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Severe inability of the LIVER to perform its normal metabolic functions, as evidenced by severe JAUNDICE and abnormal serum levels of AMMONIA; BILIRUBIN; ALKALINE PHOSPHATASE; ASPARTATE AMINOTRANSFERASE; LACTATE DEHYDROGENASES; and albumin/globulin ratio. (Blakiston's Gould Medical Dictionary, 4th ed)
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A ubiquitously expressed G-protein-coupled receptor kinase subtype that has specificity for the agonist-occupied form of BETA-ADRENERGIC RECEPTORS and a variety of other G-PROTEIN-COUPLED RECEPTORS. Although it is highly homologous to G-PROTEIN-COUPLED RECEPTOR KINASE 2, it is not considered to play an essential role in regulating myocardial contractile response.
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The endogenous peptides with opiate-like activity. The three major classes currently recognized are the ENKEPHALINS, the DYNORPHINS, and the ENDORPHINS. Each of these families derives from different precursors, proenkephalin, prodynorphin, and PRO-OPIOMELANOCORTIN, respectively. There are also at least three classes of OPIOID RECEPTORS, but the peptide families do not map to the receptors in a simple way.
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A group of polycyclic compounds closely related biochemically to TERPENES. They include cholesterol, numerous hormones, precursors of certain vitamins, bile acids, alcohols (STEROLS), and certain natural drugs and poisons. Steroids have a common nucleus, a fused, reduced 17-carbon atom ring system, cyclopentanoperhydrophenanthrene. Most steroids also have two methyl groups and an aliphatic side-chain attached to the nucleus. (From Hawley's Condensed Chemical Dictionary, 11th ed)
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Compounds that interact with ANDROGEN RECEPTORS in target tissues to bring about the effects similar to those of TESTOSTERONE. Depending on the target tissues, androgenic effects can be on SEX DIFFERENTIATION; male reproductive organs, SPERMATOGENESIS; secondary male SEX CHARACTERISTICS; LIBIDO; development of muscle mass, strength, and power.
Finasteride
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The pharmacokinetic modelling of GI198745 (dutasteride), a compound with parallel linear and nonlinear elimination. (1/97)
AIMS: To characterize the pharmacokinetics of the dual 5alpha-reductase inhibitor GI198745 (dutasteride) to allow for more accurate predictions of GI198745 concentrations after different dosing schedules. METHODS: In this randomized, single-blind, parallel group study, 32 healthy male volunteers received single oral doses of GI198745 ranging from 0.01 to 40 mg. Data were analysed by nonlinear mixed effects modelling using NONMEM where both linear and nonlinear pharmacokinetic models were examined. RESULTS: The time course of GI198745 serum concentrations indicated concentration dependent elimination, with the apparent half-life increasing with dose. Data were best described by a two-compartment model with first order absorption and parallel linear and nonlinear elimination pathways. Drug absorption was rapid, and was followed by a short distribution phase. A high volume of distribution (511 l) and a low linear clearance (0.58 l h(-1)) combined to give a half-life of up to 5 (1-7) weeks at high concentrations. As concentrations declined towards Km (0.96 ng ml(-1)), the proportion eliminated by the relatively rapid saturable elimination pathway, with a maximum clearance of 6.2 l h(-1), increased and the half-life reduced to about 3 days. The estimated inter individual variability for the linear clearance was high (CV = 70%). CONCLUSIONS: G1198745 pharmacokinetics are well described by a pharmacokinetic model with parallel linear and nonlinear elimination. Simulations using this model show that at daily doses of 0.1 mg the steady state drug concentrations, and the rate at which these are achieved, are mainly influenced by the nonlinear pathway, while at daily doses above 1 mg they are almost entirely influenced by the linear pathway. (+info)Evaluation and characterization of micronuclei induced by the antitumour agent ASE [3beta-hydroxy-13alpha-amino-13, 17-seco-5alpha-androstan-17-oic-13, 17-lactam-p-bis(2-chloroethyl)amino phenylacetate] in human lymphocyte cultures. (2/97)
