Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: DrugBank:APRD00627 (MAP)
 15,705 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

A series of S-alkanoyl and benzoyl derivatives of 3-mercaptopicolinic acid (3-MPA) was prepared and studied for hypoglycemic activity. Three alkanoyl derivatives (propionyl, pivaloyl, and 1-adamantanecarbonyl, 19-21) were prepared with increasing bulk around the thio ester bond. The benzoyl derivatives contained aromatic substituents chosen from a sigma-pi cluster chart so that the esters prepared had a wide range of electronic and solubility properties. In general, compounds with substituents which increased lipid solubility [p-chlorobenzoyl (4), p-trifluoromethylbenzoyl (6), and pivaloyl (20)] had the greatest potency at a dose of 300 mg/kg. Hydrolysis rates, measured at pH 6 and 8, indicated that in vivo breakdown to 3-MPA probably did not account for the observed hypoglycemic activity of the esters. 4, 6, and 20 were less potent than 3-MPA in comparative dose range studies.
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PMID:Synthesis and hypoglycemic activity of S-acyl derivatives of 3-mercaptopicolinic acid. 1 14

This study examines the effects of MPA (medroxyprogesterone acetate) on some of the hepatic enzymes of carbohydrate and lipid metabolism in the rat, and compares these with the effects of cortisol and saline. Levels of reduced nicotinamide adenine dinucleotide phosphate (NADPH) were also measured. Intact mature female Wistar rats with average initial weight of 200 gms were injected with MPA (mO mg/kg IM) once a week for 4 weeks and were sacrificed 3 to 5 days after the last injection. Hydrocortisone (Solu-Cortef [R]) 40 mg/kg IM were given to cortisol-treated animals twice daily for 7 days. The animals were sacrificed 2-4 hours after the last dose was given. Normal saline (0.2 mg. IM) was injected in control animals twice a day. The method of Jellinek, Amako, and Willman was used to analyze NADPH. Liver samples were assayed for various enzymatic activities such as phophofructokinase (PFK); pyruvate kinase (PK), glycerol-3-phosphate dehydrogenase (G3PD), "malic" enzyme (ME), and glucose-6-phosphate dehydrogenase (G6PD). The methods of Colowick and Kaplan were used in enzymatic analyses. Lipogenic stimulation by MPA is indicated by increased levels of G3PD and ME, both of which are implicated in lipogenesis, as well as by NADPH. PFK, PK, and G6PD were all unaffected by the MPA regimen, suggesting that elevation of ME and NADPH activities may reflect increased amino acid conservation. The enzymatic pattern of MPA treatment shows lipogenesis and protein conservation, while that of cortisol regimen shows significantly lower levels of ME, G3PD, and PRK.
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PMID:Some effects of medroxyprogesterone acetate on intermediary metabolism in rat liver. 2 59

R-2323 and MPA have proved to be potent inhibitors of ovarian function in the female and of spermatogenesis and accessory gland function in the male. This study was to establish methods of determining their concentrations in human plasma in order to obtain more information about their action. Subjects were 10 31-72 year old male patients, who were treated with R-2323 with different dose schedules and 3 men suffering from benign prostatic hypertrophy who were treated with MPA. Plasma levels of testosterone (T), luteinizing hormone (LH), and follicle stimulating hormone (FSH), were monitored before, during, and after treatment. R-2323 levels were determined according to the methods of Vunikke et al. Plasma T measurements were done according to the methods of Bartke, LH and FSH levels were measured by means of the modified solid-phase radioimmunoassay method of Crosignani, and MPA determinations were done by the method of Edgvist and Johansson. Individual R-2323 values varied from 16 to 36 ng/ml. After injections of 250-1000 mg of MPA there was less difference in plasma MPA than expected. This suggested that MPA is stored, perhaps in fat tissues. With MPA, a decrease in plasma T levels took place, indicating inhibition of Leydig cell function, within 2-6 days after starting treatment. Treatment with 100 mg of R-2323 weekly for 6 weeks caused a drastic decrease in plasma T levels. Similar changes were found for LH and FSH. The only change in patients' libido was a decrease in the first 2 or 3 weeks of therapy. 6 weeks after treatment was stopped hormone levels had returned to normal in 80% of subjects.
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PMID:Radioimmunoassays of ethinyl-norgestrienone (R-2323) and medroxyprogesterone acetate (MPA) and their clinical applicability. 6 51

17 alpha-Acetoxy-6 alpha-methylprogesterone (medroxy-progesterone acetate, MPA) in doses of 50 mg followed 4 weeks later by an additional 100 mg was i.m. injected in 5 adult normal female monkeys. Serum levels of MPA, progesterone, estradiol-17-beta and LH were determined every other day for a period of 8 weeks then weekly for 8 months. Peak values of serum MPA were detected 2 weeks postinjection followed by a gradual decline to undetectable levels after variable periods ranging from 125 to 225 days. The drug, in the doses used, caused inhibition of LH and estradiol surges and suppression of progesterone for more than 6 months. The return of menstrual cyclicity preceded the return of ovulatory cyclicity. Menstrual cyclicity occurred while the drug was still detectable in the blood. The probable site of action of the drug is discussed.
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PMID:Medroxyprogesterone acetate: peripheral serum levels and its effects on pituitary and ovarian functions in the rhesus monkey. 10 56

