共查询到20条相似文献,搜索用时 31 毫秒
1.
Marazziti Donatella Rossi Alessandra Palego Lionella Giannaccini Gino Naccarato Antonio Lucacchini Antonio Cassano Giovanni B. 《Neurochemical research》1997,22(6):753-757
This study aimed at comparing the binding characteristics of [3H]ketanserin, a high-affinity serotonin 2A (5-HT2A) receptor antagonist, in the prefrontal cortex, hippocampus and striatum of human brain post-mortem. The results indicated the presence of a single population of binding sites in all the regions investigated, with no statistical difference in maximum binding capacity (Bmax) or dissociation constant (Kd) values. The pharmacological profile of [3H]ketanserin binding was consistent with the labeling of the 5-HT2A receptor, since it revealed a competing drug potency ranking of ketanserin = spiperone > clozapine = haloperidol > methysergide > mesulergine > 5-HT. In conclusion, the 5-HT2A receptor, as labeled by [3H]ketanserin, would seem to consist of a homogenous population of binding sites and to be equally distributed in human prefronto-cortical, limbic and extrapyramidal structures. 相似文献
2.
The radioiodinated pindolol analogs 125I-labeled cyanopindolol ([125I]CYP) and 125I-labeled hydroxybenzylpindolol ([125I]HBP) have been used to study binding to human platelet β-adrenergic receptors. [125I]CYP binds to a saturable class of binding sites on platelet membranes with a dissociation constant (Kd) of 14±3 pM and maximal binding capacity (Bmax) of 18±4 fmol/mg protein. Binding of [125I]CYP is reversible and is characterized by forward and reverse rate constants of 1.8·107 s?1·M?1 and 3.8·10?4 s?1, respectively. [125I]HBP binds to a saturable class of platelet membrane sites with a Kd of 50±10 pM and Bmax of 32±6 fmol/mg protein. [125I]HBP also binds to a saturable class of sites on intact platelets with a Kd of 58±14 pM and Bmax of 24±4 molecules per platelet. Binding of [125I]CYP and [125I]HBP is stereospecifically inhibited by propranolol and epinephrine; the (?) stereoisomers are at least 50-times more potent than the (+) stereoisomers. Binding of both radioligands is inhibited by adrenergic ligands with a potency order of propranolol ? isoproterenol > epinephrine > practolol > norepinephrine > phenylephrine. These observations indicate that [125I]CYP and [125I]HBP bind to platelet sites which have the pharmacological characteristics of β-adrenergic receptors but which are not typical of either the β1 or β2 sub-type. 相似文献
3.
The biochemical and pharmacological properties of nuclear [3H]flunitrazepam in brain tissues were studied. Nuclear [3Hflunitrazepam binding is saturable for both central and peripheral binding sites. Inosine and hypoxanthine displace nuclear [3H]flunitrazepam binding with greater potency than the membrane [3H]flunitrazepam binding. Triiodothyronine (T3) increases the maximum number of binding sites (Bmax) of nuclear [3H]flunitrazepam binding in vitro while thyroxine (T4) does not have any effect. Diazepam reduces the affinity of nuclear125I-T3 binding in vitro, while the Bmax is not affected significantly. Mild digestion of chromatin, using micrococcal nuclease, reveals that a major portion of nuclear [3H]flunitrazepam binding sites are located on chromatin. These data suggest a functional role for nuclear benzodiazepine binding and a possible modulatory effect of benzodiazepines on T3 binding with its nuclear receptors. 相似文献
4.
Specific β1-adrenoreceptors antagonist [3H]CGP 26505 binding was characterized in rat cerebral cortex and heart sinus atrial node. In both tissues [3H]CGP 26505 binding was maximal at 25°C, it was specific, saturable and protein concentration dependent. Scatchard analysis
of saturation isotherms of specific [3H]CGP 26505 binding in cerebral cortex showed that [3H]CGP 26505 binds a single class of high affinity sites with a dissociation constant (KD) of 1±0.3 nM and a maximal number of binding sites (Bmax) of 40±2 fmol/mg of protein. In sinus atrial node, [3H]-CGP 26505 binds a single class of high affinity sites (KD=1.9±0.4 nM, Bmax=28±2 fmol/mg of protein). 相似文献
5.