3beta - Hydroxy - 13alpha - amino - 13, 17 - seco - 5alpha - androstan - 17 -oic-13,17-lactam-p-bis(2-chloroethyl)amino phenylacetate (ASE) is a homo-aza-steroidal ester of p-bis(2-chloroethyl) amino phenyl acetic acid and has been shown to display antineoplastic, mutagenic and genotoxic activity. In the present study an effort has been made to evaluate the ability of ASE to induce micronuclei (MN) in human lymphocytes treated in vitro using the cytokinesis-block assay. Lympocytes were treated with different concentrations of ASE (0.1, 0.25, 0.5, 1, 2.5, 5, 10 and 20 microg/ml) at two different cell culture times, 21 and 41 h after culture initiation. ASE treatment lasted until cell harvest, for 51 and 31 h, respectively. Two types of cultures were used, whole blood and isolated lymphocyte cultures. The content of induced MN was identified by FISH analysis, using an alpha-satellite DNA probe, in binucleate cells. Our results suggest that ASE is capable of increasing MN frequencies in human lymphocytes under both culture conditions. This increase is related to the concentration in a linear dose-dependent manner and is also dependent on the duration of treatment. FISH analysis has shown that the induced MN resulted mainly from breakage events. Additionally, a weak aneugenic effect was found at the higher concentrations in whole blood cultures as well as in isolated lymphocyte cultures. Cytotoxic effects of ASE were observed under both cell culture conditions with a linear dose-dependent relationship according to CBPI evaluation and were more pronounced in isolated lymphocyte cultures. (+info)Linear relationships between the ligand binding energy and the activation energy of time-dependent inhibition of steroid 5alpha-reductase by delta 1-4-azasteroids. (3/97)
The inhibition of steroid 5alpha-reductase (5AR) by Delta(1)-4-azasteroids is characterized by a two-step time-dependent kinetic mechanism where inhibitor combines with enzyme in a fast equilibrium, defined by the inhibition constant K(i), to form an initial reversible enzyme-inhibitor complex, which subsequently undergoes a time-dependent chemical rearrangement, defined by the rate constant k(3), leading to the formation of an apparently irreversible, tight-binding enzyme-inhibitor complex (Tian, G., Mook, R. A., Jr., Moss, M. L., and Frye, S. V. (1995) Biochemistry 34, 13453-13459). A detailed kinetic analysis of this process with a series of Delta(1)-4-azasteroids having different C-17 substituents was performed to understand the relationships between the rate of time-dependent inhibition and the affinity of the time-dependent inhibitors for the enzyme. A linear correlation was observed between ln(1/K(i)), which is proportional to the ligand binding energy for the formation of the enzyme-inhibitor complex, and ln(1/(k(3)/K(i))), which is proportional to the activation energy for the inhibition reaction under the second order reaction condition, which leads to the formation of the irreversible, tight-binding enzyme-inhibitor complex. The coefficient of the correlation was -0.88 +/- 0.07 for type 1 5AR and -1.0 +/- 0.2 for type 2 5AR. In comparison, there was no obvious correlation between ln(1/K(i)) and ln(1/k(3)), which is proportional to the activation energy of the second, time-dependent step of the inhibition reaction. These data are consistent with a model where ligand binding energies provided at C-17 of Delta(1)-4-azasteroids is fully expressed to lower the activation energy of k(3)/K(i) with little perturbation of the energy barrier of the second, time-dependent step. (+info)Mass spectral fragmentation reactions of a therapeutic 4-azasteroid and related compounds. (4/97)
