Spontaneous activity of foregut and hindgut visceral muscle of the locust,Locusta migratoria—II. The effect of biogenic amines

1. At 10⁻⁸ M, 5-HT increased both the frequency and amplitude of contractions of isolated locust foregut. At 10⁻⁴ M the foregut general tonus was increased.2. Both spontaneously active and quiescent hindguts were less sensitive to 5-HT, showing only an increase in amplitude of contraction at 10⁻⁶−10⁻⁵ M.3. The Hill plot suggested that although the 5-HT receptor populations in these two gut divisions differed in affinities, they were essentially homogeneous.4. Octopamine (10⁻⁵−10⁻⁴ M) increased foregut contraction frequency but diminished amplitude.5. Octopamine action on the hindgut was varied. At 10⁻⁸ M it slightly increased tonus, while at 10⁻⁵ M it increased contraction amplitude without affecting frequency.6. At 10⁻⁴ M octopamine suppressed activity of spontaneously active preparations and lowered the tonus of quiescent preparations.7. Tyramine induced dose-dependent inhibition of foregut responses to 5-HT. The hindgut was exceptionally sensitive to tyramine, at only 10⁻⁸ M it suppressed 5-HT responses.8. Octopamine inhibited fore- and hindgut responses to 5-HT, but was less effective than tyramine.9. Locust fore- and hindgut have remarkably different pharmacological properties reflecting differences in innervation and in extrajunctional monoamine receptor affinities.     

The pharmacology of the isolated foregut of the locust schistocerca gregaria—I. the effect of a range of putative neurotransmitters

1. Isolated locust foreguts exhibited little or no spontaneous contractile activity.2. Proctolin (10⁻⁹m-10⁻⁶m) caused rapid and powerful contraction of the tissue while the response to similar doses of l-glutamate was much weaker.3. 5-HT (10⁻⁸M-5 × 10⁻⁶M), acting at ketanserin-sensitive receptors, was the most powerful tissue relaxant tested.4. Relaxation caused by octopamine (10⁻⁷M-10⁻⁵M), acting at ketanserin-insensitive receptors was less than 50% of that caused by similar concentrations of 5-HT.5. ACh (10⁻⁵M-10⁻³M) induced relaxation, mimicked by nicotine and antagonised by d-tubocurarine, was seen only in the presence of the anti-cholinesterase neostigmine.     

Pharmacology of the isolated foregut of the locust Schistocerca gregaria—IV. Characterization of a muscarinic acetylcholine receptor

1. Acetylcholine (ACh; 10⁻⁶ M—7 × 10⁻⁵ M), in the presence of neostigmine (10⁻⁵ M), caused contraction of the locust isolated foregut.2. The effect of ACh was mimicked by carbachol, propionylcholine (PCh), butyrylcholine (BCh), nicotine, SD35651, oxotremorine and muscarine.3. The contractions caused by ACh, BCh and carbachol were abolished by atropine (10⁻⁶M) and reduced by d-tubocurarine (10⁻⁵ M) and decamethonium (5 × 10⁻⁵ M). Hexamethonium and α-bungaro-toxin had no effect on contractions caused by the above agonists.4. None of the antagonists used in this study blocked the contractile effects of nicotine.5. It is concluded that the foregut contains a neuronal nicotinic receptor which, when activated, causes release of ACh which acts on a neuromuscular muscarinic receptor.     

The pharmacology of the isolated foregut of the locust Schistocerca gregaria—II. characterization of a 5-HT2-like receptor

1. 5-HT (10⁻⁸−5 × 10⁻⁶ M) relaxed isolated locust foreguts.2. The effects of 5-HT were mimicked by 5,6-DHT, 5-MeOT, tryptamine, 5-MeT, MK212 and methysergide while 5-hydroxyindole, 5-hydroxyindole acetic acid, 5-hydroxytryptophol, NN-DMT, 8-OH DPAT and RU 24969 were without effect.3. Ketanserin (pA₂ = 5.65) was a competitive antagonist of the effects of 5-HT, MK212 and methysergide.4. Mianserin (pA₂ = 6.3) was also a competititve antagonist of 5-HT but ICS 205-930 had no antagonistic effect on 5-HT-induced relaxation.5. It is concluded that 5-HT relaxes the locust foregut by interacting with 5-HT₂-like receptors.     

