Effect of sulphydryl reagents on the release of ox growth hormone in vitro.
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Adenosine Triphosphate↗
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Results for “Lithium Compounds”
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Lithium orotate in the treatment of alcoholism and related conditions.
The subjects were 42 alcoholic patients (33 males and 9 females) who were treated with lithium orotate during an alcohol rehabilitation program in a private clinical setting for at least six months. They derive from a total number of 105 patients who received this treatment initially, while the remainder discontinued the treatment within six months. The data were collected from a private practice record and the follow-up varied between six months and 10 years. The 42 patients studied displayed a multitude of complaints in addition to chronic alcoholism. These included liver dysfunction, seizure disorders, headaches, hyperthyroidism, affective disorders. Meniere's syndrome, liver and lung cancers. Thirty-six of the 42 patients studied had been hospitalized at least once for the management of their alcoholism. Lithium orotate was given, 150 mg daily, with a diet low in simple carbohydrates and containing moderate amounts of protein and fat. In addition, calcium orotate (for hepatic involvement), magnesium orotate, bromelaine, and essential phospholipids (for cardiac problems), and supportive measures were instituted, if required. Lithium orotate proved useful as the main pharmacologic agent for the treatment of alcoholism. Ten of the patients had no relapse for over three and up to 10 years, 13 patients remained without relapse for 1 to 3 years, and the remaining 12 had relapses between 6 to 12 months. Lithium orotate therapy was safe and the adverse side effects noted were minor, i.e., eight patients developed muscle weakness, loss of appetite or mild apathy. For these patients, the symptoms subsided when the daily dose was given 4 to 5 times weekly.(ABSTRACT TRUNCATED AT 250 WORDS)
Alcoholism↗
[Lithium].
The mode of action of the cation lithium is not well known. It is at present used as a topical drug in dermatology. Lithium inhibits many enzymes: Na/K ATPase, adenylcyclase, enzymes of the prostaglandines E1 synthesis, inositol-1-phosphatase. It is active on neutrophils et T lymphocytes, explaining in part its anti-inflammatory activity. It has a dose-dependent action on levures. It has possibly a direct inhibitory activity on DNA synthesis of herpes viruses. Lithium has a good local safety. Percutaneous penetration is weak and plasma concentrations are very much lower than that observed after oral intake. Lithium has been studied in seborrhoeic dermatitis. Its efficacy was primarily observed in psychotic patients. An assay with oral lithium did not confirmed the first observations. Topical lithium was found more efficient. Topical lithium succinate associated with zinc sulfate and lithium gluconate had a greater efficacy than placebo. Comparison with topical ketoconazole showed a non inferiority of lithium gluconate. Oral lithium also showed a reduction of symptoms' duration of herpes simplex. Cutaneous side-effects of oral lithium are frequent and numerous. Some of them may be explained by a lithium pharmacological cell activity (such as psoriasis). Teratogenicity is observed in mice and rats. Drug interactions are not expected after topical application. Irritants side effects are mainly observed after topical application; they are moderate and transitory. Lithium gluconate treatment of seborrhoeic dermatitis is a bid application during at least 8 weeks. It may be used in renal insufficiency. It is not recommended in the first trimester of pregnancy.
Administration, Oral↗
Specific modification of methionine-192 of -chymotrypsin by an affinity label exploiting the orienting properties of the linear acetylenic group.
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Alcohols↗
Dynamic thermodynamic and dynamic kinetic resolution of 2-lithiopyrrolidines.
