Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0011570 (depression)
 172,036 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Histoenzymological assay was used to investigate various structures of the ovaries of rats of two groups aged 3-4 and 12-14 months during estral cycle. The activity of 3 beta-, 17 beta- and 20 alpha-steroid dehydrogenases, glucose-6-phosphate dehydrogenase, NAD and NADP-diaphorases, esterase, acid and alkaline phosphatases was studied. It has been shown that transport alterations in the microcirculation including the hematofollicular barrier play, the leading part in age-dependent depression of reproductive and endocrine functions. Ageing rats demonstrated no linkage between endothelial, thecal and granular cells, which points to the injury of the histophysiological mechanisms of the follicular system integration.
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PMID:[Age-related characteristics of structural support for ovarian function]. 654 43

Changes in the peripheral blood leucocyte count, lymphocyte subpopulations, and in 'in vitro' responses of lymphocytes to phytohaemagglutinin and tuberculin after induced labour were investigated in 10 normal parturients and their newborns. Every other parturient was given segmental epidural analgesia at level T 10-12 for pain relief during the first stage of labour. The remaining mothers served as controls. The results of blood samples taken from the mothers before induction of labour and from the newborns immediately after delivery served as basal values against which the results of samples drawn on the 1st and on the 5th day following delivery were compared. A significant (p less than 0.05) increase from the basal values in the total leucocyte count after delivery was found only in those mothers not given epidural analgesia and in their newborns. Similarly, a significant (p less than 0.01) decrease in the T cell count characterized by both E rosette formation and acid alpha-naphthyl acetate esterase staining was found in the peripheral blood only in the mothers (but not the newborns) without epidural analgesia. The differences between the research groups were not, however, significant. The lymphocyte response to phytohaemagglutinin on the 1st and on the 5th day after delivery was also significantly (p less than 0.05) lower in the newborns of the mothers not given epidural analgesia than in those of the mothers given it. The present results show that the depression induced by the stress of parturition in some parameters of cell-mediated immunity of mothers and newborns can be at least partly prevented by using segmental epidural analgesia.
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PMID:Effect of segmental epidural analgesia on changes in peripheral blood leucocyte counts, lymphocyte subpopulations, and in vitro transformation in healthy parturients and their newborns. 660 64

Procaine esterase activity in plasma from patients with renal failure is decreased by 40%. Since cyanate is formed from urea and readily carbamylates certain blood proteins, a possible role for cyanate in the depression of plasma esterase activity in uraemic patients was considered. However, in vitro carbamylation of normal plasma in a range similar to that detected in uraemic patients did not influence procaine esterase activity. Kinetic analysis of the reaction showed that the maximal hydrolyzing capacity but not the Km in uraemic plasma was diminished (5.0 +/- 0.3 X 10(-5) moles hydrolyzed per litre of plasma per minute and a Km of 3.9 +/- 0.2 X 10(-5) mol/l in plasma from normal volunteers as compared to 3.1 +/- 0.1 X 10(-5) mol/l/min and 3.5 +/- 0.2 X 10(-5) ml/l in plasma from patients with renal failure). Therefore, not carbamylation but rather a decrease in enzyme synthesis is the likely explanation for the lower rate of procaine hydrolysis in uraemic plasma.
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PMID:Procaine hydrolysis defect in uraemia does not appear to be due to carbamylation of plasma esterases. 686 70

A significant reduction was noticed in the amount of vecuronium needed to maintain steady neuromuscular blockade at 20% twitch height (T1) in patients given nicardipine intraoperatively. Bolus injection of either nicardipine or diltiazem during constant infusion of vecuronium produced transient depression of T1 and the train-of-four ratio (TOFR). Reversal of neuromuscular blockade with a choline esterase inhibitor (neo-stigmine) was not retarded by previous administration of Ca-channel blockers but concurrent administration of anticholine-esterase agent and Ca-channel blockers caused a delay in recovery from motor blockade. Monitoring of neuromuscular junction activity is strongly recommended whenever a large cumulative dose of Ca-channel blockers is used.
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PMID:Potentiation of neuromuscular blockade by calcium channel blockers. 757 Jun 84