Mitochondrial preparations from the fruit of the apple—I. : Preparation and general activity

A fraction has been prepared from apple ftuits and shown to have many of the properties generally ascribed to “mitochoadria”. It is considered tet the activity of such preparations, which can be obtained with a degree of reproducibility, quantitatively represents the mitochondrial activity in tissue from fruit in a “steady” physiological state and warrants their use in studies of changes in mitochondrial activity with changing physiological states.     

Leg kinematics and muscle activity during treadmill running in the cockroach, Blaberus discoidalis : I. Slow running

We have combined high-speed video motion analysis of leg movements with electromyogram (EMG) recordings from leg muscles in cockroaches running on a treadmill. The mesothoracic (T2) and metathoracic (T3) legs have different kinematics. While in each leg the coxa-femur (CF) joint moves in unison with the femur-tibia (FT) joint, the relative joint excursions differ between T2 and T3 legs. In T3 legs, the two joints move through approximately the same excursion. In T2 legs, the FT joint moves through a narrower range of angles than the CF joint. In spite of these differences in motion, no differences between the T2 and T3 legs were seen in timing or qualitative patterns of depressor coxa and extensor tibia activity. The average firing frequencies of slow depressor coxa (Ds) and slow extensor tibia (SETi) motor neurons are directly proportional to the average angular velocity of their joints during stance. The average Ds and SETi firing frequency appears to be modulated on a cycle-by-cycle basis to control running speed and orientation. In contrast, while the frequency variations within Ds and SETi bursts were consistent across cycles, the variations within each burst did not parallel variations in the velocity of the relevant joints. Accepted: 24 May 1997     

Populational analysis of thermal responses—I. Changes in the heat resistance of muscle tissue and contractile muscle models of Salamandra salamandra larvae

• 1.1.|Study has been made of the heat resistance of m. rectus superficialis and their contractile models of larvae of 12 families of Salamandra salamandra kept at three different temperatures: 14, 21 (optimal) and 27°C. The heat resistance of the organism has been studied only in larvae kept at 21°C.
• 2.2.|An inverse linear relation has been found between the level of the average heat resistance of muscles for offspring, of the same family, under optimal conditions and its increase caused by a change in environmental temperature. A similar relationship was observed in contractile muscle models. This implies that a population responds to a change in environmental temperature as a function al system.
• 3.3.|The analysis of individual differences in the pattern of response of muscles, and their contractile models, to changes in environmental temperature allows the systemal and individual components to be isolated. The extent of co-ordination in responses of different individuals of the population can be evaluated from the proportion of the systemal component. The value of this component varies from 0.60 to 0.90.
• 4.4.|Selective advantage during thermal selection belongs to individuals with lower heat resistance of muscles.

     

Studies on the initiation of growth and moulting in Locusta migratoria migratorioides R. & F.—I: The time and nature of the initiating stimulus

Studies were made to determine the time during a stadium at which the growth and moulting hormone is released from the brain and/or corpora cardiaca of the locust. The criterion used was the appearance of mitotic figures in the prothoracic gland. Samples were taken at known ages from just before the second ecdysis until the middle of the fifth instar. The locusts were fixed in Bouin's fluid, the prothoracic glands dissected out, stained, and mounted, and the absolute number of mitotic figures present in each gland counted. These results show: (A) that the appearance of mitotic figures in the prothoracic gland precedes their appearance in the epidermis; (B) at 28°C and 43°C the maximum number of mitotic figures present occurs at the moment of ecdysis; no figures were found during the late middle stages of an instar; (C) at 25°C, the maximum number of figures occurs after some 20 per cent of the stadium has passed; (D) at all temperatures the first mitotic figures appear during the 12 hr period preceding ecdysis. It is therefore suggested that the release of the growth and moulting hormone coincides with the onset of ecdysis, and it is possible that the emptying of the gut at this time may provide the stimulus for its release. This would enable one moulting cycle to follow another independently of any external stimulus and as rapidly as possible. It further points to studies on the relationships of the stomatogastric and neuroendocrine systems for the elucidation of mechanisms of the initiation of growth and moulting in the locust.     