Mass spectra were acquired for a therapeutic 4-azasteroid (dutasteride), and some related compounds, using various ionization conditions (EI, CI, APCI and ESI) in both positive and negative ion modes. The ionization and fragmentation behavior of the compound dutasteride, its precursors and several analogs is reported. Positive atmospheric pressure chemical ionization (APCI+) and positive electrospray ionization (ESI+) produced distinctive collision-induced dissociation (CID) spectra for the respective [MH]+ ions of dutasteride. The spectral differences are attributed to ion populations having either different structures or different internal energy distributions (as a consequence of the method of ionization). Irrespective of their origin, the protonated molecules undergo interesting fragmentation reactions when collisionally activated. The identity of the major fragmentation products was confirmed by accurate mass measurement. The negative APCI mass spectrum of dutasteride displays extensive dehydrohalogenation, apparently due to the thermal component of the APCI process. Some of the resulting radical anions display remarkable stability toward collisional decomposition. Details of the fragmentation behavior for the negative ion species and their relationship to the positive ion results are discussed. (+info)Proteomic changes during disturbance of cholesterol metabolism by azacoprostane treatment in Caenorhabditis elegans. (5/97)
Although nematodes like Caenorhabditis elegans are incapable of de novo cholesterol biosynthesis, they can utilize nonfunctional sterols by converting them into cholesterol and other sterols for cellular function. The results reported previously and presented here suggest that blocking of sterol conversion to cholesterol in C. elegans by 25-azacoprostane-HCl (azacoprostane) treatment causes a serious defect in germ cell development, growth, cuticle development, and motility behavior. To establish a biochemical basis for these physiological abnormalities, we performed proteomic analysis of mixed stage worms that had been treated with the drug. Our results from a differential display proteomic analysis revealed significant decreases in the levels of proteins involved in collagen and cytoskeleton organization such as protein disulfide isomerase (6.7-fold), beta-tubulin (5.41-fold), and NEX-1 protein (>30-fold). Also reduced were enzymes involved in energy production such as phosphoglycerate kinase (4.8-fold) and phosphoenolpyruvate carboxykinase (8.5-fold), a target for antifilarial drugs such as azacoprostane. In particular, reductions in the expression of lipoprotein families such as vitellogenin-2 (7.7-fold) and vitellogenin-6 (5.4-fold) were prominent in the drug-treated worms, indicating that sterol metabolism disturbance caused by azacoprostane treatment is tightly coupled with suppression of the lipid transfer-related proteins at the protein level. However, competitive quantitative reverse transcriptase polymerase chain reaction showed that the transcriptional levels of vit-2, vit-6, and their receptors (e.g. rme-2 and lrp-1) in drug-treated worms were 3- to 5-fold higher than those in the untreated group, suggesting a presence of a sterol regulatory element-binding protein (SREBP)-like pathway in these genes. In fact, multiple predicted sterol regulatory elements or related regulatory sequences responding to sterols were found to be located at the 5'-flanking regions in vit-2 and lrp-1 genes, and their transcriptional activities fluctuated highly in response to changes in sterol concentration. Thus, many physiological abnormalities caused by azacoprostane-mediated sterol metabolism disturbance appear to be exerted at least in part through SREBP pathway in C. elegans. (+info)Four-amino acid segment in steroid 5 alpha-reductase 1 confers sensitivity to finasteride, a competitive inhibitor. (6/97)
