Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0011570 (depression)
 172,036 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

1 The positive inotropic and chronotropic responses to sympathomimetic amines were examined in guinea-pig isolated atria. 2 The order of potency measured from EC50 values was isoprenaline greater than orciprenaline greater than salbutamol greater than or equal to fenoterol greater than terbutaline. Terbutaline and salbutamol were partial agonists on rate and together with orciprenaline and fenoterol also on tension responses. 3 Functional antagonism by carbachol caused a rightwards shift of the dose-response curve and depression of the maximum response. The rate maxima for orciprenaline, fenoterol and terbutaline were above that of isoprenaline. All the tension maxima were below isoprenaline. 4 Dissociation constants (KA) and relative efficacies (er) were determined by analogy with irreversible antagonism. 5 The relative orders of affinity (KA) were isoprenaline greater than orciprenaline greater than fenoterol greater than salbutamol greater than terbutaline. Affinities were identical on rate and tension. 6 The relative efficacies were all greater than isoprenaline for rate responses. On tension they were the same or less than isoprenaline. 7 The implications of these results are discussed, in particular the fact that a partial agonist has a greater efficacy than a full agonist.
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PMID:Functional antagonism as a means of determining dissociation constants and relative efficacies of sympathomimetic amines in guinea-pig isolated atria. 52 9

Dissociation constants and receptor reserves for histamine acting at H2 receptors in guinea-pig right atria and papillary muscles were measured using the irreversible H2 receptor antagonist L-643,441. Histamine alone was less potent in papillary muscles than in right atria, and maximum responses of papillary muscles to histamine were more susceptible to depression by L-643,441 than were maximum responses of right atria. However, dissociation constants (-log KA values) for histamine calculated using 3 different doses of L-643,441 were 0.5 log unit greater in papillary muscles than in right atria. A more marked difference was found in the estimates of receptor reserve for histamine, which appeared to be much greater in right atria than papillary muscles.
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PMID:Irreversible antagonism of histamine H2 receptors in guinea-pig myocardium. 287 36

[3H]-Imipramine and [3H]-paroxetine label with high affinity a recognition site which is associated with the serotonergic transporter in blood platelets. The pharmacological profile of [3H]-imipramine and [3H]-paroxetine binding is highly correlated with the potency of drugs to inhibit the uptake of serotonin. Dissociation kinetic experiments suggest that the substrate recognition site for serotonin may be different from the modulatory site which is labeled with [3H]-imipramine or [3H]-paroxetine. The existence of an endocoid acting on the imipramine receptor to modulate the serotonin transporter has been proposed by several laboratories. In clinical studies most laboratories have reported a decrease in Bmax of [3H]-imipramine binding in platelets from depressed untreated patients when compared with matched healthy volunteers. The Bmax of [3H]-imipramine binding in platelets appears to be a state-dependent biological marker in depression.
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PMID:Studies on the serotonin transporter in platelets. 296 77

[3H]-Imipramine and [3H]-paroxetine label with high affinity a site which is associated with the serotonergic transporter in brain and platelets. The pharmacological profile of inhibition by drugs of [3H]-imipramine and [3H]-paroxetine binding is highly correlated with the potency of the drugs to inhibit the uptake of 5HT. Denervation of serotonergic neurons by electrolytic lesions or with 5,7-dihydroxytryptamine produces marked decreases in the density of [3H]-imipramine as well as [3H]-paroxetine binding. Dissociation kinetic experiments support the view that the substrate recognition site for 5HT is different from the modulatory site which is labelled by [3H]-imipramine or [3H]-paroxetine. The existence of an endogenous ligand acting on the [3H]-imipramine recognition site to modulate the 5HT transporter was proposed by several laboratories. [3H]-Imipramine binding in platelets appears to be a biological marker in depression. Studies carried out in several laboratories report a significant decrease in the Bmax of platelet [3H]-imipramine binding without changes in Kd, when severely depressed untreated patients are compared with healthy volunteers matched for age and sex. The Bmax of platelet [3H]-imipramine binding appears to be a state-dependent biological marker in depression. It is tempting to speculate that the endocoid of the [3H]-imipramine recognition site may play a role in the pathogenesis of depression.
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PMID:Association of [3H]-imipramine and [3H]-paroxetine binding with the 5HT transporter in brain and platelets: relevance to studies in depression. 304 Sep 83

