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1.
Animal ; 15(2): 100080, 2021 Feb.
Article in English | MEDLINE | ID: mdl-33573966

ABSTRACT

Lowland-type Racka is an indigenous sheep breed that beside Hungarian Grey cattle and Mangalitza pig is one of the national symbols of Hungary. However, the genetic description of Racka sheep has not yet been conducted based on whole-genome screening. By using the Geneseek Ovine SNP50 BeadChip, we have sampled the genome of 126 Black and 128 White Racka sheep. For comparative purposes, we used 134 Hungarian Merinos and further 3345 animals from 81 different breeds have been included from an available database. Performance of a multidimensional scaling plot showed that White and Black Rackas represent well-separated groups among other sheep breeds and clustered separately from each other. However, the number and total length of Runs of Homozygosity was similar to other sheep breeds, except Soay. The inbreeding coefficients (method-of-moments relatedness F coefficient) of Black and White Racka were 0.147 and 0.133, respectively. Based on multidimensional scaling and admixture analyses and on comparisons of genetic distances of the investigated 84 populations, we suggest considering the colour variants of Racka as genetically differentiated breeds. The most differentiated markers between Black and White Racka highlight several candidate genes including 5-Hydroxytryptamine Receptor 5A, Insulin Induced Gene 1, Cyclin Dependent Kinase 5 and Melanocortin 1 Receptor. The results of this study help the recognition of Racka as a unique genetic resource among sheep and pave the way of application of genome screens to guide the resolution of questions arising among breeders.


Subject(s)
Genetic Variation , Polymorphism, Single Nucleotide , Animals , Cattle , Color , Hungary , Sheep , Sheep, Domestic , Swine
2.
J Phys Condens Matter ; 26(21): 216003, 2014 May 28.
Article in English | MEDLINE | ID: mdl-24806308

ABSTRACT

A method is proposed to study the finite-temperature behaviour of small magnetic clusters based on solving the stochastic Landau-Lifshitz-Gilbert equations, where the effective magnetic field is calculated directly during the solution of the dynamical equations from first principles instead of relying on an effective spin Hamiltonian. Different numerical solvers are discussed in the case of a one-dimensional Heisenberg chain with nearest-neighbour interactions. We performed detailed investigations for a monatomic chain of ten Co atoms on top of a Au(0 0 1) surface. We found a spiral-like ground state of the spins due to Dzyaloshinsky-Moriya interactions, while the finite-temperature magnetic behaviour of the system was well described by a nearest-neighbour Heisenberg model including easy-axis anisotropy.


Subject(s)
Cobalt/chemistry , Gold/chemistry , Magnetics , Models, Theoretical , Anisotropy , Quantum Theory , Spin Labels , Stochastic Processes , Temperature
3.
J Phys Condens Matter ; 25(50): 506002, 2013 Dec 18.
Article in English | MEDLINE | ID: mdl-24275952

ABSTRACT

A spin model including magnetic anisotropy terms and Dzyaloshinsky-Moriya interactions is studied for the case of a ferromagnetic monolayer with C2v symmetry like Fe/W(110). Using the quasiclassical stochastic Landau-Lifshitz-Gilbert equations, the magnon spectrum of the system is derived using linear response theory. The Dzyaloshinsky-Moriya interaction leads to asymmetry in the spectrum, while the anisotropy terms induce a gap. It is shown that, in the presence of lattice defects, both the Dzyaloshinsky-Moriya interactions and the two-site anisotropy lead to a softening of the magnon energies. Two methods are developed to investigate the magnon spectrum at finite temperatures. The theoretical results are compared to atomistic spin dynamics simulations and good agreement is found between them.


Subject(s)
Magnets/chemistry , Models, Theoretical , Temperature , Anisotropy , Computer Simulation , Electric Conductivity
4.
J Parasitol ; 92(4): 867-9, 2006 Aug.
Article in English | MEDLINE | ID: mdl-16995408

ABSTRACT

Avian lice occupy different habitats in the host plumage that the physical environment outside the host body may affect in several ways. Interactions between host plumage and water may be an important source of such effects. Here, we use a comparative approach to examine the effect of a host's diving behavior on the taxonomic richness of its lice. Louse genera richness was significantly lower in clades of diving birds than on their nondiving sister clades. Species richness of host and body mass did not differ significantly between these clades; thus, these factors did not bias our results. This study suggests that the hosts' diving behavior can effectively influence ectoparasite communities.