Toshiyuki Kimura Paul A. Saunders Ikuo Yamamoto Ing K. Ho 《Neurochemical research》1991,16(10):1133-1137
Effects of pentobarbital pellet implantation on [3H]baclofen binding in the frontal cortex of cerebellum of rat brains were examined. In the frontal cortex, pentobarbital tolerance caused an increase in the number of binding sites (Bmax) without changing their affinity (KD). Twenty-four hours after withdrawal of the pentobarbital pellets, there was a significant increase in the KD and Bmax values. Cerebellar binding, in contrast, was not significantly changed in any of the treatment groups. Addition of 1 mM of pentobarbital directly to binding assays using cortical membrane produced as increase in KD without a change in Bmax.In vitro, pentobarbital affected neither the KD nor the Bmax in the cerebellar [3H]baclofen binding. These results suggest that like the GABAA receptor, [3H]baclofen binding to the GABAB receptor in rat frontal cortex was affected by pentobarbital tolerance and dependence, and that there are regional differences in the properties of the GABAB receptor. 相似文献
6.
O Hechter D Mechaber A Zwick L A Campfield B Eychenne E E Baulieu P Robel 《Archives of biochemistry and biophysics》1983,224(1):49-68
This study was undertaken to define optimal conditions for exchange of 3H-R-1881 with endogenous hormone bound to androgen receptor (AR) sites in homogenates of rat ventral prostate (RVP) of mature animals. To minimize inactivation of AR binding sites under exchange conditions, extracellular proteases present in RVP were removed by mincing and washing tissue fragments in a Ca2+-free cell culture medium (J-MEM) containing 1% casein, prior to homogenization in a TEDG buffer (50 mm Tris-maleate buffer, pH 7.4; 1.5 mm EDTA; 2.0 mm DTT; and 10% () glycerol) containing 0.5 mm phenylmercuric sulfonyl fluoride (PMSF) and 1.0 mm sodium azide. Na2MoO4 (final concentration, 20 mm) was added to homogenate fractions which then were incubated at 0–4 °C for 1–5 days with a saturating concentration of 3H-R-1881 (20 nm) in the absence and presence of 2 μm radioinert R-1881. Heparin (200 μg/ml) was added to the incubation medium to “solubilize” nuclear chromatin. Free and bound R-1881 were separated by a hydroxylapatite (HAP) batch procedure. Using these conditions, it has been found that (i) incubation periods of 72–96 h at 0–4 °C were required to achieve maximal specific exchange binding of 3H-R-1881 (Bmax) in total homogenates from normal intact rats. Heparin addition (200 μg/ml) did not change Bmax and had little or no effect on the rate of exchange. Mean Bmax was 6.7 ± 1.6 (SD) pmol 3H-R-1881/mg DNA. R-1881 exchange at 24 h of incubation was only about 40% of Bmax. Nonspecific binding, a small fraction (<10%) of Bmax, was near maximal at 2 h. Incubation at 15 °C gave similar R-1881 exchange values to those obtained at 0 °C during the first 24 h, but at 48 h and thereafter R-1881 binding markedly decreased. These Bmax values in total homogenates of normal intact RVP are about 2.5 times greater than the AR values obtained in 1-day castrated rats, when compared on a DNA basis, (ii) Addition of gelatin (0.25%) to inhibit seminin activity had no effect on Bmax. Deletion of either MoO42? or PMSF from the standard exchange medium reduced Bmax values ~20%; if both PMSF and MoO42? were deleted, Bmax was reduced to a greater extent (~35%). Bmax was reduced (40%) when homogenates were prepared without preliminary J-MEM:casein pretreatment and incubated in standard exchange medium with PMSF and MoO42?. (iii) Despite AR stabilization by MoO42? and inhibition of protease activities during exchange incubation, AR inactivation increased exponentially, so that the maximal 3H-R-1881 binding value achieved at 96 h was estimated to represent about 50% of the AR sites originally present. (iv) The binding sites in total homogenates occupied by 3H-R-1881 at 24, 72, and 96 h of exchange exhibited steroid specificity characteristics of AR, as determined by competition studies with a wide variety of steroid hormones and analogues. Scatchard plots of 3H-R-1881 exchange binding in total homogenates of normal intact RVP incubated for 72 or 96 h indicated a single class of affinity sites with apparent Kd of 5 to 6 nm. (v) Sucrose density gradient centrifugation of homogenates incubated for 72 or 96 h showed that the specific 3H-R-1881 binding sites were distributed in two broad peaks associated with low-molecular-weight components. One with S value ~3.5 may be “activated” AR; the other near the top of the gradient (S < 1.6) may include meroreceptor forms of AR. 相似文献
7.