1. Dissociation constant (KA) of isoprenaline and orciprenaline were determined for the positive inotropic and chronotropic responses of guinea-pig isolated atria. Cumulative dose-response curves to the agonists were constructed before and after incubation with and washout of the irreversible beta-adrenoreceptor antagonist, Ro 03-7894 1-(5-chloracetylaminobenzfuran-2-yl)-2-isopropylaminoethanol). 2. After 20 min washout, the curves were displaced to the right with depression of the maxima. After 3 h washout, there was only depression of the maxima. 3. Dissociation constants were determined by plotting reciprocals of molar concentrations before Ro 03-7894 (1/A) against reciprocals of the equiactive concentrations after Ro 03-7894 (1/A'). KA = (slope - 1)/ intercept. 4. Isoprenaline had a greater affinity (KA) than orciprenaline on both rate and tension. The affinity for rate and tension was identical for both agonists, indicating that the beta-adrenoceptors were identical. 5. Isoprenaline and orciprenaline produced identical rate response maxima when compared in the same preparation but the orciprenaline tension maximum was only 92.0 +/- 0.3% that of isoprenaline. 6. These dose-response curves were replotted as response against -log RA/Rt (fraction of receptors occupied) for each agonist concentration, calculated from the equation RA/Rt = (A)/(KA + (A)). The antilogarithm of the distance along the -log RA/Rt axis gave the efficacy of orciprenaline relative to isoprenaline. It had a greater efficacy (2.24) for rate but a lower efficacy for tension responses (0.5).
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PMID:Dissociation constants of isoprenaline and orciprenaline and their relative efficacies on guinea-pig isolated atria determined by use of an irreversible beta-adrenoceptor antagonist. 611 9

Hypothermia increases the sensitivity of isolated cardiac muscle to stimulation by beta-adrenoceptor agonists. The purpose of this study was to determine pharmacologically whether this supersensitivity is associated with a change in the affinity of agonists for the receptor. The positive inotropic and chronotropic responses of guinea-pig paced left and spontaneously beating right atria were recorded. Cumulative dose--response curves to noradrenaline (or adrenaline) were compared with isoproterenol in each tissue. At 38 degrees C, the rate curves were to the left of the tension curves, with lower mean effective concentration (EC50) values. However, this difference was less for noradrenaline and adrenaline which were therefore tension selective relative to isoproterenol. Lowering the temperature to 25 degrees C induced supersensitivity, all dose--response curves being displaced to the left. In the presence of carbachol the curves were shifted to the right with depression of the maxima. Dissociation constants (KA) were calculated from plots of reciprocals of equiactive concentrations obtained before and in the presence of carbachol. KA values for rate and tension responses of each agonist were identical at 38 degrees C, indicating that the rate selectivity was not due to affinity differences. The efficacies (er) of noradrenaline and adrenaline were greater than isoproterenol for tension, but smaller for rate responses, which may explain their relative tension selectivity. At 25 degrees C, the KA values of all agonists were reduced approximately 10-fold. Hypothermia-induced supersensitivity is therefore associated with an increase in affinity for the cardiac beta-adrenoceptor.
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PMID:Dissociation constants (KA) and relative efficacies of sympathomimetic amines in isolated atria during hypothermia-induced supersensitivity. 688 10

A total of 388 patients from 10 Belgian and French Centers were evaluated with the 1981 revision of the psychopathological and somatic scales of the AMDP System. Principal components factor analyses indicate that the somatic items contribute little to the structure. A 10-factors solution of the psychopathological items generate the following factors after orthogonal rotation: Obsessions-Phobias, Dramatization, Anxiety, Depression, Retardation, Organicity, Dissociation, Delusions, Mania, Dysphoria. This structure is similar to the analyses of the previous German edition except for Anxiety (due to additional French items) and Dramatization (which replaces the German factor on Hypochondriasis). The correlations between raw factor scores and item scores of the BPRS and of a similar AMDP-derived scale contribute to the validation of the AMDP factors and to the justification of a 13-item AMDP Syndromic Scale.
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PMID:[Factor analysis of the French revision of the AMDP rating scales. Results of an international study of 388 cases]. 716 60