The 4-azasteroid 17 beta-(N-t-butyl)carbamoyl-4-aza-5 alpha-androst-1-en-3-one (finasteride) is 100-fold more potent as a competitive inhibitor of the rat NADPH:delta 4-3-oxosteroid-5-alpha- oxidoreductase (steroid 5 alpha-reductase) type 1 enzyme (Ki = 3-5 nM) than of the human type 1 enzyme (Ki greater than or equal to 300 nM). In this study, we exploit this differential sensitivity to map a major determinant of finasteride sensitivity in steroid 5 alpha-reductase. Chimeric steroid 5 alpha-reductase cDNAs composed of different combinations of rat and human exon sequences were created by genetic engineering, expressed in human embryonic kidney 293 cells, and assayed for their sensitivity to finasteride. Hybrid proteins containing sequences encoded by rat exon 1 were found to be as sensitive to finasteride as the parental enzyme. The exchange of progressively smaller protein segments encoded within exon 1 identified a tetrapeptide sequence (Val-Ser-Ile-Val) in the rat enzyme that conferred sensitivity to finasteride. The analogous sequence in the human enzyme (Ala-Val-Phe-Ala) conferred partial resistance to the drug. Finasteride was a competitive inhibitor of the native and all chimeric enzymes tested, suggesting that the tetrapeptide segments form a portion of the substrate-binding domain of steroid 5 alpha-reductase. (+info)Laboratory monitoring of androgenic activity in benign prostate hypertrophy treated with a 5 alpha-reductase inhibitor. (7/97)
Testosterone and androstenedione are metabolized by 5 alpha- and 5 beta-reductases to androsterone (A) and etiocholanolone (E), respectively. These are excreted in the urine as conjugates, and the A/E ratio in normal men is usually greater than or equal to 1.5 (as opposed to 1 in women) because of the high 5 alpha-reductase activity in the prostate. The A/E ratio can be determined simply by gas chromatography after acid hydrolysis of a urine sample, extraction of steroids, and formation of trimethylsilyl derivatives. A timed collection of urine is unnecessary because the ratio of A/E is used rather than absolute values. In men suffering from benign prostate hypertrophy who are treated with Finasteride (a 5 alpha-reductase inhibitor), the A/E ratio decreases to less than 0.5. The A/E ratio decrease can be detected long before there is clinical improvement. (+info)The effect of finasteride in men with benign prostatic hyperplasia. The Finasteride Study Group. (8/97)
BACKGROUND: Benign prostatic hyperplasia is a progressive, androgen-dependent disease resulting in enlargement of the prostate gland and urinary obstruction. Preventing the conversion of testosterone to its tissue-active form, dihydrotestosterone, by inhibiting the enzyme 5 alpha-reductase could decrease the action of androgens in their target tissues; in the prostate the result might be a decrease in prostatic hyperplasia and therefore in symptoms of urinary obstruction. METHODS: In a double-blind study, we evaluated the effect of two doses of finasteride (1 mg and 5 mg) and placebo, each given once daily for 12 months, in 895 men with prostatic hyperplasia. Urinary symptoms, urinary flow, prostatic volume, and serum concentrations of dihydrotestosterone and prostate-specific antigen were determined periodically during the treatment period. RESULTS: As compared with the men in the placebo group, the men treated with 5 mg of finasteride per day had a significant decrease in total urinary-symptom scores (P less than 0.001), an increase of 1.6 ml per second (22 percent, P less than 0.001) in the maximal urinary-flow rate, and a 19 percent decrease in prostatic volume (P less than 0.001). The men treated with 1 mg of finasteride per day did not have a significant decrease in total urinary-symptom scores, but had an increase of 1.4 ml per second (23 percent) in the maximal urinary-flow rate, and an 18 percent decrease in prostatic volume. The men given placebo had no changes in total urinary-symptom scores, an increase of 0.2 ml per second (8 percent) in the maximal urinary-flow rate, and a 3 percent decrease in prostatic volume. The frequency of adverse effects in the three groups was similar, except for a higher incidence of decreased libido, impotence, and ejaculatory disorders in the finasteride-treated groups. CONCLUSIONS: The treatment of benign prostatic hyperplasia with 5 mg of finasteride per day results in a significant decrease in symptoms of obstruction, an increase in urinary flow, and a decrease in prostatic volume, but at a slightly increased risk of sexual dysfunction. (+info)
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Aza-steroids. Part VII. 3-aza-A-homopregn-4a-ene and related compounds". Journal of the Chemical Society (Resumed): 3388. doi: ...