Abstract: The present study indicates that central 5-hydroxytryptamine (5-HT; serotonin) receptors can be modulated in opposite directions by Ca2+ and guanine nucleotides [guanosine triphosphate (GTP), β, γ-imidoguanosine 5′-triphosphate (GppNHp)]. Thus CaCl2 (≥0.5 mm ) inhibited whereas GTP and GppNHp (10 μm ) stimulated the 5-HT-sensitive adenylate cyclase in the hippocampus of newborn rats. Both the affinity (Kd ?1) and the number (Bmax) of [3H]5-HT binding sites in hippocampal membranes from adult rats were increased in the presence of Ca2+ (≥0.25 mm ); GTP (≥0.1 mm ) and GppNHp (≥0.3; μm ) produced reverse effects. The efficacy of guanine nucleotides in inhibiting specific [3H]5-HT binding was counteracted by Ca2+: the addition of this cation (5mm -CaCl2) to the assay mixture resulted in a 40-fold increase in the IC50 for GTP; the IC50 for GppNHp increased five-fold under the same condition. The examination of the respective effects of Ca2+ and of GTP on the specific binding of [3H]5-HT to various hippocampal membrane preparations (from developing rats, from subcellular fractions of adult tissues, and from adult rats after the selective degeneration of serotoninergic innervation in the forebrain) indicated that the amplitudes of the Ca2+-induced increase and of the GTP-induced decrease were generally correlated. This conclusion did not apply to striatal membranes of kainic acid-treated rats because [3H]5-HT binding sites persisting after the intrastriatal injection of kainic acid (i.e., half of the total number in striatal membranes from control rats) were markedly less affected by GTP but at least as responsive as control membranes to the Ca2+-induced increase. These data are compatible with the hypothesis of a possible coupling of some–but not all–[3H]5-HT binding sites to adenylate cyclase in the rat brain. 相似文献
8.
The binding characteristics of [3H]U46619 to washed human platelets were studied. [3H]U46619 binding to washed human platelets was saturable and displaceable. Kinetic studies yielded a Kd of 11 ± 4 nM (n=4). Scatchard analysis of equilibrium binding studies revealed one class of high affinity binding sites with a Kd of 20 ± 7nM and a Bmax of 9.1 ± 2.3 fmole/107 platelets (550 ± 141 binding sites per platelet) (n=4). A number of compounds that act as either agonists or antagonists of the TXA2/PGH2 receptor were tested for their ability to inhibit the binding of [3H]U46619 to washed human platelets. The Kds of the agonists and antagonists were similar to their potencies to induce or inhibit platelet aggregation. These data provide some evidence that [3H]U46619 binds to the putative human platelet TXA2/PGH2 receptor. 相似文献
9.
