are different for the substance P system, suggesting that thyroxine plays an important role in the maturation of substance P-containing neurons.
41 citations
TL;DR: It was concluded that 0.1, 0.15, and 0.2% thiouracil (TU) are equally effective in producing hypothyroid changes up to age 3 weeks, but PTU has a greater depressive effect on body weight because of its probably disagreeable taste and consequent effect upon food intake.
41 citations