The Antagonistic Effect of Cholecystokinin Octapeptide (CCK-8) on Opioid Effects in Cardiovascular Activities Was Mediated by CCK-B Receptor

Previous studies have shown that CCK-8 has distinct antiopioid effect in the central sites related with pain control and blood pressure control. The aim of this study was to explore the receptor mechanism by which CCK-8 antagonized the depressor effect of u- and k-opioid(?) agonists, and to observe whether CCK-8 could antagonize the depressor effect induced by muscimol, a nonopioid substance. The results showed that (i) The antagonistic effect of CCK-8 on opioid-induced hypotension could be blocked by intrathecal (i.t.) administration of CCK-B antagonist L-365, 260 at nanogram doses, or by CCK-A antagonist devazepide at doses 20—40 times higher than L-365, 260, indicating that it was the CCK-B receptor which mediates the antiopioid effect. (ⅱ) The depressor effect induced by intrathecal muscimol, a GABA agonist, was blocked neither by naloxone nor by CCK-8, supporting the notion that CCK-8 is an endogenous opioid antagonist rather than a universal anti-hypotension agent.     

THE ANTAGONISTIC EFFECTS OF TETRAHYDRO-PROTOBERBERINES ON DOPAMINE RECEPTORS: ELECTROPHYSIOLOGICAL STUDIES

Tetrahydroprotoberberines (THPBs), including (-)-stepholidine ((-)-SPD), (-)-tetrahydropalmatine ((-)-THP) and tetrahydroberberine (THB), have been demonstrated to be a new class of DA antagonists in biochemical and neuropharmacological studies. In this paper, the antagonistic action of THPBs was examined by means of single unit recording from nigral DA neuron in chloral hydrate-anesthetized and gallamine-paralyzed rats. Intravenous injection of these compounds could promptly and completely reverse the inhibition of the spontaneous firing induced by DA agonist apomorphine (APO) in a dose-dependent way. Pretreatment with (-)-SPD, (-)-THP or THB could significantly reduce the inhibitory effect of APO and shift the dose-action curve to the right. Besides, the compounds could increase the spontaneous firing of DA neurons. The above results not only strongly support the conclusion that (-)-SPD, (-)-THP and THB are DA antagonists, but also demonstrate that one of their blocking sites is at somatodendritic DA     

DIFFERENT EFFECTS OF ENANTIOMERS OF TETRAHYDROPALMATINE ON DOPAMINERGIC SYSTEM

Tetrahydropalmatine (THP) has two enantiomers with different effects on the brain dopaminergic system. Using [~3H]spiperone for DA receptor binding assay, it was found that l-THP had an affinity to DA receptors (K_1=0.2μM). Neither d-THP nor reserpine showed such an effect even at concentrations higher than 100 or 1000μM. Based on the fact that the presynaptic DA receptors take part in feed-back regulation on tyrosiue hydroxylase activity, DOPA accumulation could be observed in rat striatum after injection of benserazide. A small dose of l-THP (2.5, 5, 10 mg/kg, ip.) caused an elevation of DOPA level by 49—282% versus the control value, and could reverse the decrease of DOPA level induced by apomorphine, a DA receptor agonist. On the contrary, d-THP displayed a biphasic effect on DOPA level, slight decrement (26—37%) at 10 and 25mg/kg, naught at 50mg/kg, and a 91% increment at 100 mk/kg, which was less than that of l-THP at 5mg/kg. Moreover, measured by pulse voltammetry, DOPAC level in the striatum     

CORRELATION BETWEEN GLASS TRANSITION OF POLYMERS AND ENERGY OF ROTATIONAL ISOMERIZATION OF MOLECULAR CHAINS

It has been shown that the free volume fraction at T_g is not a universal parameter for linear polymers of different molecular structure. The reason is that the volume expansion at T_g is partially contributed from the change of the numbers of conformations of isolated molecular chains due to internal rotation. In this paper, glassy transformation was connected with internal rotation of isolated molecular chains, and the relationship between free volume fraction of polymers at T_g and energy e of rotational isomerization of isolated molecular chains was formulated, e=-k·T_g·In (△α·T_g/1-△α. T_g). The values of calculated from the above formula are in good agreement with those published in the literatures. Thus, the method described in this paper can be used to estimate a parameter for the flexibility of isolated molecular chains.7     