Dynamic resolution has been studied as a method for the asymmetric synthesis of 2-substituted pyrrolidines. Highly enantioselective electrophilic substitutions of racemic 2-lithiopyrrolidines in the presence of a chiral ligand have been achieved. The organolithium compounds were prepared by tin-lithium exchange from the corresponding tributylstannanes and n-butyllithium or by deprotonation of N-(tert-butyloxycarbonyl)pyrrolidine with sec-butyllithium. A range of N-substituents and chiral ligands were investigated for the dynamic resolution. Electrophilic quench of the resolved diastereomeric 2-lithiopyrrolidine-chiral ligand complexes provided the enantiomerically enriched 2-substituted pyrrolidines. With N-alkyl derivatives, the resolution occurs conveniently at (or just below) room temperature and either enantiomer of the product can be formed by appropriate choice of the chiral ligand. The asymmetric induction occurs as a result of a thermodynamic preference for one of the diastereomeric complexes. The minor complex was found to have a faster rate of reaction with the electrophile. The use of N-allylic derivatives provides a means to prepare the N-unsubstituted pyrrolidine products. Best results were obtained with the N-2,3-dimethylbut-2-enyl derivative, and this N-substituent could be cleaved using 1-chloroethyl chloroformate. With N-Boc-2-lithiopyrrolidine, the enantioselectivity arises by a kinetic resolution and high levels of asymmetric induction in the presence of excess n-butyllithium can be obtained. Dynamic kinetic resolution of the N-Boc derivative is limited in the scope of electrophile that can be used.
Journal Article↗
Mixed La-Li heterobimetallic complexes for tertiary nitroaldol resolution.
A kinetic resolution of tertiary nitroaldols derived from simple ketones is described. Mixed BINOL/biphenol La-Li heterobimetallic complexes gave the best selectivity in retro-nitroaldol reactions of racemic tertiary nitroaldols. By using a mixture of La-Li3-(1a)3 complex (LLB 2a) and La-Li3-(1b)3 (LLB* 2b) complex in a ratio of 2/1, chiral tertiary nitroaldols were obtained in 80-97% ee and 30-47% recovery yield.
Alcohols↗
Synthesis and muscarinic activities of 1,2,4-thiadiazoles.
A series of novel 1,2,4-thiadiazoles bearing a mono- or bicyclic amine at C5 were prepared. Quinuclidine and 1-azabicyclo[2.2.1]heptane derivatives were synthesized by reaction of the lithium enolate of the 3-methoxycarbonyl compounds followed by ester hydrolysis and decarboxylation. The receptor-binding affinity and efficacy of these compounds as muscarinic ligands was assessed by radioligand binding assays using [3H]-N-methylscopolamine and [3H]oxotremorine-M. Optimal agonist affinity was observed for 3'-methyl compounds. Smaller substituents (H) retained efficacy with reduced affinity while larger groups led to substantially lower efficacy. The observed binding affinity was influenced both by the conformational energy of rotation around the C3-C5' bond and the steric requirement of the mono- or bicyclic amine.
Animals↗
Synthesis and pharmacological activity of 2,3,4,5,-tetrahydro-1,5-methano-1H-3-benzazepines.
2,3,4,5-Tetrahydro-1,5-methano-1H-3benzazepine (4) has been synthesized from 2,3-dioxobenzonorbornene. Oxidative cleavage of the diketone to cis-1,3-indandicarboxylic acid, followed by closure to the corresponding amhydride, conversion to the imide, and lithium aluminum hydride reduction, gave 4. Compound 4 and its N-derivatives show no analgesic activity in the mouse hot-plate assay and little antagonist activity in a tail-flick assay.
Analgesics↗
Simple entry to 3'-substituted analogues of anti-HIV agent stavudine based on an anionic O --> C stannyl migration.
Reaction of 5'-O-protected derivatives of the anti-HIV agent stavudine (d4T) with LTMP was investigated with the aim to lithiate the vinylic hydrogens (H-3' and H-2'). When the lithiation of the 5'-O-tert-butyldiphenylsilyl derivative 5 was carried out in the presence of HMPA, an anionic silyl migration took place to give the 3'-C-silylated product 4a. The stannyl version of this reaction was found to be also possible, which has disclosed a highly simple entry to the d4T analogues variously substituted at the 3'-position by manipulating the 3'-C-stannyl d4T as a common intermediate.