Erik H. F. Wong Douglas W. Bonhaus Irene Wu Eric Stefanich Richard M. Eglen 《Journal of neurochemistry》1993,60(3):921-930
Abstract: RS-42358–197{(S)-N-(1-azabicyclo[2.2.2]oct-3-yl)-2,4,5,6-tetrahydro-1H-benzo[de]isoquinolin-1-one hydrochloride} displaced the prototypic 5-hydroxytryptamine3 (5-HT3) receptor ligand [3H]quipazine in rat cerebral cortical membranes with an affinity (pKi) of 9.8 ± 0.1, while having weak affinity (pKi < 6.0) in 23 other receptor binding assays. [3H]RS-42358–197 was then utilized to label 5-HT3 receptors in a variety of tissues. [3H]RS-42358–197 labelled high-affinity and saturable binding sites in membranes from rat cortex, NG108–15 cells, and rabbit ileal myenteric plexus with affinities (KD) of 0.12 ± 0.01, 0.20 ± 0.01, and 0.10 ± 0.01 nM and densities (Bmax) of 16.0 ± 2.0, 660 ± 74, and 88 ± 12 fmol/mg of protein, respectively. The density of sites labelled in each of these tissues with [3H]RS-42358–197 was similar to that labelled with [3H]GR 65630, but was significantly less than that found with [3H]-quipazine. The binding of [3H]RS-42358–197 had a pharmacological profile similar to that of [3H]quipazine, as indicated by the rank order of displacement potencies: RS-42358–197 > (S)-zacopride > tropisetron > (R)-zacopride > ondansetron > MDL72222 > 5-HT. However, differences in 5-HT3 receptors of different tissues and species were detected on the basis of statistically significant differences in the affinities of phenylbiguanide, and 1-(m-chlorophenyl)biguanide when displacing [3H]RS-42358-197 binding. [3H]RS-42358–197 also labelled a population (Bmax= 91 ± 17 fmol/mg of protein) of binding sites in guinea pig myenteric plexus membranes, with lower affinity (KD= 1.6 ± 0.3 nM) than those in the other preparations. Moreover, the rank order of displacement potencies of 15 5-HT3 receptor ligands in guinea pig ileum was found not to be identical to that in other tissues. Binding studies carried out with [3H]RS-42358–197 have detected differences in 5-HT3 receptor binding sites in tissues of different species and further underscore the unique nature of the guinea pig 5-HT3 receptor. 相似文献
10.
Human platelet alpha 2-adrenergic receptors: labeling with 3H-yohimbine, a selective antagonist ligand 总被引:7,自引:0,他引:7
3H-Yohimbine, a potent and selective pharmacological antagonist of α2-adrenergic receptors, labeled human platelet membrane α2-receptors with high affinity. Binding was rapid and reversible at 25°C. Both saturation and kinetic experiments indicated a single order of binding sites, with an equilibrium KD value of 1.0–1.5 nM. Low Mg2+ concentrations increased the KD for 3H-yohimbine without altering the Bmax. The 3H-yohimbine site exhibited α2-receptor specificity: (?)-norepinephrine and (?)-isoproterenol were 4.8 and 330 times less potent than (?)-epinephrine; (?)-catecholamines were 17–35 times more potent than corresponding (+)-catecholamines; the selective α1-antagonist prazosin was 340 times less potent than yohimbine. Catecholamine agonists exhibited shallow curves in inhibiting 3H-yohimbine binding, with pseudo-Hill coefficients (nH) of less than 1.0, whereas the nH of antagonists was 1.0. No specific binding of 3H-prazosin to platelet membranes was observed, indicating the absence of α1-receptors. 3H-Yohimbine labeled fewer platelet sites than did 3H-dihydroergocryptine under identical conditions (80 vs 130 receptors/ cell), and may be a more specific and useful antagonist probe of platelet α2-receptors than 3H-dihydroergocryptine. 相似文献
11.
The purpose of this study was to investigate the role of central 5-HT2C receptor binding in rat model of pancreatic regeneration using 60–70% pancreatectomy. The 5-HT and 5-HT2C receptor kinetics were studied in cerebral cortex and brain stem of sham operated, 72 h pancreatectomised and 7 days pancreatectomised rats. Scatchard analysis with [3H] mesulergine in cerebral cortex showed a significant decrease (p < 0.05) in maximal binding (Bmax) without any change in Kd in 72 h pancreatectomised rats compared with sham. The decreased Bmax reversed to sham level by 7 days after pancreatectomy. In brain stem, Scatchard analysis showed a significant decrease (p < 0.01) in Bmax with a significant increase (p < 0.01) in Kd. Competition analysis in brain stem showed a shift in affinity towards a low affinity. These parameters were reversed to sham level by 7 days after pancreatectomy. Thus the results suggest that 5-HT through the 5-HT2C receptor in the brain has a functional regulatory role in the pancreatic regeneration. 相似文献
12.
