Reserpine

Major technical progress in the development of computer-based image analysis has made possible the entry of autoradiography and immunohistochemistry into a new era where quantification by densitometry has become easily accessible. Autoradiography could become quantitative and displayed adequate reproducibility with the help of emulsion-coated films and the use of scales of standards of known radioactivity exposed and analyzed in parallel to the tissue sections.Immunohistochemistry after revelation by a color-based enzymatic technique can also become quantitative, providing that standardization of the crucial steps of the procedure and calibration through a parallel treatment ofa scale of antigen standards can be ensured. Such an approach is described here in the rat with reference to tyrosine hydroxylase (TH), the main synthesizing enzyme for catecholamines, and with dopamine (DA) itself, a catecholaminergic neurotransmitter. The different parts of the procedure, which can influence the results, such as the fixation of the animals by perfusion and the evaluation of the fluctuations via the calibration curve, are discussed in detail.Biological validation of the proposed procedure is described by reference to experiments already well documented biochemically, such as the induction effect of reserpine on TH in the rat locus coeruleus and the depleting effect of α-methyltyrosine (AMPT), a well-known blocker of TH activity, on rat striatal DA content. Finally the importance of restricting the measurements to the (pseudo)linear portion of the calibration curve is illustrated by the autoradiographic identification of the differential intrastriatal repartition of the dopaminergic D1 and D2 receptorsites, particularly the dual patch-matrix compartments.

Triadimefon is a triazole fungicide that produces hyperactivity in both mice and rats similar to that seen following administration of compounds with catecholaminergic activity (e.g., d-amphetamine). To determine whether the triadimefon-induced hyperactivity is due to an action on CNS catecholaminergic systems, we evaluated the effects of combined treatment of triadimefon with either the tyrosine hydroxlase inhibitor d,l-a-methyl-p-tyrosine methyl ester HCl

The aim of the study was to evaluate the antiulcer activity of Linum usitatissimum fixed oil against aspirin-, indomethacin-, ethanol-, reserpine-, serotonin- and stress-induced gastric ulceration in rats and histamine-induced gastric ulceration in guinea pigs. Attempts were also made to evaluate the in vitro anticholinergic and antihistaminic activity and in vivo antisecretary and antiulcer activity of oil following pylorus ligation in rats. L. usitatissimum fixed oil exhibited significant antiulcer activity against different ulcerogens in experimental animal models. The fixed oil significantly inhibited acetylcholine- and histamine-induced contraction of guinea pig and rat ileums, respectively, suggesting its anticholinergic and antihistaminic activity. The oil also exhibited significant inhibitory effect on gastric secretion/total acidity and aspirin-induced gastric ulceration in pylorus-ligated rats. The lipoxygenase inhibitory, histamine antagonistic and antisecretory (anticholinergic) effects of the oil could probably have contributed towards antiulcer activity. L. usitatissimum fixed oil may be considered to be a drug of natural origin which possesses significant antiulcer activity. The present observation is the first experimental data showing antiulcer activity of L. usitatissimum fixed oil.

Chronic administration of reserpine to rats increases, in sympathetic ganglia and adrenal medulla, the activity of tyrosine hydroxylase (EC 1.14.3.x), the enzyme catalyzing the rate-limiting step in the biosynthesis of catecholamines. Immunochemical titration of the enzyme in both adrenal gland and innervated superior cervical ganglia demonstrates that enhanced enzyme activity is entirely attributable to accumulation of more specific enzyme protein and not activation of pre-existent enzyme molecules.

The study revealed the growth performance, root yield and reserpine content in the root part of R. serpentina and R. tetraphylla under four different treatment regimes (T1,T2, T3, T4). Three types of cutting like root, root-stem junction and stem of 2 to 2.5 years old plants of both the species were used. It was concluded that root formation percentage from cuttings of root, root-stem junction and stem under different treatment conditions in R. serpentina were varied from 33.33–85.00 %, 31.67– 50.00% and 20.00–33.33 %, respectively. A similar trend
was observed in in R. tetraphylla. Vermicompost (T1) showed comparatively maximum root biomass increased percentage followed by Cowpat (T2) in R. serpentina though it was more or less similar in R. tetraphylla. The application of T1, T2, T3 and T4 compositions significantly (P=0.01) increased root mean dry weight in all plant cutting types of both the species against control and the trend was root-stem junction cutting > root cutting > stem cutting. Application of NPK fertilizer decreased the soil pH from 6.73 (T5) to 6.6 (T3 and T4). In T1 and T2
pots the available soil nitrogen significantly increased by 0.0079 % and 0.0072 %, respectively. NAA at 50 ppm had highest impact on root formation followed by IAA and IBA then at 5 ppm of 2,4–D in R. tetraphylla. Quantification of reserpine in root of treated plants by HPTLC revealed significant variation.