Anions↗
A novel dilithiation approach to 3,4-dihydro-2H-1,3-benzothiazines, 3,4-Dihydro-2H-1,3-benzoxazines, and 2,3,4,5-tetrahydro-1,3-benzothiazepines.
3,4-Dihydro-2H-1,3-benzothiazines 4, 3,4-dihydro-2H-1,3-benzoxazines 9, and 2,3,4,5-tetrahydro-1,3-benzothiazepines 6 were synthesized by directed ortho-lithiation of thiophenols and phenols and by side-chain lithiation of substituted thiophenols, respectively, in one-pot by reacting with N,N-bis[(benzotriazol-1-yl)methyl]amines 3 as 1,3-biselectrophile synthons.
Central Nervous System Agents↗
Variable coordination chemistry of the phospha(III)guanidinate anion; application as a metal-functionalised phosphine ligand.
Structural investigation of Li-complexes of the phospha(III)guanidinate anion [Ph2PC[NiPr]2]- revealed variable coordination to lithium; synthesis of the dimethyl aluminium compound, (Ph2PC[NiPr]2)AlMe2, which behaves as a metal-functionalised phosphine ligand towards platinum, is reported.
Journal Article↗
TMSCH2Li-induced regioselective lithiation of (S)-nicotine.
The first regioselective C-4 lithiation of (S)-nicotine has been realized using TMSCH2Li as basic reagent in toluene. The reaction proceeded under mild conditions with a small excess of electrophile. The 4-chloro derivative was subsequently metallated at C-5 with the same basic reagent in THF at -78 degrees C. This methodology opens a straightforward access to functional diversity in (S)-nicotine chemistry.
Indicators and Reagents↗
Effect of pH, ionic strength and univalent inorganic ions on the reconstitution of aspartate aminotransferase.
1. The effect of pH change on the reconstitution of aspartate aminotransferase (EC 2.6.1.1), i.e. the reactivation of the apoenzyme with coenzyme (pyridoxal phosphate and pyridoxamine phosphate), was studied in the pH range 4.2-8.9 by using three buffer systems at concentrations ranging from 0.025 to 0.1m. 2. Although the profile of the reconstitution rate-pH curve in the range pH5.2-6.8 (covered by sodium cacodylate-HCl buffer) reflects the influence of the H(+) concentration on the reconstitution process, the profile of the curve in the pH ranges 4.2-5.6 and 7.2-8.25 (covered respectively by sodium acetate-acetic acid and Tris-HCl buffers) appears to be influenced by the ionic strength of the buffer. 3. The reconstitution is also influenced by univalent inorganic ions such as halide ions and, to a lesser extent, alkali metal ions, which are known to alter the water structure.
Animals↗
Influences of cholecystokinin octapeptide on phosphoinositide turnover in neonatal-rat brain cells.
Cholecystokinin octapeptide (CCK-8) has been shown to be coupled to phosphoinositide turnover in pancreatic acini as well as in a kind of neuroblastoma cell and a human embryonic cell line. Little is known, however, about its link with phosphatidylinositol breakdown in the brain. The brains (minus cerebella) from 1-2-day-old neonatal rats were enzymically dissociated into single cells. The intact cells were prelabelled by incubation with myo-[3H]inositol for 3 h, and were then stimulated with agonists in the presence of 10 mM-LiCl. Carbachol at 1 mM induced an increase in InsP3 labelling in brain cells (peak at 30 min, and then a gradual decrease), and a static accumulation of InsP with time, whereas the labelling of InsP2 remained essentially unchanged. A very similar time-response curve was obtained for 10 nM-CCK-8 in stimulating phosphoinositide turnover. The dose-response curve for incubated brain cells revealed that the formation of InsP3 increased when the concentration of CCK-8 was increased from 0.1 to 10 nM. A further increase in CCK-8 concentration to 100-1000 nM resulted in a gradual decrease in InsP3 formation. InsP and InsP2 levels stayed relatively stable. The production of InsP3 stimulated by 10 nM-CCK-8 was dose-dependently suppressed by the CCK-A antagonist Devazepide in the concentration range 1-10 nM; the effect declined when the concentration was further increased to 100-1000 nM. In contrast, the CCK-B antagonist L365,260 showed a sustained suppression of InsP3 production at concentrations above 0.1 nM, i.e. in the range 1-1000 nM. The results provide evidence that CCK-8 stimulates the turnover of phosphoinositide and increases InsP3 labelling in dissociated neonatal-rat brain cells, in which both CCK-A and CCK-B receptors seem to be involved.