Alice H. Lin Patricia L. Ruppel Robert R. Gorman 《Prostaglandins & other lipid mediators》1984,28(6):837-849
[3H] Leukotriene B4 (LTB4) binds concentration dependency to intact human polymorophonuclear leukocytes (PMN's). The binding is saturable, reaches equilibrium in 10 min at 4°C, and is readily reversible. Mathematical modeling analysis reveals biphasic binding of [3H] LTB4 indicating two discrete populations of binding sites. The high affinity binding sites have a dissociation constant of 0.46 × 10−9M and Bmax of 1.96 × 104 sites per neutrophil; the low affinity binding sites have a dissociation constant of 541 × 10−9M and a Bmax of 45.6 × 104 sites per neutrophil. Competitive binding experiments with structural analogues of LTB4 demonstrate that the interaction between LTB4 and the binding site is stereospecific, and correlates with the relative biological activity of the analogs. At 25°C[3H] LTB4 is rapidly dissociated from the binding site and metabolized to 20-OH and 20-COOH-LTB4. Purification of neutrophils in the presence of 5-lipoxygenase inhibitors significantly increases specific [3H] LTB4 binding, suggesting that LTB4 is biosynthesized during the purification procedure. These data suggest that stereospecific binding and metabolism of LTB4 in neutrophils are tightly coupled processes. 相似文献
13.
Isabel J. Wajda Miriam Banay-Schwartz Isaac Manigault Abel Lajtha 《Neurochemical research》1986,11(7):949-957
In vivo effects of chronic lithium administration on dopaminergic and serotonergic receptor binding were studied in the striatum and cerebral cortex of the rat. [3H]Domperidone was used as the ligand for the dopaminergic receptor, and [3H]ketanserin for the serotonergic system. Long-term ingestion of lithium (2–3 months) resulted in high levels of lithium in the cerebral cortex and significantly higher potassium levels; the sodium content remained at normal levels. The kinetic constants (K
d andB
max) of [3H]domperidone binding sites measured in the striatum did not show any deviation from control values, but the receptor concentration (B
max) of [3H]ketanserin binding sites was significantly reduced in the cerebral cortex of lithium-treated rats. The apparent dissociation constant (K
d) was not changed. The results indicate that the serotonergic component of the [3H]spiperone binding site, which we had previously found to be affected by chronic lithium treatment and which was shown by Peroutka and Snyder (1) to be the 5-HT2 receptor, is selectively affected by lithium.Special Issue dedicated to Prof. Eduardo De Robertis. 相似文献
14.
Kulczykowska E Kalamarz H Warne JM Balment RJ 《Journal of comparative physiology. B, Biochemical, systemic, and environmental physiology》2006,176(4):277-285
Some of melatonin’s (Mel) well-established physiological effects are mediated via high-affinity cell-membrane receptors belonging
to the superfamily of G-protein-coupled receptors. Specific binding of ligand 2-[125I]iodomelatonin, using membrane preparations from osmoregulatory tissues of flounder, rainbow trout and sea bream, together
with Mel concentrations in the tissues and plasma were studied. The kidney, gill and small intestine samples were collected
during the day and at night. The dissociation constants (K
d) and maximal binding densities (B
max) were calculated for each tissue at 11:00 and 23:00 h. The binding sites with K
d values in the tissues in the picomolar range indicated the high affinity. K
d and B
max values were tissue- and species-dependent. The GTP analogue [Guanosine 5′-O-(3-thiotriphosphate)] treatment significantly reduced the B
max value, indicating that the 2-[125I]iodomelatonin-binding sites are probably coupled to a G-protein. No daily variations in K
d and B
max values were observed. These are the first studies of the presence of 2-[125I]iodomelatonin-binding sites in the small intestine, kidney tubule and gill of fish. The data strongly suggest new potential
targets for Mel action and the influence of Mel on water/ion balance in fish. The intestine seems to be a site of Mel synthesis
and/or an active accumulation of the hormone. 相似文献
15.