Subject(s)
Bird Diseases/parasitology , Birds/physiology , Diving , Lice Infestations/veterinary , Phthiraptera/classification , Animals , Birds/anatomy & histology , Body Size , Diving/physiology , Feathers/parasitology , Female , Humidity , Lice Infestations/parasitology , Linear Models , Male
5.
J Parasitol ; 86(2): 228-32, 2000 Apr.
Article in English | MEDLINE | ID: mdl-10780537

ABSTRACT

Whereas terminological recommendations require authors to use mean intensity or mean abundance to quantify parasites in a sample of hosts, awkward statistical limitations also force them to use either the median or the geometric mean of these measures when making comparisons across different samples. Here, we propose to reconsider this inconsistent practice by giving priority to biological realism in the interpretation of different statistical descriptors and choosing the statistical tools appropriate to our decisions. Prevalence, mean intensity, and indices of parasite distribution (such as median intensity) are suitable descriptors to quantify parasites in a sample of hosts. These measures have different biological interpretations and need different statistical methods to be compared between samples.


Subject(s)
Parasites/growth & development , Parasitic Diseases/parasitology , Parasitology/methods , Animals , Binomial Distribution , Chi-Square Distribution , Confidence Intervals , Host-Parasite Interactions , Linear Models , Parasitic Diseases/epidemiology , Prevalence , Sample Size
6.
J Parasitol ; 85(6): 1032-5, 1999 Dec.
Article in English | MEDLINE | ID: mdl-10647033

ABSTRACT

This study introduces an individual-based model on a host-parasite assemblage to investigate whether hosts are necessarily selected for obstructing the transmission of virulent parasites to conspecifics. Contrary to the widespread notion, a host's ability to influence parasite transmission within the host population is a neutral character provided that parasite transmission routes are random, with no reference to genetic relatedness. Due to a lack of selection pressure under such circumstances, hosts may fail to evolve counteradaptations against manipulations by parasites to enhance transmission. However, vertically biased transmission (biased toward kin) selects hosts for a decrease of parasite transmission, while it is also known to select parasites to decrease virulence. Horizontally biased transmission routes (biased toward nonrelated conspecifics) select hosts to increase parasite transmission. In this case, their interests coincide with that of their virulent parasites in enhancing transmission to conspecifics. This finding yields the predictions that hosts infected by virulent pathogens, but unable to recover from disease, should be prone to emigrate from their natal territories and also to enhance transmission at a distance from their natal ranges. These results may considerably improve our understanding of the epidemiology of contagious pathogens and the evolution of social and sexual behavior in host species.


Subject(s)
Models, Biological , Parasites/pathogenicity , Parasitic Diseases/transmission , Alleles , Animals , Behavior, Animal , Computer Simulation , Disease Reservoirs , Gene Frequency , Host-Parasite Interactions , Parasites/genetics , Parasitic Diseases/parasitology , Virulence
7.
J Parasitol ; 84(3): 491-8, 1998 Jun.
Article in English | MEDLINE | ID: mdl-9645845

ABSTRACT

Site segregation of coexisting ectoparasite species may result either from a direct interaction such as resource competition between them or from a host-mediated interaction. Here we present an individual-based model for the coevolution of 1 host and 2 parasite species to study this latter hypothesis. Parasite species are generalists at the start of the simulation and develop site specificities under the following assumptions. Parasite populations are not subject to resource limitations but are limited directly by host defense as predation. Hosts have 2 sites that need different defensive abilities to reduce their parasite burden. Parasites need to exhibit different evasive abilities to survive on different sites. Host grooming selects parasites for an increasing capability for evasion, whereas parasites select hosts for an increasing efficiency of grooming. Two trade-offs are incorporated into the model: one between host defensive abilities on the 2 sites, and another between parasite evasive abilities on the 2 sites. We conclude that, under these assumptions, the optimization of host defense and parasite evasion strategies may select ectoparasites for site segregation and this may stabilize the coexistence of parasite species.


Subject(s)
Bird Diseases/parasitology , Computer Simulation , Ectoparasitic Infestations/veterinary , Models, Biological , Phthiraptera/physiology , Animals , Binomial Distribution , Bird Diseases/genetics , Bird Diseases/immunology , Birds , Ectoparasitic Infestations/immunology , Ectoparasitic Infestations/parasitology , Grooming , Host-Parasite Interactions , Phthiraptera/genetics , Phthiraptera/immunology , Selection, Genetic , Sensitivity and Specificity
8.
Stroke ; 28(12): 2479-82, 1997 Dec.
Article in English | MEDLINE | ID: mdl-9412636