Discovery and development of 5α-reductase inhibitors
Azasteroids are a type of steroid derivatives which have nitrogen atoms replaced at various positions for one of the carbon ... Two 4-azasteroids, finasteride and dutasteride are marketed as 5-ARIs. Finasteride (Proscar or Propecia) was the first ... Two of them are 4-azasteroids and will be covered here. As mentioned above, the third one, epristeride is only marketed in ... The main problems for 4-azasteroids is the rapid conversion into inactive 4,5-dihydro form, which is done by the enzyme. ...
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"Neuromuscular and other blocking actions of a new series of mono and bisquaternary aza steroids". J Pharm Pharmacol. 26 (11): ... "The neuromuscular and autonomic blocking effects of azasteroids containing choline or acetylcholine fragments". J Pharm ...
Azasteroid
Two azasteroids, finasteride and dutasteride, are used clinically as 5α-reductase inhibitors. Some of the 6-azasteroids may ... "6-Azasteroids: Potent dual inhibitors of human type 1 and 2 steroid 5.alpha.-reductase". Journal of Medicinal Chemistry. 36 (26 ... "6-Azasteroids: Structure-Activity Relationships for Inhibition of Type 1 and 2 Human 5.alpha.-Reductase and Human Adrenal 3. ...
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... and related 4-azasteroids as selective inhibitors of human type 1 5 alpha-reductase". J. Med. Chem. 37 (23): 3871-4. doi: ...
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While the above figure gives examples of 4-aza steroids, 6-aza steroids have also been developed by GSK, although none of these ...
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... azasteroids MeSH D04.808.925.100.250 - finasteride The list continues at List of MeSH codes (D05).. ...
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Steroids; Azasteroids. In Wikidata. 5α-Reductase inhibitors (5-ARIs), also known as dihydrotestosterone (DHT) blockers, are a ...
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Three series of 6-azasteroids and 4-azasteroids were employed to define the substrate preferences of M. tb 3β-hydroxysteroid ... 6-Azasteroids with large, hydrophobic side chains at the C17 position are the most effective inhibitors. Substitutions at C1, ... Inhibition of the M. tuberculosis 3β-hydroxysteroid dehydrogenase by azasteroids Bioorg Med Chem Lett. 2011 Apr 15;21(8):2216-9 ...
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Process for the preparation of 4-azasteroids. The invention relates to a process for the preparation of 4-azasteroids of the ... PROCESS FOR THE PREPARATION OF 4-AZASTEROIDS. Abstract. The invention relates to a process for the preparation of 4-steroids ... 1. A process for the preparation of 4-azasteroids of the formula. (Formula Removed). wherein. R1and R2 are independently ... Compounds of formula I are key intermediates for the production of pharmaceutically active 4-azasteroids, e.g. 17-substituted-4 ...
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MARSHALL IG, HARVEY AL, SINGH H, BHARDWAJ TR, PAUL D. The neuromuscular and autonomic blocking effects of azasteroids ... The neuromuscular and autonomic blocking effects of azasteroids containing choline or acetylcholine fragments. / MARSHALL, I. G ... title = "The neuromuscular and autonomic blocking effects of azasteroids containing choline or acetylcholine fragments", ... T1 - The neuromuscular and autonomic blocking effects of azasteroids containing choline or acetylcholine fragments ...
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3) 10-azasteroids, for example, AS97004, are competitive 5α-RI with a similar mechanism of action to 6-azasteroids [9]. ... 3-azasteroids, 19-nor-10-azasteroids, and diazasteroids [9].. 8.2. Nonsteroidal Inhibitors [9, 30, 46]. Several pharmaceutical ... 2) 6-Azasteroids (e.g., GIlS7669X) have a heterocyclic B ring (nitrogen atom at position 6) and a Δ4,5 bond in the A ring and ... d)Pyridines lack B and C rings.(e)Benzo[c]quinolinones tricyclic compounds derived from 6-azasteroids (no D ring, aromatic ring ...
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Synthesis, Spectral Characterization, and In Vitro Cytotoxicity of N-2′-Hydroxyethyl-Substituted Azacholestanes Prepared from 6...