Animals↗
X-ray crystal analysis of the substrates of aconitase. VII. The structure of lithium ammonium hydrogen citrate monohydrate.
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Chemical Phenomena↗
Enhanced chemical strengthening of feldspathic dental porcelain.
Previous studies on ion exchange of dental ceramics have shown that the biaxial flexural strength can be improved by exchanging potassium for sodium ions at temperatures below the strain point. The rubidium ion is bigger than the potassium ion and can also be considered as a candidate for replacing smaller ions, i.e., sodium or potassium, although it has not been used for dental ceramics. The double-step method uses the exchange of a small ion for a large ion (Li for Na) above the strain point, and the further exchange of a large ion for a small ion (K for Li) below the strain point. The purpose of this study was to compare the effect of rubidium-for-potassium ion exchange with that of potassium-for-sodium exchange (Tuf-Coat, G-C International Corp., Japan) on the flexural strength of a feldspathic dental porcelain and to test the hypothesis that a double-step ion exchange can lead to greater strengthening than potassium ion exchange alone. Weight measurements were performed before and after treatment. Qualitative chemical analyses allowed the rubidium, potassium, and sodium concentration profiles to be determined along cross-sections of the specimens. The maximum biaxial stresses were calculated after specimens were fractured in water on a ball-on-ring fixture at 0.5 mm/min. Relative to the untreated control group, the flexural strength of the potassium-exchanged groups was significantly increased, except for those treated at 400 or 500 degrees C. All the groups treated with RbNO3 exhibited a significant increase in flexural strength, with a maximum for the group treated at 450 degrees C.(ABSTRACT TRUNCATED AT 250 WORDS)
Aluminum Silicates↗
[Lithium oxybutyrate and the rhythmic structure of the actively exploratory behavior and body temperature in rats under constant illumination conditions].
Under constant illumination (LL 24) conditions, lithium hydroxybutyrate (LHB, daily dose 10 mg/kg, 10 days) facilitated the formation of synchronized 24-h rhythms in the active-search (open-field) behavior and body temperature variation in rats, independently of the objective drug administration time. In the dark (DD 24), LHB increased the free-running rhythms and facilitated synchronization of the internal harmonics, especially upon the drug administration in the objective p.m. phase.
Animals↗
[Effect of lithium hydroxybutyrate on the circadian dynamics of the urinary excretion of Li(+), Na(+), K(+), and Ca(2+) in rats depending on the circadian phase of the drug administration].
In winter solstice, the urinary excretion of Li+ and Na+ in intact rats has a uniform circadian profile, while K+ and Ca2+ exhibit a 23-h and 24-h rhythm, respectively. The administration of lithium hydroxybutyrate (10 mg/kg, 6 days) at 8 a.m. forms the 24-h Li+ and Na+ excretion rhythm, while not significantly affecting the circadian profiles of K+ and Ca2+. The lithium loading at 8 p.m. made the circadian urinary excretion profiles of Ca2+ and Na+ uniform, while the excretion of Li+ and K+ acquired a 24-h rhythm. Irrespective of the circadian phase, the administration of lithium hydroxybutyrate decreased the average daily concentration of Na+ in the urine, while the average concentration of Ca2+ remains unchanged; the concentration of K+ decreases after lithium hydroxybutyrate injections in the morning. Upon the morning treatment, lithium cations are excreted faster than after the evening injections.
Animals↗