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Biomedical subjects

X Bai

Publications and source records attributed to X Bai.

102 records · Page 6Linked to original sources
PubMed1995

Stimulation of rat striatal tyrosine hydroxylase activity following intranigral administration of sigma receptor ligands.

The effects of sigma ligands on turning behavior and striatal tyrosine hydroxylase activity were determined following microinjection of two chemically dissimilar sigma ligands into the rat substantia nigra. Striatal tyrosine hydroxylase activity was monitored by measuring the amount of 3,4-dihydroxyphenylalanine (DOPA) formed following inhibition of DOPA decarboxylase activity with m-hydroxybenzylhydrazine (NSD-1015). The sigma ligands, 1,3-di-o-tolylguanidine (DTG) and (-)-deoxy-N-benzylnormetazocine, produced a significant increase both in contralateral turning and in tyrosine hydroxylase activity. The DTG-induced increase in tyrosine hydroxylase activity was not antagonized by intranigral injection of the NMDA receptor antagonist, 3-(2-carboxypiperazine-4-yl)-propyl-1-phosphonic acid (CPP). CPP alone produced significant contralateral turning that was not accompanied by an increase in striatal tyrosine hydroxylase activity, indicating that turning per se is not sufficient to activate striatal tyrosine hydroxylase. The DTG-induced increase in tyrosine hydroxylase activity was antagonized by general anesthetics such as halothane and chloral hydrate. These results indicate that occupancy of sigma receptors in the substantia nigra is associated with an activation of dopamine formation in dopaminergic terminals in the striatum and support the concept that sigma activity in the substantia nigra produces an activation of dopamine-mediated responses in the striatum.

Animals↗
PubMed1995

(+)-cis-N-(para-, meta-, and ortho-substituted benzyl)-N-normetazocines: synthesis and binding affinity at the [3H]-(+)-pentazocine-labeled (sigma 1) site and quantitative structure-affinity relationship studies.

sigma 1 receptor ligands have potential pharmacological significance as antipsychotic drugs, as tools in the study of drug-induced motor function disorders, and as radiopharmaceutical imaging agents for the noninvasive imaging of malignant tumors in human subjects. A series of substituted N-benzyl-N-normetazocines were synthesized and their binding affinity at the sigma 1 receptor evaluated in order to examine the details of the structure--affinity relationships (SAR) of a previously determined high-affinity lead compound, (+)-cis-N-benzyl-N-normetazocine (Ki = 0.67 nM). Variation in the benzyl substituents of these compounds produced a 1590-fold range in affinity at the sigma 1 receptor from the unsubstituted benzyl analog to the lowest affinity p-tert-butylbenzyl analog (Ki = 1066 nM). The nanomolar binding affinity for the sigma 1 receptor of (+)-cis-N-(4-fluorobenzyl)-N-normetzocine suggests that this analog may be a useful PET imaging agent.

Animals↗
PubMed1995

Acidic metabolites of tamoxifen. Aspects of formation and fate in the female rat.

The nonsteroidal antiestrogen tamoxifen (TAM) is subject to extensive biotransformation in humans and laboratory animals. In particular, the dimethylamino group of TAM undergoes N-demethylation and formal replacement with a hydroxyl group, affording major metabolites TAM amine and TAM alcohol, respectively. In the present study in ovariectomized rats, TAM was eliminated in part as metabolites arising from conversion of its basic side chain to an oxyacetic acid moiety. Thus, TAM acid (TA) was characterized spectrally from the urine of rats after intraperitoneal administration of TAM. TA was not detected in fecal extracts. In contrast, a second metabolite, 4-hydroxy TA (4HTA), was detected and characterized only from fecal extracts, indicative of a qualitative difference in routes of elimination for TA and 4HTA. Studies with rat liver fractions suggested TAM alcohol to be an intermediate metabolite in the conversion of TAM to TA and 4HTA. In liver microsomal fraction, TAM alcohol was converted to a novel metabolite, TAM aldehyde, which was isolated and characterized as its semicarbazone derivative. Coenzyme requirements for formation of this (derivative) metabolite, as well as for conversion of TA to 4HTA, indicated these transformations to be catalyzed by cytochromes P450. TAM aldehyde was shown to be a plausible intermediate in the formation of acidic metabolites by experiments that indicated oxidation of this to TA was catalyzed by aldehyde oxidase derived from liver cytosolic fraction.