M. S. Ahmad, Shafiullah, and M. Mushfiq, "Azasteroids from 3α, 5α-Cyclocholestan-6-one and 3β-bromo-5α-cholestan-6-one," ... A. Guarna, E. G. Occhiato, F. Machetti, and D. Scarpi, "A concise route to 19-nor-10-azasteroids, a new class of steroid 5α- ... 20-22]. During the last decade, a number of azasteroids have been synthesized as 5α-reductase inhibitors [23-27]. Guarna and ... General Procedure of Synthesis of N-Substituted Azasteroids [46-56]. Steroidal ketone 1 (0.45 mmol) in CH2Cl2 (6 mL) was ...
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Azasteroids are a type of steroid derivatives which have nitrogen atoms replaced at various positions for one of the carbon ... Two 4-azasteroids, finasteride and dutasteride are marketed as 5-ARIs. Finasteride (Proscar or Propecia) was the first ... Two of them are 4-azasteroids and will be covered here. As mentioned above, the third one, epristeride is only marketed in ... The main problems for 4-azasteroids is the rapid conversion into inactive 4,5-dihydro form, which is done by the enzyme. ...
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urinary tract neoplasms benign drug therapy 2000:2010[pubdate] *count=100 - BioMedLib™ search engine
MeSH-major] Azasteroids / therapeutic use. Enzyme Inhibitors / therapeutic use. Prostatic Hyperplasia / drug therapy ... Azasteroids / therapeutic use. Dihydrotestosterone / blood. Dutasteride. Enzyme Inhibitors / therapeutic use. Finasteride / ... Chemical-registry-number] 0 / 5-alpha Reductase Inhibitors; 0 / Azasteroids; 0 / Enzyme Inhibitors; 0 / Sulfonamides; ...
Inhibitors4
- 6-Azasteroids with large, hydrophobic side chains at the C17 position are the most effective inhibitors. (nih.gov)
- During the last decade, a number of azasteroids have been synthesized as 5 α -reductase inhibitors [ 23 - 27 ]. (hindawi.com)
- Azasteroids as Inhibitors of Testosterone 5 Alpha-Redustase in Mammalian Skin," J. Steroid Biochem. (regrowth.com)
- Efficient construction of 6-azasteroids: dual inhibitors of steroidal 5 alpha-reductase. (brushnet.site)
Steroidal1
- Azasteroids have N- substitutions in steroidal rings. (medworm.com)
Steroids1
- The first 5-ARIs were designed by modifying the structure of natural substrates, including the substitution of one carbon atom of the rings of the steroids by a heteroatom such as nitrogen thereby forming azasteroids. (wikipedia.org)
Heterosteroids1
- The heterosteroids, particularly azasteroids are obtained by this protocol [ 11 - 14 ]. (hindawi.com)
Metabolism1
- Oxidation and isomerization of 3β-hydroxysterols to 4-en-3-ones is requisite for sterol metabolism and the reaction is catalyzed by 3β-hydroxysteroid dehydrogenase (Rv1106c). (nih.gov)
Inhibition1
- A detailed investigation on the inhibition activity of 5a-reductase by several 4-azasteroids and their preparation is disclosed in Rasmusson, Gary H. et al. (allindianpatents.com)
Atoms2
- Azasteroids are a type of steroid derivatives which have nitrogen atoms replaced at various positions for one of the carbon atoms in the steroid ring system. (wikipedia.org)
- For competitive inhibiting functions there are two functions considered crucial, 4-en-3-one function and a lipophilic 17β-side chain with one or more oxygen atoms. (wikipedia.org)
Main1
- The main problems for 4-azasteroids is the rapid conversion into inactive 4,5-dihydro form, which is done by the enzyme. (wikipedia.org)
Applications1
- Besides, the large number of synthetic applications, azasteroids also owes versatile biological activities. (hindawi.com)
Preparation1
- Several reports pertaining with the preparation of azasteroids have been mentioned in the literature [ 29 - 32 ]. (hindawi.com)