PARADOXICAL EFFECT OF A GnRH AGONIST ON STEROIDOGENESIS IN CULTURED MONKEY GRANULOSA CELLS

In this study we demonstrate: (i) The GnRH agonist exerts a direct dose-dependet stimulative effect on the aromatase activity and progesterone production in cultured monkey granulosa cells; (ii)the stimulative effect on steroidogenesis can be completely blocked by concomitant treatment with a GnRH antagonist, suggesting that the actions of GnRH are mediated through stringent stereospecific recongnition sites; (iii) in addition to the stimulative effect, the GnRH agonist in the presence of gonadotropins also exerts an inhibitory effect, even though the peptide by itself is more effective in the stimulation of steroidogenesis, and the stimulation of gonadotropin on steroidogenesis could be gradually restored by decreasing the concentration of the GnRH agonist in the culture; and (iv) paradoxical effect can also be observed in the presence of cAMP-inducing agents, suggesting that the inhibitory action of the peptide on gonadotropin-induced steroidogenesis is localized at a step distal to the stringent reco     

THE ROUTE OF INCORPORATION OF NITROGEN ATOM INTO RIFAMYCIN DURING ITS BIOSYNTHESIS

In this paper, it was first shown that under various conditions of nitrogen supply therifamycin yield was positively correlated with the mycelial specific activity of glutaminesynthetase (GS), then the enhancing effect of glutamine, the product of GS, on rifamycin bio-synthesis was demonstrated with resting cell system. The stimulatory effect of glutaminewas more pronounced than that of glutamate, and not reduced by a GS specific inhibitor, DON.However, the increase in yield brought about by glutamate, and by asparagine was stronglyinhibited by this inhibitor. Glutamine-CO~(15)NH_2 and glutamato-α-~(15)NH_2 were synthesized andcompared for the incorporation of ~(15)N into rifamycin. It was found that the amide nitrogenwas incorporated to a much greater extent than the α-amino nitrogen, showing that glutaminewas a direct precursor of the nitrogen atom in rifamycin. In addition, synthesis of A-32(C_7N), an intermediate secreted by an inactive mutant rif 1, was also greatly stimulatedby glutamine, and the synthetic C_7N was found to be able to stimulate the biosynthesis ofrifamycin. Based upon the above results, the route of incorporation of nitrogen atom into rifamycinis summarized as follows:     

ZnO纳米粒子自建场的形成及对其光电特性的影响

The effect of built-in field on the surface photovoltage(SPV) response of ZnO nanoparticles was investigated by means of surface photovoltage spectroscopy(SPS). From the results of in situ SPS in atmosphere and in vacuum, we suggest that the built-in field should be a main condition for producing SPV response. By comparison of SPS with PL in vacuum as well as in atmosphere, we deduce that by changing the ambience of ZnO, its functional properties can be modulated.     

Detection of OH Radical in the Photodissociation of p-Aminobenzoic Acid at 266 nm

Photodissociation of p-aminobenzoic acid at 266 nm was investigated by probing the nascent OH photoproduct employing the laser-induced fluorescence technique. It was found that the nascent OH radical was vibrationally cold and its rotational state distribution conformed to be a Boltzmann behavior, characterized by a rotational temperature of 1040±110 K. The rotational energy of OH was determined to be 8.78±0.84 kJ/mol. Between the two spinorbit states of OH, ^2Ⅱ3/2 and ^2Ⅱ1/2, the former was found to be preferentially populated. The distribution of the II（A＇） state for the A-doublet was dominant. Finally, a probable mechanism for the formation of OH produced from the photodissociation of p-aminobenzoic acid is discussed.     

PHARMACOLOGICAL STUDY OF AN IRREVERSIBLE PARTIAL AGONIST OF OPIATE RECEPTORS, A-α-CAO

A-α-CAO induces weak analgesia with very short duration in mice and is able to antagonize the analgesic effect of morphine (Mor) up to 3—4 days after a single injection. No tendency of dependence has been observed. It acts as a partial agonist on MVD with Ke value of 9×10~(-9) mol/L. Its antagonist effect remains after several washes and its agonist effect cannot be reversed by naloxone (Nx), provided the incubation time or the concentration of the agent is sufficient. On isolated GPI, A-α-CAO is a pure agonist with IC_(50) of 5.7×10~(-10) mol/L; this agonist effect cannot be removed by washing but can be reversed by Nx. On RVD and RbVD, it has antagonist effect against β-endorphine (β-end) and US0488H, which cannot be washed out easily, and the pA_2are 7.5 and 7.6 respectively. A-α-CAO also inhibits the specific binding of ~3H-etorphine (~3H-Etor) to the P_2 fraction of the mouse brain membrane with an IC_(30) of 3.2×10~(-9) mol/L. The inhibition on the high affinity binding sites of ~3H-Etor     

A STUDY OF THE EFFECT OF ANTAGONISTIC ELEMENTS OF SELENIUM WITH GRAPHICAL AND COMPUTER BASED STATISTIC PATTERN RECOGNITION