ABSTRACT

BACKGROUND AND PURPOSE: Vasospasm in aneurysmal subarachnoid hemorrhage results in proliferative vasculopathy. Systemic hypertension also causes vascular hypertrophy. Both of these histological changes can lead to rigidity of the cerebrovascular system, reducing its autoregulatory capacity. METHODS: Blood flow velocity (BFV) in the middle cerebral artery at rest and cerebrovascular reserve capacity (CVRC) (percent rise in BFV after acetazolamide stimulation) measured by means of transcranial Doppler sonography were studied many years after aneurysmal subarachnoid hemorrhage in patients with proven cerebral vasospasm (mean BFV > 160 cm/s). The BFV under resting conditions and the CVRC values of the ipsilateral and the contralateral hemispheres were measured in 29 patients (mean age, 43 years; mean follow-up, 4.6 years) and compared with those of control subjects. RESULTS: Persistent high BFV (> 120 cm/s) was found in three patients in the peripheral branch of the ipsilateral middle cerebral artery. In the main trunks of the arteries of the anterior circle of Willis, BFV was normal in all cases. CVRC was normal in all patients (ipsilateral, 52 +/- 21%; contralateral, 56 +/- 17%); values did not differ significantly from each other or from the control value (45 +/- 18%). The higher value of CVRC on the contralateral side was found to be statistically significant in selected groups (hypertensive patients and patients with residual infarct on late CT). CONCLUSIONS: Proliferative vasculopathy developed at the time of vasospasm must have resolved and did not reduce late vasoreactivity. Comorbidity with hypertension also did not seem to influence the late vasoreactivity toward normalization.


Subject(s)
Cerebrovascular Circulation/physiology , Intracranial Aneurysm/complications , Ischemic Attack, Transient/etiology , Ischemic Attack, Transient/physiopathology , Subarachnoid Hemorrhage/complications , Ultrasonography, Doppler, Transcranial , Acetazolamide , Adolescent , Adult , Blood Flow Velocity/physiology , Female , Follow-Up Studies , Humans , Ischemic Attack, Transient/diagnostic imaging , Male , Middle Aged , Reference Values , Time Factors
9.
J Parasitol ; 83(3): 543-4, 1997 Jun.
Article in English | MEDLINE | ID: mdl-9194847

ABSTRACT

The sex-ratio pattern of an exceptional population of human head lice (collected in the Colombo Prison, Ceylon, in 1934 to 1936) was found to be consistent with a current hypothesis on adaptive sex-ratio manipulation. Data suggest that the louse burdens were isolated and, therefore, small burdens were inbred. Thus, local mate competition favored females that produced offspring with a female bias. This is the first report to suggest that anopluran lice are capable of adaptive sex-ratio manipulation.


Subject(s)
Lice Infestations/parasitology , Pediculus/physiology , Scalp Dermatoses/parasitology , Adaptation, Physiological , Animals , Female , Humans , Linear Models , Male , Retrospective Studies , Sex Ratio
10.
Neurosurg Rev ; 20(3): 188-95, 1997.
Article in English | MEDLINE | ID: mdl-9297721

ABSTRACT

In this retrospective study of 67 aneurysmal patients, the predictive role of central conduction time (CCT) on vasospasm occurrence evaluated by means of transcranial Doppler sonography (TCD) and the correlation of CCT to blood flow velocity measured simultaneously in postoperative course were studied. Data about the clinical state of patients at the time of admission (Hunt Hess scale), severity of subarachnoidal hemorrhage on initial CT scan (Fisher grade), timing of surgery (acute or delayed), outcome (Glasgow Outcome Scale), severity of vasospasm graded by highest mean blood flow velocity (BFV) during the entire clinical course and CCT values measured at admission (preoperatively), then postoperatively (one day after surgery) and simultaneously with later TCD investigations were collected from the files. Interhemispheric difference of CCT was also calculated. The results showed that CCT at admission was not predictive for vasospasm. CCT measured either at admission or on the first postoperative day did not differ significantly in the different grades of vasospasm. Similar results were obtained in the acute and in the late operated group of patients. The results also suggest that increased CCT and interhemispheric difference at the time of admission indicate a worse prognosis, but this can be related to higher surgical risk rather than to a higher incidence of late ischemic deterioration. Simultaneous CCT and TCD examinations demonstrated that coincident and statistically significant (p < 0.01) increase of actual CCT (6.7 msec) was found only in the severe grade of vasospasm (BFV 200 cm/s). The authors discuss the role of CCT and TCD monitoring in the management of aneurysmal subarachnoid hemorrhage.