Animals↗
PubMed1993

A comparison of (-)-deoxybenzomorphans devoid of opiate activity with their dextrorotatory phenolic counterparts suggests role of sigma 2 receptors in motor function.

Three novel benzomorphans, (+)-N-benzylnormetazocine, (-)-deoxy-N-benzylnormetazocine, and (-)-deoxypentazocine were tested for their ability to produce circling behavior in rats following intranigral microinjections. Dose studies revealed the following rank order of potency: (-)-deoxypentazocine > (-)-deoxy-N-benzylnormetazocine > (+)-N-benzylnormetazocine. This rank order approximates that for affinities for sigma 2 receptors but not sigma 1 receptors. It is very unlikely that the effects of the (-)-deoxybenzomorphans were mediated by opiate receptors for the following reasons: (1) consistent with the known requirement for the phenolic hydroxyl group for opiate activity, both (-)-deoxy compounds showed very low affinity for opiate receptors; (2) naloxone (4 micrograms) co-administered with (-)-deoxy-N-benzylnormetazocine failed to reduce its efficacy; (3) both (-)-deoxy compounds failed to produce marked analgesic effects in the tail flick test following systemic injections of 20 mg/kg s.c. These finding suggest that sigma 2 receptors mediate the motor effects of sigma ligands in rats.

Animals↗
PubMed1993

Comparisons of nucleotide and deduced amino acid sequences of the glycoprotein genes of a Chinese street strain (CGX89-1) and a Chinese vaccine strain (3aG) of rabies virus.

We analyzed the glycoprotein gene sequences of a Chinese street rabies virus strain (CGX89-1) and a Chinese human rabies vaccine strain (3aG). The complete glycoprotein gene sequence of each strain has 1575 nucleotides and encodes a polypeptide of 524 amino acids. The overall nucleotide homology of these glycoprotein genes is 84.5%, and the deduced amino acid homology is 89.5%. Twenty-one percent of the base changes result in amino acid substitutions. Comparison of the homologies of the glycoprotein genes showed that the most conserved region is the ectodomain, whereas the most variable regions are the transmembrane and cytoplasmic domains. The overall nucleotide homologies of the 3aG glycoprotein and the CGX89-1 glycoprotein compared with the Pasteur virus glycoprotein are 91.2% and 84.1% respectively. The glycoprotein gene sequences presented here, the first from isolates of Chinese origin, provide insights into the biologically significant regions of this rabies gene.

Amino Acid Sequence↗
PubMed1992

Enantiomeric N-substituted N-normetazocines: a comparative study of affinities at sigma, PCP, and mu opioid receptors.

The optical antipodes of N-allyl-N-normetazocine (2; SKF 10047, NANM) were the original compounds used for the classification of the sigma receptor as distinct from other receptors such as the PCP (NMDA), opioid, and dopamine receptors. Later studies showed that (+)-N-(dimethylallyl)-N-normetazocine [(+)-4, (+)-pentazocine] was more potent and selective for the sigma receptor. In order to gain additional structure-activity relationship information, several N-substituted N-normetazocine analogs were prepared and evaluated for their sigma-1 ([3H]-(+)-3-PPP or [3H]-(+)-pentazocine), PCP ([3H]TCP), and mu opioid ([3H]DAMGO) receptor binding affinities. (+)-N-Benzyl-N-normetazocine [(+)-10)] possessed subnanomolar affinities for the sigma site, Ki = 0.67. The analog (+)-10 showed greater than 14,000- and 2400-fold selectivity, respectively, for the sigma receptor relative to the PCP and mu opioid receptors. The N-substituted N-normetazocines were enantioselective for the sigma site. The (+)-N-benzyl analog, (+)-10, showed a 55-fold selectivity relative to (-)-10. Analysis of the data also revealed that (+)-normetazocine [(+)-1] [Ki = 30 nM] possessed the highest affinity for the PCP receptor. However, (+)-metazocine [(+)-5] (Ki = 41 nM) was the most selective compound for the PCP receptor relative to the sigma (51-fold) and mu opioid (greater than 200-fold) sites.