THE antagonistic effect is important in the research on bio-trace elements,the practical aspects and an understanding ofthe mechanism of which depend on a knowledge of this effect.In this paper,the data of the per-capita intake of Seand Se-antagonistic elements (Zn,Cd,Cu,Cr,Mn,As) in 27countries and areas and the age-correlated mortalities fromcancer of the breast were treated with the graphical and com-puter based statistic pattern recognition method.The 22equations derived from computer programs of linear regressionanalysis show that a multidimensional space can be reduced toa two-dimensional one.Then the two-dimensional figures wereobtained and they illustrate some empirical rules from whichinformation on the degree and area of the antagonistic effectis obtained.The calculation results of breast mortalitiescoincide with those of the U.S.female breast observed valueand the Keshan disease in China.     

ISOLATION, CHEMICAL AND BIOLOGICAL CHARACTERIZATION OF MARGARATENSIN, A NEUROTENSIN-RELATED PEPTIDE FROM THE SKIN OF Rana margaratae

A new neurotensin (NT)-related peptide, margaratensin, was obtained by Sep-Pak C_(18) and RP-HPLC from methanol extracts of the skin of Chinese frog Rana margaratae. The structure of the peptide has been determined to be Asp-Lys-Arg-Pro-Tyr-lle-Leu-His-Glu, which is found to be homologous to the COOH-terminal sequence of NT, but has an extra His-Glu at the COOH-terminus. The synthetic preparation was shown to be indistinguishable from the native peptide during HPLC, amino acid analysis and bioassay. Margaratensin exhibited a hypotensive effect in the rat but the response was weaker than NT. The peptide could induce a potent and reproducible contractile activity on GPI which was different from xenopsin, another NT-related peptide from amphibian skin.     

STUDY OF INHIBITORY EFFECT OF AMYGDALOID STIMULATION ON AUDITORY RESPONSE OF MEDIAL GENICULATE BODY(MGB) AND ANALYSIS OF TRANSMISSIVE PATHWAY OF THE SAID EFFECT

Experiments performed on 103 rabbits immobilized with Flaxedil, and the recording of the electrical discharges of single MGB neuron caused by clicks, burst or sustained tone showed marked inhibition of the reaction of 47 out of 75 (62.7%) MGB units responding to sound stimuli, when the amygdaloid complex was stimulated. The latent period of such an inhibitory effect was 5-12 msec and its duration about 2-13 msec. Evoked responses with the latency of 1-2 msec for the stimulation of medial, central and lateral nuclei of amygdala could be recorded from the temporal and parietal cortex. The largest response was recorded from Woolsey's AI area of the temporal cortex. Stimulation of the Woolsey's AI auditory area could also result in a distinct inhibition of the spontaneous as well as the evoked discharges of MGB neurons in response to sound stimulation. Moreover, application of 1% procaine to the surface of auditory cortex could block the inhibitory effect of the amygdala on the MGB neurons. Based on the fac     

STUDY OF THE MOLECULAR MOTION AND COMPATIBILITY IN AB-CROSSLINKED POLYMER BASED ON POLYURETHANE AND POLYSTYRENE-co-ACRYLIC ACID BY SOLID STATE HIGH RESOLUTION NMR

The ~(13)C T_(1s) of --CH_3 side group in PPU/P (St-co-AA), AB-crosslinked polymers (i. e.ABCP) was studied by using high resolution solid state NMR. The rotation motion of --CH_3 sidegroup in PPU was analyzed by means of the average spectral density functions of internal rota-tion. The results showed that the rotation of the --CH_3 side group is related closely to the com-patibility between the two components. The compatibility was studied by analyzing the protonspin-lattice relaxation in rotating frame, spin-spin relaxation and spin-diffusion. The resultsshowed that the hydrogen bonds between the components play a major role in determining thecompatibility. Through spin diffusion studying, the soft phase domain size was calculated. Bystudying proton spin-spin relaxation, the content of each component in each phase and that ofeach phase in the samples can be obtained. The result shows that the content of interphase is related closely to the compatibility.     

ENVIRONMENTAL STABILITY OF THE POLYENE PREPARED BY DEHYDROCHLORINATION OF POLY(VINYL CHLORIDE)

A high-quality polyene can be obtained by exensive dehydrochlorination of poly(vinyl chloride) (PVC) in aliquid/solid two-phase system. The liquid phase is a tetrahydrofuran solution of PVC containing a small amount ofpoly(ethylene glycol) with molar mass of 400 g as a phase transfer catalys. The solid phase is potassium hydroxide particles.The structure of the polyene is polyacetylene-like and has a long conjugated C=C sequence and a narrow dispersity ofpolyene sequences according to its FT-infrared and Raman spectra. The environmental stability of the polyene was alsostudied by IR, Raman spectra and elemental analysis. Experimental results demonstrated that the polyene was susceptible toair and could be changed into a material containing high concentrations of hydroxyl and carbonyl groups. The polyenesequences were shortened and its dispersity became broader due to the effect of dioxygen.     