Harmane, harmine and norharmane are β-carboline compounds which have been referred to as inverse agonists of benzodiazepine receptors. The effect of these compounds on apomorphine-induced licking behavior was studied in rats. Subcutaneous (s.c.) injection of apomorphine (0.5 mg/kg) induced licking. The licking behavior was counted with a hand counter and recorded for a period of 75 min by direct observation. Intraperitoneal (i.p.) injections of harmane (1.25–5 mg/kg), harmine (2.5–10 mg/kg) and norharmane (1.25–5 mg/kg) significantly reduced the licking behavior. In rats pretreated with reserpine (5 mg/kg, i.p., 18 h before the test), the effects of harmane (4 mg/kg, i.p.), harmine (7.8 mg/kg, i.p.) and norharmane (2.5 mg/kg, i.p.) were unchanged. When flumazenil (2 mg/kg, i.p.) was administered 20 min before apomorphine, it was able to antagonize the effects of harmane, harmine and norharmane. It was concluded that the β-carbolines harmane, harmine and norharmane reduce the licking behavior via an inverse agonistic mechanism located in the benzodiazepine receptors.Harmane, harmine and norharmane are β-carboline compounds which have been referred to as inverse agonists of benzodiazepine receptors. Effects of these compounds on apomorphine-induced licking behavior were studied in rats.► Harmane, harmine and norharmane are β-carboline compounds. ► Effect of these compounds on apomorphine-induced licking was studied in rats. ► Harmane, harmine and norharmane significantly reduced the licking behavior. ► The effects were prevented in rats treated by flumazenil but not by reserpine. ► The results indicated an involvement of benzodiazepinergic system.

l-DOPA is the most widely used treatment for Parkinson's disease. The anti-parkinsonian and pro-dyskinetic actions of l-DOPA are widely attributed to its conversion, by the enzyme aromatic l-amino acid decarboxylase (AADC), to dopamine. We investigated the hypothesis that exogenous l-DOPA can induce behavioural effects without being converted to dopamine in the reserpine-treated rat-model of Parkinson's disease. A parkinsonian state was induced with reserpine (3 mg/kg s.c.). Eighteen hours later, the rats were administered l-DOPA plus the peripherally acting AADC inhibitor benserazide (25 mg/kg), with or without the centrally acting AADC inhibitor NSD1015 (100 mg/kg). l-DOPA/benserazide alone reversed reserpine-induced akinesia (4158 ± 1125 activity counts/6 h, cf vehicle 1327 ± 227). Addition of NSD1015 elicited hyperactive behaviour that was approximately 7-fold higher than l-DOPA/benserazide (35755 ± 5226, P < 0.001). The hyperactivity induced by l-DOPA and NSD1015 was reduced by the alpha2C antagonist rauwolscine (1 mg/kg) and the 5-HT2C agonist MK212 (5 mg/kg), but not by the D2 dopamine receptor antagonist remoxipride (3 mg/kg) or the D1 dopamine receptor antagonist SCH23390 (1 mg/kg). These data suggest that l-DOPA, or metabolites produced via routes not involving AADC, might be responsible for the generation of at least some l-DOPA actions in reserpine-treated rats.

Effect of methanolic extract of Hibiscus rosa sinensis (100-300 mg/kg) was studied on reserpine-induced orofacial dyskinesia and neurochemical alterations. The rats were treated with intraperitoneal reserpine (1 mg/kg, ip) for 3 days every other day. On day 5, vacuous ...