Remifentanil is a newly synthesized 4-anilido-piperidine with an ester side chain susceptible to esterase metabolism. We evaluated the safety, analgesic efficacy, and pharmacokinetics of remifentanil in 48 male volunteers. Volunteers were randomized to receive increasing doses of remifentanil, alfentanil, or placebo. Analgesic efficacy was evaluated by increasing tolerance to a spring-loaded rod measured at the tibia and sternum at multiple time points. Respiratory depression was measured by changes in arterial blood gas tensions and peripheral hemoglobin oxygen saturation. Hemodynamics were continuously monitored by means of an intra-arterial catheter. Both remifentanil and alfentanil produced a dose-dependent increase in analgesia and respiratory depression. Remifentanil was 20 to 30 times more potent (milligram to milligram) than alfentanil when assessed by either analgesic efficacy or respiratory measures. The pharmacokinetics of remifentanil were best described by a biexponential decay curve. Remifentanil had a small volume of distribution of 0.39 (SD, +/- 0.25) L/kg (alfentanil, 0.52 +/- 2 L/kg), with a rapid distribution phase of 0.94 (SD, +/- 0.57) min and an extremely short elimination half-life of 9.5 (SD, +/- 4) min compared with an elimination half-life of alfentanil of 58 (SD, +/- 7.6) min. The t1/2 ke0 (half-time for equilibration between plasma and the effect compartment) of remifentanil for analgesia was calculated as 1.3 min. Thus, remifentanil appears to have a pharmacologic profile similar to other potent mu agonists, but with exceptionally short-lasting pharmacokinetics, which is likely to make it a very useful opioid for clinical practice.
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PMID:Preliminary pharmacokinetics and pharmacodynamics of an ultra-short-acting opioid: remifentanil (GI87084B). 1203 62

Acetylcholine (ACh) exerts a crucial role in learning and memory. The striatum contains the highest concentration of this transmitter in the brain. This structure expresses two different forms of synaptic plasticity, long-term depression (LTD) and long-term potentiation (LTP), which might contribute to the storage of motor skills and some cognitive processes. We have investigated the role of M2-like muscarinic receptors in striatal LTP by utilizing intracellular recordings in vitro from a rat corticostriatal slice preparation. Methoctramine (250 nM), an antagonist of M2-like muscarinic receptors, enhanced striatal LTP induced in the absence of external magnesium (Mg2+) by high-frequency stimulation (HFS) of corticostriatal fibres. Methoctramine did not affect the amplitude of excitatory postsynaptic potentials (EPSPs) when bath applied either before or after the conditioning tetanus suggesting that a critical increase of ACh concentrations is produced only during HFS. Methoctramine per se failed to enhance the NMDA-mediated EPSPs recorded in the absence of external Mg2+ and in the presence of 10 microM CNQX. Methoctramine antagonized the presynaptic inhibitory action of neostigmine, an inhibitor of ACh-esterase, and oxotremorine, an agonist of M2-like muscarinic receptors. These data indicate that the activation of M2-like muscarinic receptors exerts a negative influence on striatal LTP, probably by reducing the release of glutamate from corticostriatal fibres and they suggest a complex modulatory effect of ACh in striatal synaptic plasticity.
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PMID:Blockade of M2-like muscarinic receptors enhances long-term potentiation at corticostriatal synapses. 975 72

While in membrane patches nicotinic channels from end-plates desensitize with time constants of 10-100 ms and recover with time constants of 100-200 ms, doubts remain as to whether such rapid reactions are also found in intact neuromuscular junctions. Therefore, the desensitization effected by a single end-plate current (EPC) on monoquantal EPCs (qEPCs) was studied. Using a published reaction scheme for the adult end-plate receptor, the desensitizing effects of an EPC on a following one were simulated. Twenty milliseconds after an EPC, a subsequent qEPC was reduced to 90% of control, and to 70-80% if acetylcholine esterase (AChE) was blocked. EPCs were elicited and recorded through a macropatch electrode. Series of four EPCs (control qEPC, conditioning EPC, test qEPC 1 and 2) were repeated several thousand times and the amplitudes and decay time constants of the qEPCs were evaluated. A highly significant average depression of the qEPC to 96.4% of control was found 20 ms after the conditioning EPC; if the AChE was blocked the depression after 40 ms was to 76% of control. Under both conditions, the time constant of recovery from desensitization was below 100 ms. The time constant of decay of the qEPC, taudecay, tended to be slightly shortened during depression in the presence of AChE. If AChE was blocked, taudecay was lengthened to 130-140% of control after a preceding EPC, and this lengthening outlasted the depression of the EPC amplitude by a second. These changes in taudecay are not predicted by the channel reaction scheme, and possible additional modulatory effects are discussed.
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PMID:Desensitization reduces amplitudes of quantal end-plate currents after a single preceding end-plate current in mouse muscle. 1008 70