Imprinted Polymeric Film-Based Sensor for the Detection of Dopamine Using Cyclic Voltammetry

The imprinted polymeric film was synthesized on the glass-carbon electrodes dlrectly. The response to the template molecule-dopamine and other molecules with similar structure was measured by cyclic voltammetry. The response of dopamine on imprinted electrode was much higher than that of other molecules,because of the existing of micro-cavities in polymeric rdm fitting with the size and shape of dopamine in the imprinted polymer.Experimental results showed that dopamlne can be enriched by the imprinted film, therefore increasing the sensitivity of the sensor. The imprinted film could also efface the interference of ascorbic acid, indicating that dopamine can be determined with a large excess of ascorbic acid.     

THE ROTATION BARRIER OF ELECTRON SPIN PROBE IN THE STUDY OF POLYMER SYSTEM

In the study of molecular motion of polymer by means of ESR in combination with spin probe, owing to that the ESR spectrum depicts only the behavior of spin probe, the information obtained is of indirect nature. Hence the relationship between them must first be investigated before any conclusion could be drawn. In this paper, two parameters T_R and C_R are introduced to characterize the changing of tumbling rate of spin probe, and the concept of rotation barrier of spin probe is proposed. It is considered that the magnitude of the rotation barrier is determined by the internal cavity size and distribution in polymer. When the temperature is raised, the size and distribution of the cavities change accordingly, thus the tumbling of spin probe changes gradually from a slower to a higher rate.     

STUDY OF THE MOLECULAR MOTION IN POLYEPICHLOROHYDRIN BY HIGH RESOLUTION NMR

The molecular motion in polyepichlorohydrin (PEPCH), in solution and bulk, was studied by high resolution NMR by means of line width, spin-lattice relaxation time T_1 and nuclear Overhauser effect NOE. The results show that the VJGM model can describe the main chain motion of PEPCH in solution perfectly. In bulk state, the relationship between the line width and the temperature is consistent with WLF equation, but that between the high frequency molecular motion correlation time (in T_1 scale ) and temperature is consistent with Arrhenius equation. The motion parameters of PEPCH in both states were calculated. The internal rotation motion of side—CH_2Cl group was analyzed by using equal three-site jump and diffusion internal rotation model in both states.     

THE EFFECT OF ETHERS ON ALTERNATING COPOLYMERIZATION OF BUTADIENE AND PROPYLENE CATALYZED BY VANADIUM-ALUMINUM SYSTEM

The effect of five ethers on alternating copolymerization of br(?)adiene and propylene were investigated. It was found that under appropriate conditions, by adding ether into reaction system, the conversion could be increased by 10-20% and the catalytic efficiency doubled at -45℃. The interaction between ether and active center was also studied.     

β-PHASE CRYSTALLIZATION OF ISOTACTIC POLYPROPYLENE

Effects of cooling rate and crystallization and melt temperatures on the melting curves of predomi-nately β-phase isotactic polypropylene (IPP) were investigated by using DSC instrument. Experimental re-sults indicate that the magnitude of βmelting endctherm increases with decreasing cooling rate and withincreasing crystallization temperature. The temperature of melt has no effect on the β-phase crystallizationof IPP below 300℃, but a further increase of the melt temperature will destroy the β-phase nuclei,then the β-phase crystals will not be produced upon cooling. The linear growth rates of α- and β-phasespherulites were determined as a function of temperature between 123 and 140℃. It was found that thegrowth rate of βspherulites is higher than that of αspherulites below 140℃. Studies of the kinetics ofβ-phase crystallization of IPP were also made using a DSC instrument. The results obtained do not fitthe usual Avrami equation. But it can be described by kinetic theory of imcomplete spher     

EFFECT OF TEMPERATURE ON LOWER ALCOHOL SYNTHESIS OVER MODIFIED Cu-Zn CATALYSTS

The temperature effect on lower alcohol synthesis from CO H2 over modified Cu- Zn catalyst was investigated in this paper. The experimental results showed that the reaction temperature affected the yields of alcohols and the formation of C2 OH obviously. The content of C2 OH increased but the yields of alcohols decreased when reaction temperature increased. The cooperation roles between active components of catalyst could be regulated by the third (or fourth) component and modified by adding alkali metal and rare earths. As a result, the reaction temperature could be reduced.