Various factors influencing the performance of a Hadamard transform time-of-flight mass spectrometer (HT-TOFMS) have been investigated. Using a nitrogen corona discharge to produce an ion stream of N 2+, N 3+, and N 4+, it is found for spectra containing only N 4+ that the signal-to-noise ratio (SNR) closely approaches the value calculated from the ion background by assuming that the ion background follows a Poisson distribution. In contrast, for a more intense beam containing N 2+, N 3+, and N 4+, the SNR is less than its theoretical value because of the appearance of discrete spikes in the mass spectrum caused by deviations in the actual modulation sequence from the ideal one. These spikes can be reduced, however, by decreasing the modulation voltage. Under these optimized conditions, the pseudo-random sequence length is varied to understand how it alters SNR, mass resolution, and scan speed. When the length of the pseudo-random sequence is doubled, the SNR increases by √2 while the time necessary to record a mass spectrum also doubles. Mass resolution can be varied between 500 and 1200 at m/z = 609 as the sequence length, modulation speed (10 MHz, 25 MHz), and acquisition rate (up to 50 MHz) are changed. Scan speeds of 6000 passes per s can be obtained using a sequence containing 4095 elements modulated at 25 MHz. The capability to tailor the HT-TOFMS to increase the scan speed and resolution with a constant 50% duty cycle makes the technique extremely appealing as a mass analyzer for measuring rapid changes in the composition of an ion stream.

Methylmercury (MeHg) produces significant increases in the spontaneous output of dopamine (DA) from rat striatal tissue. The mechanism through MeHg produces such increase in the extracellular DA levels could be due to increased DA release or decreased DA uptake into DA terminals. One of the aims of this study was to investigate the role of DA transporter (DAT) in the MeHg-induced DA release. Coinfusion of 400 μM MeHg and nomifensine (50 μM) or amphetamine (50 μM) produced increases in the release of DA similar to those produced by nomifensine and amphetamine alone. In the same way, MeHg-induced DA release was not attenuated under Ca2+-free conditions or after pretreatment with reserpine (10 mg/kg i.p.) or tetrodotoxin (TTX), suggesting that the DA release was independent of calcium and vesicular stores, as well as it was not affected by the blockade of voltage sensitive sodium channels. Thus, to investigate whether depolarization of dopaminergic terminal was able to affect MeHg-induced DA release, we infused 75 mM KCl through the dyalisis membrane. Our results clearly showed a decrease induced by MeHg in the KCl-evoked DA release. Taken together, these results suggest that MeHg induces release of DA via transporter-dependent, calcium- and vesicular-independent mechanism and it decreases the KCl-evoked DA release.

The results show that this inhibitor only affects the MIC of nalidixic acid, while the MIC of ciprofloxacin did not change. In 45% of the A. baumannii clinical isolates the MIC of nalidixic acid decreased at least eight-fold in the presence of this compound, while the MIC decreased in only 18% of the S. maltophilia clinical isolates (Table). The results

The ethanolic root extract of Croton zambesicus was investigated for its potential to protect gastric mucosa against ulcers induced by indomethacin, ethanol and reserpine. The anticonvulsant activity of the root extract against pentylene tetrazol(PTZ )- and picrotoxin-induced convulsion in mice was also studied. The extract (27- 81mg/kg) produced a significant (P&lt;0.005-0.001) dose-dependent effects against the ulcerogenic effect of differents agents

In vivo electroporation (EP) is gaining momentum for drug and gene delivery. In particular, DNA transfer by EP to muscle tissue can lead to highly efficient long-term gene expression. We characterized a vascular effect of in vivo EP and its consequences for drug and gene delivery. Pulses of 10–20 000 μs and 0.1–1.6 kV/cm were applied over hind- and forelimb of mice and perfusion was examined by dye injection. The role of a sympathetically mediated vasoconstrictory reflex was investigated by pretreatment with reserpine. Expression of a transferred gene (luciferase), permeabilization (determined using 51Cr-EDTA), membrane resealing and effects on perfusion were compared to assess the significance of the vascular effects. Above the permeabilization threshold, a sympathetically mediated Raynaud-like phenomenon with perfusion delays of 1–2 min was observed. Resolution of this phase followed kinetics of membrane resealing. Above a second threshold, irreversible permeabilization led to long perfusion delays. These vascular reactions (1) affect kinetics of drug delivery, (2) predict efficient DNA transfer, which is optimal during short perfusion delays, and (3) might explain electrocardiographic ST segment depressions after defibrillation as being caused by vascular effects of EP of cardiac muscle.

The effects of a previous long-term administration of the mitochondrial toxin 3-nitropropionic acid were studied on an animal model of tardive dyskinesia, i.e., the frequency of spontaneous tongue protrusions in rats repeatedly treated with reserpine. 3-Nitropropionic acid (10 or 15 mg/kg i.p., every other day for 17 days) potentiated the increase in tongue-protrusion frequency induced by reserpine (1 mg/kg, s.c., every other day for 3 days) but did not modify reserpine-induced increase in immobility duration and decrease in locomotion frequency. These results support the notion that neurotoxic events are associated with the development of tardive dyskinesia.