Histological specificity of respiratory pigments—I. Comparisons of the coelom and muscle hemoglobins of the polychaete worm travisia pupa and the echiuroid worm arhynchite pugettensis

Ion-equalized samples of hemoglobins from the blood vessels, coelomic erythrocytes, and the body-wall muscles of the polyuchaete Travisia pupa indicate that these proteins are biochemically distinct on the basis of oxygen equilibria and denaturation. The differences in oxygen affinity suggest the following oxygen transfer system: paradopial gills, via the blood, then to the coelom, and finally to the body-wall musculature. The oxygen affinities of all three pigments are exceedingly high, as might be expected for an animal that lives in an extremely oxygen-deficient environment and is markedly sensitive to oxygen poisoning even at atmospheric oxygen partial pressures. Ion-equalized preparations of hemoglobin from the coelomic erythrocytes and the body-wall muscles of the echiuroid Arynchite pugettensis have distinct oxygen equilibria. The oxygen affinity of both pigments is much lower than those of Travisia hemoglobins. The muscle hemoglogin has a lower oxygen affinity than the coelomic pigments. Lack of informatiion on the respiratory physiology of the rare echiuroid Arhynchite and absence of data on the intracellular oxygen equilibria of the hemoglobins render the physiological interpretation of these results difficult, even though it is clear that biochemical tissue specificity of hemoglobin occurs in this worm, as well as in Travisia.     

Nonsteroidal anti-inflammatory drugs: I. A study of “structure-efficacy of the anti-inflammatory effect relationship activity”

Using the computer system SARD-21 (Structure Activity Relationship &; Design) structural features typical for the high-and low-effective nonsteroidal anti-inflammatory drugs (NSAIDs) have been recognized and the influence of these features on the anti-inflammatory properties have been evaluated. This information has been used for generation of the model for prediction of anti-inflammatory effectiveness of pharmaceutical preparations with 76% and 81% levels of recognition by two methods. The recognized structural parameters may be successfully used for creation of new highly effective NSAIDs, and also for modification of structures of known NSAIDs for the increase of effectiveness of their anti-inflammatory action.     

Computer simulation of the motoneuron pool–muscle complex. I. Input system and motoneuron pool

 The aim of the present study was to simulate the input system and the motoneuron (MN) pool of the MN pool–muscle complex (MNPMC). Input fibers, which can originate from command centers in the central nervous system or from sensory organs, activate the MN pool. They generate sequences of action potentials, the frequency of which is proportional to a time-dependent activation factor (which is an input to the model). Different connection patterns between the input fibers and motor units (MUs) are allowed. For simplicity and since no precise experimental data are available, 70 input fibers and 4 boutons per fiber and MN are simulated (this corresponds approximately to the monosynaptic group-Ia input of the cat medial gastrocnemius muscle). Each bouton generates the same conductance change in the postsynaptic membrane. The MNs are modeled with a single compartment and a homogenous membrane. According to experimental data, the membrane leakage conductance and capacitance are MU dependent. Since the precise relation is unknown: (a) the computed relation between MU contraction force and the MN leakage conductance was taken from a steady-state MNPMC model, and (b) the capacitance was assumed to be proportional to the leakage conductance. The MN membrane includes time- and voltage-dependent ionic channels (fast and slow K⁺ and low- and high-threshold Ca²⁺ channels). The density and time constant of the slow K⁺ channels and the density of the Ca²⁺ channels were fitted to approximate afterhyperpolarization characteristics and frequency-injected current relations of type-identified cat MNs. If the membrane reaches a voltage threshold the MNs generate action potentials, which were simulated by voltage pulses. The activation of the MN pool of the human first dorsal interosseus muscle was simulated with injected and synaptic currents in order to illustrate the size principle, synaptic noise, and other features of muscle activation. It is concluded that the present model reproduces the main properties of the input–output relations of different MN types within a muscle. Together with the simulation of the muscle force and the surface EMG, which will be published in subsequent papers, it will be a powerful tool for reproducing experiments on the motor system and investigating functional mechanisms of motor control. Received: 17 April 2001 / Accepted in revised form: 6 November 2001     