The binding of [3H]serotonin ([3H]5-HT) to cerebral cortex from young and old adult humans was studied. With cortex from human males 23–29 years old, the binding of [3H]5-HT was a saturable process, and bound [3H]5-HT could be displaced by unlabeled 5-HT or by lysergic acid diethylamide (LSD). Two separate binding sites were discernible by Scatchard analysis. The dissociation constants were 7 nM (Kd1) and 52 nM (Kd2), and the total number of binding sites were 0.65 (n1) and 2.06 (n2) pmoles/mg protein, respectively. In cerebral cortex from aged humans (61–70 years old), the dissociation constant for [3H]5-HT binding was 198 nM, and the total number of binding sites were 4.78 pmoles/mg protein. The alteration of serotonin binding sites may be related to cerebral malfunction in old people, particularly to mental depression and sleep disturbances that commonly occur. 相似文献
16.
《Life sciences》1995,58(5):PL81-PL86
Thieno-triazolodiazepines WEB 2086 and BN 50739 have been described as the potent PAF receptor antagonists. Binding of radiolabeled [3H]WEB 2086 has been widely employed to characterize PAF receptors in different cells. In a search for a PAF receptor in isolated rat hepatocytes, we discovered that the binding of [3H]WEB to rat hepatocytes was highly specific but had a relatively low affinity with a Kd of 113 nM and Bmax of 0.65 pmol/106 cells in freshly isolated cell suspension and Kd of 1.65 μM and Bmax of 2.0 pmol/plate in cultured hepatocytes. No consistent specific binding of [3H]PAF itself was found in the same cell preparations. The binding of [3H]flunitrazepam in the presence of the peripheral type of benzodiazepine receptor antagonist Ro 5-4864 was saturated and exhibited a Ki of 3.8 nM and Bmax of 3.5 pmol/plate. The central type of benzodiazepine receptor antagonist clonazepam also competed for the [3H]flunitrazepam binding, however with a much lower affinity. Various antagonists inhibited the binding of [3H]WEB 2086 with a rank order BN 50739⪢Ro 5-4864≥clonazepam. Interestingly, bicuculline, a specific antagonist of GABA(A) recognition sites, also significantly reduced the binding of [3H]WEB 2086. The binding of [3H]flunitrazepam was inhibited with a rank potency BN 50739⪢WEB 2086. Taken together, these findings suggest that the specific binding of PAF receptor antagonists WEB 2086 and BN 50739 in rat hepatocytes does not involve PAF receptors and occurs via peripheral benzodiazepine and, possibly GABA(A) receptor sites. 相似文献
17.
Abd-Elfattah Anwar-Saad A. Hoehner Jeff Wechsler Andrew S. 《Molecular and cellular biochemistry》1998,180(1-2):105-110
The role of nucleoside transport in ischemia-reperfusion injury and arrhythmias has been well documented in various animal models using selective blockers. However, clinical application of nucleoside transport inhibitors remains to be demonstrated in humans. It is not known whether human heart has nucleoside transport similar to that of animals. The aim of this study is to pharmacologically identify the presence of nucleoside transport binding sites in the human myocardium compared to animals.Myocardial tissue was obtained from guinea pig left and right ventricle, canine left ventricle, human intraoperative right atrium and human cadaveric right atrium and right and left ventricles. Myocardial preparations were obtained from tissue samples after homogenized and a differential centrifugation.Equilibrium binding assays were performed using [3H]-p-nitrobenzylthioinosine (NBMPR) at room temperature in the presence or absence of non-radioactive NBMPR or other nucleoside transport blockers such as p-nitrobenzylthioguanosine dipyridamole, lidoflazine, papaverin, adenosine and doxorubcine. From saturation curves and inhibition kinetics, we determined the relative maximal binding (Bmax) and dissociation constant (Kd) of [3H]-NBMPR binding of human myocardial preparations.Results demonstrated that the fresh human myocardial preparations have a specific binding site for NBMPR with a Bmax of 283 ± 32 fmol/mg protein and Kd of 0.56 ± 0.12 nM. These values are lower than those obtained from guinea pigs (Bmax = 1440 ± 187 fmol/mg protein and Kd = 0.21 ± 0.03 nM) and canine atrium (Bmax 594 ± 73 fmol/mg protein, and Kd = 1.12 ± 0.22 nM).Displacement kinetics studies revealed the relative potencies (of certain unrelated drugs as follow: p-nitrobenzylthioguanosine > dipyridamole > lidoflazine > pavaverine > Diltazam > adenosine > doxyrubicin. It is concluded that human myocardium contains an active nucleoside transport site which may play a crucial role in post-ischemic reperfusion-mediated injury in a wide spectrum of ischemic syndromes. 相似文献
18.