Nociceptive flexion reflexes (RIII response) of the lower limbs were recorded after unilateral cervico-thoracic anterolateral cordotomy (ALC) in 7 patients. Pre-operative recordings were also obtained in 1 patient and follow-up observations in 3 patients. Flexion reflexes ipsilateral to cordotomy remained normal after surgery. Conversely, responses contralateral to the cordotomy exhibited two consistent postoperative changes: first, the RIII reflex was always dissociated from subjective pain, i.e., it appeared in the absence of any pain sensation, and, second, the RIII was depressed in the limb contralateral to ALC in 5 of 7 patients. RIII attenuation ranged from slight reduction to total abolition, and proved to be reversible in 2 of 3 patients tested during the follow-up. The reappearance of withdrawal reflexes was never accompanied by a recovery of pain sensation in the stimulated limb. We conclude that the dissociation between flexion reflexes and pain sensation, which was evidenced even in case of depressed RIII responses, should be attributable to the surgical lesion of spinothalamic fibers. Dissociation between RIII and subjective pain is a landmark indicating a lesion of the spinothalamic fibers, and may be used for the clinical assessment of spinothalamic dysfunction. Conversely, RIII depression after ALC does not depend upon the surgical lesion to the spinothalamic axons, but may be secondary to interruption of ascending spinoreticular fibers in the anterolateral quadrant, and/or of descending excitatory axons in the ventral cord.
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PMID:Flexion reflexes following anterolateral cordotomy in man: dissociation between pain sensation and nociceptive reflex RIII. 830 5

The outcome of abuse-focused treatment was examined in a sample of 105 sexually abused children, 71 of whom completed 3 months of treatment or longer. Symptom change was measured with the Trauma Symptom Checklist for Children (TSCC; Briere, in press) and the Children's Depression Inventory (CDI; Kovacs, 1983, 1992), administered at 3 month intervals. The CDI and all TSCC scales but Sexual Concerns decreased after 3 months of therapy, and of these, all but Dissociation continued to decline at one or more assessment periods thereafter. At 6 months, those remaining in therapy continued to decrease on the CDI and on the Anxiety, Depression, Post-traumatic Stress, and Sexual Concerns scales of the TSCC. At 9 months Anxiety and Post-traumatic Stress continued to decrease, and at 1 year those still in treatment showed decrements in Anxiety, Depression, and Post-traumatic Stress. These changes are hypothesized to be due to treatment per se, rather than merely as a result of the passage of time. In this regard, multiple regression analyses indicated that time from the end of abuse to either the beginning or the end of treatment was far less predictive of post-treatment TSCC or CDI scores than was number of months specifically spent in treatment.
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PMID:Outcome of therapy for sexually abused children: a repeated measures study. 852 20

This study examined the construct validity of the Trauma Symptom Checklist-40 (TSC-40; Elliot & Briere, 1992) in a sample of 130 female psychiatric inpatients. Consistent with other findings, the TSC-40 displayed criterion-related validity in relation to childhood sexual abuse. Survivors of sexual abuse obtained significantly higher scores than those without such a history on the overall TSC-40 and on each of the six subscales, except the Depression subscale. Convergent validity of three subscales was demonstrated, and divergent validity on the total TSC-40 and each of its subscales was established. Further, among a range of abuse-effects measures, the Sexual Abuse Trauma Index (SATI) subscale was the most powerful predictor of sexual abuse. The SATI and Dissociation subscales were the subscales most sensitive to the specific features of the sexual abuse.
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PMID:The validation of the Trauma Symptom Checklist-40 (TSC-40) in a sample of inpatients. 880 May 25


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