Animals↗
PubMed1992

Analysis of electromagnetic heating patterns inside a cryopreserved organ.

Computer analysis of the induced electromagnetic field and heating distribution inside cryopreserved organs subjected to electromagnetic illumination at frequencies of 84 MHz, 434 MHz and 2.45 GHz were carried out using a spherical model for the organ, with special reference to heating in a single-mode resonant cavity. The interaction between the frequency of the incident field and the size and dielectric properties of the sample was investigated. It is shown that uniform heating of organs is likely to be achieved at lower frequencies, as might be expected. However, the ratio between the power penetration depth for plane waves and the size of the organ is not a sufficient basis on which to judge quantitatively the uniformity of the power absorption. Hot or cold spots can occur within the organ even when this ratio is greater than unity; the wavelength in the material is also an important factor. The results from this study indicate that the use of a resonant cavity as a heating applicator has advantages over plane-wave illumination. A sharp upper limit can be set to the frequency suitable for rapid and uniform heating of a given organ.

Animals↗
PubMed1992

Thrombomodulin as a marker of radiation-induced endothelial cell injury.

Cultured confluent human umbilical vein endothelial cells were irradiated in vitro with 60Co gamma rays at doses from 0 to 50 Gy. After irradiation thrombomodulin was measured at different times over 6 days in the supernatants of endothelial cell culture medium, on the surface of the cells, and within the cells. At 24 h after irradiation, an increase in the release of thrombomodulin from irradiated endothelial cells and an increase in the number of molecules and the activity of thrombomodulin on the surface of the cells were observed; these reactions were dependent on radiation dose. The capacity of the cells to produce and release thrombomodulin was decreased from 2 to 6 days after exposure to 60Co gamma rays. Our data indicate that radiation can injure endothelial cells, and that thrombomodulin may be used as a marker of radiation-induced injury in endothelial cells. The interrelationship between the dysfunction of irradiated endothelial cells and the pathological mechanisms of acute radiation disease is also discussed.

Biomarkers↗
PubMed1992

Effect of new-breviscapine on fibrinolysis and anticoagulation of human vascular endothelial cells.

Cultured confluent human umbilical vein endothelial cells were incubated with new-breviscapine (NB), a flavonoid consisting of 4-OH-scutellarin-7-O-glucuronide (C33H30O18) and FeCl3, MgCl2, and CaCl2, which is first extracted from Erigeron breviscapus (Vant) Hand-Mazz in China, 0, 6.25, 12.5, 25, 50, 100, and 1,000 micrograms.ml-1. The releases of tissue-type plasminogen activator (t-PA), and epoprostenol (Epo) from endothelial cells were stimulated by NB, but no significant effect of plasminogen activator inhibitor (PAI) activity was seen. NB 25-1,000 micrograms.ml-1 induced a production of thrombomodulin (TM) within the cells, an expression of TM on the surface of the cells, and a release of TM from the cells. Our data provide a new evidence that NB is a stimulant to fibrinolysis and anticoagulation of endothelial cells.

Anticoagulants↗
PubMed1991

A monoclonal antibody (SZ-53) against thrombomodulin inhibits thrombin-mediated release of t-PA and PGI2 from endothelial cells.

Monoclonal antibodies against thrombomodulin have become a useful means to study the structure and function of thrombomodulin. In this study, we used a monoclonal antibody against human thrombomodulin, named SZ-53, to investigate the function of thrombomodulin on the surface of cultured human umbilical vein endothelial cells. Preincubation of endothelial cells with SZ-53 before addition of thrombin not only inhibited thrombomodulin mediated activation of protein C, but also inhibited thrombin mediated release of t-PA and PGI2 from endothelial cells. The inhibitory effects depended on the concentration of SZ-53 IgG. According to our experimental results, we suggest that thrombomodulin on the surface of endothelial cells could participate in the regulation of thrombin mediated release of t-PA and PGI2 from these cells.

Antibodies, Monoclonal↗