ObjectivesTo estimate the effect of pharmacotherapy on PTSD, anxiety, and depression among combat veterans; to determine whether the effects varied according to patient and intervention characteristics; and to examine differential effects of pharmacotherapy on outcomes.ResultsPharmacotherapy significantly reduced (Δ, 95%CI) PTSD (0.38, 0.23-0.52), anxiety (0.42, 0.30-0.54), and depressive symptoms (0.52, 0.35-0.70). The effects of SSRIs and tricyclic antidepressants on PTSD were greater than other medications independent of treatment duration. The effect of SSRIs and tricyclic antidepressants were greater than other medications up to 5.2 and 13.6 weeks for anxiety and depression, respectively. The magnitude of the effect of pharmacotherapy on concurrently-measured PTSD, anxiety, and depression did not significantly differ.ConclusionsPharmacotherapy reduced PTSD, anxiety, and depressive symptoms in combat veterans. The effects of SSRIs and tricyclic antidepressants were greater for PTSD and occurred quicker for anxiety and depression than other medications. 相似文献
19.
Jacqueline M. Skeer David B. Sattelle 《Archives of insect biochemistry and physiology》1993,23(3):111-124
This study has identified specific, stereoselective phenylalkylamine (PAA, (±)- [3H]verapamil) binding sites of low-affinity and high-density in cockroach (Periplaneta americana) nervous system and skeletal muscle membranes. Scatchard transformation of equilibrium binding data revealed a single population of binding sites in both tissues with dissociation constants (Kd) of 273 nM and 377 nM and binding capacities (Bmax) of 23 pmol·mg protein?1 and 37pmol·mg protein?1 for cockroach nervous tissue and skeletal muscle membranes, respectively. The PAA binding site in cockroach nervous tissue membranes was found to be dihydropyridine (DHP)-insensitive, whereas the corresponding site in cockroach skeletal muscle membranes was DHP-sensitive. This property of a DHP-sensitive PAA receptor distinguishes the binding sites identified in cockroach skeletal muscle from those in cockroach nervous tissue and indicates that pharmacologically distinct putative Ca2+ channel subtypes are present in insect nerve and muscle. © 1993 Wiley-Liss, Inc. 相似文献
20.
Kinya Kuriyama Etsuo Kurihara Yoshihisa Ito Yukio Yoneda 《Journal of neurochemistry》1980,35(2):343-348
The effect of intrastriatal microinjection of kainic acid (KA) on specific binding of [3H]muscimol to the particulate fractions obtained from corpus striatum (CS), globus pallidus (GP), substantia nigra (SN), and cerebral cortex (CC) was examined. Seven days after the unilateral intrastriatal microinjection of KA, the amount of specifically bound [3H]muscimol was significantly increased at the injected site, whereas no significant alteration of [3H]muscimol binding was found in GP, SN, or CC. Scatchard analysis of striatal binding revealed that microinjection of KA significantly increased the affinity (KD) of GABA receptors on the injected (lesioned) side of the CS without affecting the total number of binding sites (Bmax) therein. This significant increase in [3H]muscimol binding, however, was eliminated by pretreating particulate fractions from the CS with Triton X-100, a non-ionic detergent. No statistically significant difference in amounts of [3H]muscimol binding was detected when the preparations from the KA-treated and non-treated CS were preincubated with 0.05% Triton X-100, respectively. Scatchard analysis using CS preparations treated with 0.05% Triton X-100 revealed that the affinity of the GABA receptor was increased by treatment with Triton X-100, while the total number of binding sites (Bmax) was unchanged by this treatment. These results suggest that neuronal degeneration produced by KA in vivo and pretreatment of particulate preparations with Triton X-100 in vitro may increase the amount of specifically bound [3H]muscimol to CS preparations by a similar molecular mechanism. 相似文献