Search PubMed⌕ Search

Biomedical subjects

H Kruse

Publications and source records attributed to H Kruse.

At least 55 records · Page 3Linked to original sources
PubMed1987

Resolution, absolute stereochemistry, and enantioselective activity of nomifensine and hexahydro-1H-indeno[1,2-b]pyridines.

Nomifensine and three selected compounds from the series of H4a,H5-trans,H4a,H9b-cis-2,3,4,4a,5,9b-hexahydro-1H-in deno[1,2-b]pyridines have been resolved into their enantiomers. All compounds exhibit pronounced enantioselective activity with respect to their inhibition of tetrabenazine-induced ptosis and potentiation of yohimbine toxicity. Nomifensine exhibits the same preference for one enantiomer with respect to dopamine and norepinephrine reuptake, whereas in the indeno[1,2-b]pyridine series in vitro experiments do not discriminate between the optical antipodes. The absolute stereochemistry of the pharmacologically active enantiomers in both series was determined by X-ray analyses and comparative CD spectra. For biological activity the diphenylmethane is an essential structure feature in both series. Its absolute configuration proved to be 4S for nomifensine and 5S for indenopyridines. The similar pharmacological profile of the two chemical entities is therefore reflected in an identical configuration of this pharmacologically important molecular part.

Animals↗
PubMed1985

Organochlorines and mercury in blood of a fish-eating population at the River Elbe in Schleswig-Holstein, FRG.

The blood of people living near the River Elbe who eat contaminated fish from the river was checked for organochlorines (n = 136): Hexachlorobenzene, HCB, the Hexachlorocyclohexanes beta-HCH, gamma-HCH, Octachlorostyrene, OCS, p,p-DDE and Mercury, Hg (n = 43). The concentrations (ng/ml blood) of OCS (less than 0.5-9.2) and Hg (1.1-79.2) can be attributed to fish consumption, those of the organochlorines--exept gamma-HCH--are related to age.

Age Factors↗
PubMed1983

[Discrepancy between the clinical and immunologic picture of in vitro diagnosis during transfer factor therapy in a patient with Wiscott-Aldrich syndrome].

The attempt of an interval treatment in a patient affected with Wiscott-Aldrich syndrome with transfer factor between the 6th and 14th month of life had good clinical success initially which coincided with the normalization of in vitro stimulation of the patient's lymphocytes. Only short-term (in vitro) measurable effects could be achieved by the transfer factor. Whereas clinical therapy effects were diminishing from treatment phase to treatment phase, it was possible to observe further positive results in paraclinical findings. It was only MLC reactivity that correlated with the clinical picture. Etiologically, all findings gained speak in favour of a helper cell defect and/or monocyte defect. TF therapy was not repeated because of the findings obtained and the clinical course.

Child, Preschool↗
PubMed1982

(+/-)-4-Aryl-4,5-dihydro-3H-1,3-benzodiazepines. 1. Synthesis and evaluation of (+/-)-4,5-dihydro-2,3-dimethyl-4-phenyl-3H-1,3-benzodiazepine and analogues as potential antidepressant agents.

A series of (+/-)-4,5-dihydro-4-phenyl-3H-1,3-benzodiazepines and (+/-)-4,5-dihydro-4-phenyl-1H-1,3-benzodiazepines was synthesized as part of a program to develop novel psychotropics. Of these compounds, (+/-)-4,5-dihydro-2,3-dimethyl-4-phenyl-3H-1,3-benzodiazepine (10a, HRP 543) emerged as a potential antidepressant. In in vivo mouse tests (inhibition of tetrabenazine-induced ptosis and potentiation of yohimbine toxicity) which are predictive of antidepressant-like activity, 10a is comparable to amitriptyline. The similarity is also maintained in vitro, as both 10a and amitriptyline inhibit norepinephrine and serotonin uptake into rat brain synaptosomes. No significant inhibition of rat brain monoamine oxidase A or B was found with 10a, nor did the compound potentiate tryptamine-induced seizures. On chronic administration, the number of cortical beta-adrenergic receptor sites was similarly reduced by 10a and desipramine. The anticholinergic activity of clinically useful antidepressants, such as amitriptyline, is a proposed cause of side effects which reduce patient compliance. In contrast to the tricyclics, 10a apparently lacks anticholinergic activity, as evidenced in vitro by negligible displacement of [3H]quinuclidinyl benzylate from rat brain muscarinic receptors and in vivo by insignificant antagonism of the cholinergic stimulation produced by physostigmine or oxotremorine. These data suggest that 10a may be clinically useful as a novel nontricyclic antidepressant which is devoid of anticholinergic side-effect liability. Further evaluation of 10a in nonrodent species is in progress.

Aggression↗
PubMed1982

Thyroliberin (thyrotropin releasing hormone): antagonism of halothane and hexobarbital narcosis in mice. Comparison with pentetrazol, caffeine, d-amphetamine and adrenaline.

The effect of L-pyroglutamyl-L-histidyl-L-prolinamide (thyroliberin, thyrotropin releasing hormone, TRH) on halothane and hexobarbital narcosis was investigated in mice and compared with pentetrazol, caffeine, d-amphetamine and adrenaline. TRH shortened dose-dependently the halothane and hexobarbital sleeping-time with ED50 values of 3.1 and 6.6 mg/kg s.c., respectively. The analeptic effect of TRH was superior to all reference compounds in terms of potency, efficacy and drug safety. Due to its ergotropic activity TRH may be a useful aid in anaesthesiology and intensive care.

Animals↗
PubMed1982

Immunologic parameters of children with acute leucosis after cessation of polychemotherapy under repeated immunostimulation with intradermal B.C.G.

11 children with acute leucosis (10 with ALL, 1 with AML) showed a significant increase of the absolute number of lymphocytes and E-rosette forming cells in the peripheral blood after 3-years-polychemotherapy under repeated intradermal B.C.G. vaccination. Such an increase of the absolute number of lymphocytes could not be found in an analogous control group without immunostimulation. At present 14 children with acute leucosis (11 with ALL, 3 with AML) in our hematologic-oncologic primary center of Rostock are still living in a first stable remission from the first up to the third year under regular immunostimulation with intradermal B.C.G. when polychemotherapy off.

Antineoplastic Agents↗