Oral Glucose Tolerance and Related Factors in a Normal Population Sample—I. Blood Sugar,Plasma Insulin,Glyceride, and Cholesterol Measurements and the Effects of Age and Sex

Oral glucose tolerance tests were performed on 220 people, a representative sample of the employees of a large pharmaceutical company. Blood sugar and plasma immunoreactive insulin levels were measured on each sample of venous blood obtained before and at half-hourly intervals for two hours after 50 g. of glucose by mouth; plasma cholesterol and glycerides were measured on the fasting sample only.Women had higher mean insulin levels throughout the test, though their mean blood sugar levels were higher only at 90 and 120 minutes. In both sexes there were positive correlations between age and the levels of blood sugar, plasma cholesterol, and plasma glycerides. Though the levels of glucose rose with age, those of insulin did not.     

Interrelationships between ornithine,glutamate and GABA—I. Feed-back inhibition of ornithine aminotransferase by elevated brain GABA levels

In this work new methods for the determination of ornithine (Orn) and l-ornithine:2-oxoacid aminotransferase (OAT) activity are described. These methods were used to demonstrate linear interrelationships between brain GABA and Orn concentrations. Brain GABA levels were modulated by administration of vigabatrin (4-aminohex-5-enoic acid), a specific inactivator of GABA-T, which is not an inhibitor of OAT. The results suggest feed-back inhibition of OAT by GABA, a mechanism which is compatible with the assumption that Orn may serve in certain neurons as a precursor of glutamate and GABA.     

Effects of the venom of the solitary wasp Philanthus triangulum F. on glutamate uptake in the nerve endings of locust muscles—A high resolution autoradiographic study

Using electron microscope autoradiography it was shown that the glutamate uptake in both glia cells and axon in the synaptic region of locust muscles was reduced to ca. 50% under the influence of the venom of the solitary wasp Philanthus triangulum F. However, the ratio of the glutamate accumulation in the glia and the nerves remained identical. Implications are discussed in relation to known postsynaptic effects of the venom of Philanthus triangulum F.     

Determination of the transgalactosylation activity of Aspergillus oryzae β-galactosidase: effect of pH, temperature, and galactose and glucose concentrations

The catalytic potential of β-galactosidase is usually determined by its hydrolytic activity over natural or synthetic substrates. However, this method poorly predicts enzyme behavior when transglycosylation instead of hydrolysis is being performed. A system for determining the transgalactosylation activity of β-galactosidase from Aspergillus oryzae was developed, and its activity was determined under conditions for the synthesis of galacto-oligosaccharides and lactulose. Transgalactosylation activity increased with temperature up to 55 °C while the effect of pH was mild in the range from pH 2.5 to 5.5, decreasing at higher values. The effect of glucose and galactose on transgalactosylation activity was also assessed both in the reactions for the synthesis of galacto-oligosaccharides and lactulose and also in the reaction of hydrolysis of o-nitrophenyl β-d-galactopiranoside. Galactose was a competitive inhibitor and its effect was stronger in the reactions of transgalactosylation than in the reaction of hydrolysis. Glucose was a mild activator of β-galactosidase in the reaction of hydrolysis, but its mechanism of action was more complex in the reactions of transgalactosylation, having this positive effect only at low concentrations while acting as an inhibitor at high concentrations. This information is relevant to properly assess the effect of monosaccharides during the reactions of the synthesis of lactose-derived oligosaccharides, such as galacto-oligosaccharides and lactulose.