The parasitic wasp Tranosema rostrale transmits a polydnavirus (PDV) to its host, Choristoneura fumiferana, during oviposition. Last-instar C. fumiferana larvae parasitized by T. rostrale early in the stadium fail to undergo metamorphosis, and injection of the wasp's calyx fluid (CxF; contains PDV) into healthy caterpillars induces a dose-dependent delay in initiation of metamorphosis (D. Doucet and M. Cusson, 1996, Entomol. Exp. Appl. 81, 21-30). In the present work, parasitization and injection of CxF (0.5 female equivalent) on the first day of the last stadium both prevented the rise in hemolymph 20-hydroxyecdysone (20HE) titer observed between day 4 and day 7 in control and saline-injected larvae. Similarly, juvenile hormone esterase (JHE) activity was depressed following parasitization or CxF injection, whereas control larvae displayed a peak on day 4. However, neither parasitism nor injection of CxF on day 1 prevented the JH-producing glands from turning off during the first half of the last stadium. Likewise, low but clearly detectable JH titers were observed in the first hours following the molt but very low titers, at or near the detection limit of our radioimmunoassay, were seen in both control and parasitized larvae on day 4. Prothoracic glands showed no apparent sign of degeneration 4 days after injection of CxF but had significantly smaller cells than saline-injected larvae 7 days postinjection. It is not clear whether this was a direct effect of T. rostrale PDV. Thus, disruption of spruce budworm metamorphosis by T. rostrale CxF involves depression of 20HE titers but is not associated with a measurable increase in the level of JH, as shown for some other host-parasitoid systems. In view of the latter observation, we put forward three hypotheses regarding the functional significance of the observed suppression of JHE activity in developmentally arrested C. fumiferana larvae.
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PMID:Functional significance of parasitism-induced suppression of juvenile hormone esterase activity in developmentally delayed Choristoneura fumiferana larvae. 1076 46

Dementia with Lewy bodies (DLB) is the second most frequent neuropathologically diagnosed degenerative dementing illness. The clinical characteristics are progressive dementia, parkinsonian syndrome, fluctuations of cognitive functions, alertness, and attention, visual hallucinations (usually detailed and well described), depression, REM sleep behavior disorder, adverse responses to standard neuroleptics doses, falls, syncopes, systematized delusions, and other modalities of hallucinations. Specificity of the clinical diagnostic criteria is high (95%), and sensitivity is considerably lower. Mean age at disease onset ranges between 60 and 68 years. The male gender prevails. Disease duration is 6 to 8 years. The differential diagnoses of DLB are dementia of the Alzheimer type, Parkinson's disease, subcortical arteriosclerotic encephalopathy, progressive supranuclear palsy, multiple system atrophy, and rarely Creutzfeldt-Jakob disease. The genetic background of the disease is unclear. Magnetic resonance imaging and single photon emission tomography can contribute to the diagnosis. Controlled pharmacological studies have so far not been published. The disease is treated with L-dopa, atypical neuroleptics, acetylcholine esterase inhibitors, antihypotensive agents, and peripheral anticholinergic and alpha receptor-blocking medications to improve neurogenic bladder dysfunction.
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PMID:[Dementia with Lewy bodies]. 1113 88

Dimebon, launched earlier in Russia as an antihistamine drug, was evaluated as a representative of a new generation of anti-Alzheimer's drugs that have two beneficial actions: (1) to alleviate symptoms, and (2) to prevent progression of the disease. The drug demonstrated cognition and memory-enhancing properties in the active avoidance test in rats treated with the neurotoxin AF64A, which selectively destroys cholinergic neurons. Dimebon protected neurons in the cerebellum cell culture against the neurotoxic action of beta-amyloid fragment (A beta 25-35, EC50 = 25 microM). In vitro, Dimebon displayed Ca(2+)-blocking properties (IC50 = 57 microM, on isolated rat ileum intestine) and pronounced anticholinesterase activity (IC50 = 7.9 microM and 42 microM for butyrylcholine esterase and acetylcholine esterase, respectively). It also exhibited strong anti-NMDA activity in the prevention of NMDA-induced seizures in mice (EC50 = 42 +/- 6 mg/kg i.p.). A beneficial effect of Dimebon in the therapy of Alzheimer's disease was demonstrated in a pilot clinical trial performed in the Moscow Center of Gerontology. Fourteen patients who participated in the trial were evaluated for their state of personality and for the severity of the disease. The evaluation included orientation (space, place, time, and patient personality), memory for the past and present, life in present, speech, irritability, and so forth. During and after the eight-week therapy with Dimebon, cognitive and self-service functions of patients improved significantly, and psychopathic symptoms, anxiety, depression, tearfulness, and headache were substantially diminished. The results of these studies suggest Dimebon as a new candidate for the therapy of Alzheimer's-like disorders.
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PMID:Antihistamine agent Dimebon as a novel neuroprotector and a cognition enhancer. 1146 98


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