Evidence for the role of androgens in the male aggressive and sexual behavior is reviewed. Medroxyprogesterone acetate (MPA; Provera, Upjohn) has a marked antiandrogen property; it is effective in lowering the testosterone level and controlling certain otherwise intractable sex deviations. The finding in 6 patients treated for sex deviation are summarized. The effects of MPA in the treatment of 11 temporal lobe epileptics and 5 other patients with severe angry-aggressive behavior disorder are reported. Most temporal lobe epileptics responded well to MPA. Weight gain and earlier sleep were consistent side effects. The values of plasma testosterone, serum luteinizing hormone, and urinary 17-ketosteroids were decreased by the treatment. Four patients were XYY individuals with lack of control over their sexual-aggressive or angry-aggressive impulses.
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PMID:Hormone and hormonal agents in the treatment of aggression. 12 69

The sublethal dose of calcium hypochlorite (CH) of 0.2--0.3 mg/ml active chlorine did not cause, after 5 min, morphological changes in the spores of Bacillus anthracoides which could be detected by phase contrast microscopy, or a decrease in the content of dipicolinic acid (DPA) in the spores. Further cultivation of the spores treated with the sublethal dose of CH om MPA resulted in a delay of changes which were typical of normal germination process (swelling, loss of light refraction, decrease in DPA content). The action of the lethal dose of CH (0.2--0.3 mg/ml active chlorine during 1.5 hr or 5.6 mg/ml active chlorine during 1 hr) causes a decrease in light refraction, changes in the dimensions of spores, and a decrease in the content of DPA in the spores by a factor of 4--5. A sharp decrease in the content of DPA in the spores may characterize not only their germination but also their death caused by lethal doses of the chlorine containing disinfectant.
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PMID:[Effect of calcium hypochlorite on Bacillus anthracoides spores]. 18 5

A clinical study with 361 female rats was conducted to elucidate the mechanism whereby MPA (medroxyprogesterone acetate) lowers 5-HT/5-HIAA ratio in the brain area and the possible role of serotoniergic mechanisms. In addition, the participation of MAO (monoamino oxidase) system and the effects of some steroids were studied in order to establish a relationship between chemical structure and activity. The effects of the following steroids were studied: MPA (medroxyprogesterone acetate), melengestrol acetate, chlormadinone, pregnenolone, -methyl pregnenolone, DOCA, acetoxi-progesterone, and ACTH (synacthen). Effects of these substances on LTP (liver tryptophan pyrrolase) activity, total and free plasma and brain stem Trp (tryptophan), and the 5HT and 5HTAA content in brain stem are tabulated. Of all the substances, only MPA and melengestrol acetate significantly raised LTP activity and both also lowered 5-HT content of brain stem. The high levels of ACTH in the blood of the adrenalectomized rats, as in those under fasting conditions, antagonized MPA effects. To further test this seeming result, ACTH and ACTH-MPA were injected into another group of animals. The ACTH not only increased plasma corticosterone but also antagonized the effect of MPA on the 5-HT content of brain stem. The study did not identify a relationship between chemical structure of the steroids studied and effects observed.
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PMID:Role of ACTH on the effect of medroxyprogesterone in brain stem serotonin. 21 92

Mechanical firmness of 4 UV hardened composites was estimated by the bending test according to DIN 13922. Bending strength and breaking point lie between 70 and 120 MPA and 0.5 and 0.25 mm compared with 110 MPA and 0.13 mm for Adaptic. The results show that the combination of filling substance and UV irradiation is well balanced.
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PMID:[Bending strength of UV hardening composites]. 27 75

Progesterone administration increase VE in man, but its effects on ventilatory response to hypercapnia and hypoxia have not been well documented. Accordingly, VE, HVR, and HCVR were measured during placebo and MPA administration in 11 normal men. The effect of MPA (20 mg orally q 8 hr for 32 hr) on T degrees, metabolic rate (VO2 and VCO2) was also determined. With MPA, T degrees, rose 0.4 degrees C +/- 0.0008 (S.E.M.) p less than 0.0001), VE increased 0.46 +/- 0.16 L/min (p less than 0.01), and VO2 and VCO2 did not change significantly. HCVR (measured under hyperoxic conditions during rebreathing) increased significantly (P less than 0.01) from 2.9 +/- 0.33 L/min/mm Hg (placebo) to 4.0 +/- 0.29 (MPA). HVR was measured as the shape parameter A, so that when A increased, HVR was augmented. During MPA, HVR increased from A = 132 +/- 19.1 to 179 +/- 20.5 (P less than 0.02). We conclude that 60 mg of MPA daily in normal men increases VE and chemosensitivity as measured by the ventilatory response to hypercapnia and hypoxia.
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PMID:Effects of progesterone on chemosensitivity in normal men. 35 85

Temporal changes in the incidence of soil bacteria were estimated using different methods such as luminescent microscopy, direct count according to Vinogradsky, growth on MPA. The method of Vinogradsky gave less stable results as compared to luminescent microscopy. The method of calculating microorganisms was found to influence the results obtained while studying the temporal dynamics of bacterial incidence in sod-podzolic soil.
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PMID:[Dynamics of the number of soil bacteria calculated by different methods]. 38 64


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