Subject(s)
Brain Ischemia/etiology , Evoked Potentials, Somatosensory , Intracranial Aneurysm/physiopathology , Subarachnoid Hemorrhage/physiopathology , Adult , Aged , Blood Flow Velocity , Brain Ischemia/diagnostic imaging , Brain Ischemia/physiopathology , Cerebrovascular Circulation , Female , Humans , Intracranial Aneurysm/complications , Intracranial Aneurysm/diagnostic imaging , Male , Middle Aged , Retrospective Studies , Somatosensory Cortex/physiology , Subarachnoid Hemorrhage/complications , Subarachnoid Hemorrhage/diagnostic imaging , Ultrasonography
11.
Acta Vet Hung ; 45(2): 151-63, 1997.
Article in English | MEDLINE | ID: mdl-9270138

ABSTRACT

One hundred and twelve Holstein bulls (179-203 kg) were allotted to four dietary treatment groups (I: control; II: fullfat soybean diet; III: sunflower seed diet, and IV: protected fat diet) and used in a 120-day comparative feedlot trial to evaluate the effect of toasted fullfat soybean, whole sunflower seed and protected fat (calcium soap) on their weight gain, feed conversion and carcass fatty acid composition. The diets consisted of 45-46% concentrate and 55-54% corn silage. Digestibility, nutritive value as well as degradability were also determined. The apparent digestibility of dry matter, organic matter, N-free extract and crude protein as well as nutritive value were almost similar for the four diets. However, crude fibre, acid detergent fibre (ADF) and neutral detergent fibre (NDF) digestibilities decreased with increasing fat level but the differences were not significant. The inclusion of fullfat soybean or whole sunflower seed significantly (P < 0.05) increased the digestion of fat. Ruminal degradability of protein and dry matter were significantly (P < 0.01) lower for toasted fullfat soybean mixture compared to whole sunflower mixture. The inclusion of toasted fullfat soybean, whole sunflower seed and calcium soap in the diets was not effective in improving the bulls' weight gain or feed conversion in this trial. As both toasted fullfat soybean and whole sunflower seed increased the proportions of C18:1, C18:2 and C18:3 in adipose fat tissue and decreased the proportion of C16:0, they consequently significantly (P < 0.01) increased the ratio of unsaturated fatty acids. Whole sunflower seed was more effective than fullfat soybean. However, inclusion of the calcium soap had no effect on the fatty acid profiles in the present study.


Subject(s)
Body Composition/drug effects , Cattle/physiology , Dietary Fats/pharmacology , Fatty Acids/analysis , Meat/analysis , Plant Oils/pharmacology , Soybean Oil/pharmacology , Adipose Tissue/physiology , Animal Nutritional Physiological Phenomena , Animals , Body Composition/physiology , Cattle/growth & development , Cattle/metabolism , Dietary Fats/administration & dosage , Dietary Fats/metabolism , Dietary Fiber/metabolism , Dietary Proteins/metabolism , Eating/physiology , Fatty Acids/metabolism , Fermentation , Food, Fortified , Male , Plant Oils/administration & dosage , Plant Oils/metabolism , Rumen/metabolism , Rumen/physiology , Soybean Oil/administration & dosage , Soybean Oil/metabolism , Sunflower Oil , Weight Gain/physiology
12.
J Parasitol ; 79(6): 968-70, 1993 Dec.
Article in English | MEDLINE | ID: mdl-8277395

ABSTRACT

Site specificities of ectoparasites on the host may have evolved due to the selective pressure exerted by host grooming. The present study demonstrates that the efficiency of avian preening varies among sites on the host. The study relies on the simple idea that the effectiveness of preening behavior to control lice can be quantified by the removal rate of dead lice glued onto the feathers of living birds. Two treatments were done to document site-specific differences in the efficiency of preening for louse control. The first treatment showed that lice disappear from the underwing covert feathers significantly more than from the tail feathers. A second treatment showed that preening was responsible for the differential removal of lice. There seems to be some correspondence in the site specificity of the louse species Columbicola columbae and that of the efficiency of preening by the host, which is the feral pigeon (Columba livia).


Subject(s)
Bird Diseases/prevention & control , Columbidae/parasitology , Feathers/parasitology , Grooming , Lice Infestations/veterinary , Analysis of Variance , Animals , Animals, Wild , Female , Lice Infestations/prevention & control , Phthiraptera/physiology
13.
Int J Parasitol ; 23(7): 859-64, 1993 Nov.
Article in English | MEDLINE | ID: mdl-8314369

ABSTRACT

Two competing views have been expressed to explain ectoparasite speciation patterns, one emphasizing co-speciation and one emphasizing host-switching. Though recent authors preferred a combination of these views, the available phylogenetic trees cannot be interpreted without revisiting island biogeography theory. Parasite extinction due to a temporal decline in host population size seems to be a prerequisite of subsequent speciation by host-switch. The need for a re-evaluation of "stragglers" (ectoparasites found on non-specific hosts) is emphasized.


Subject(s)
Ectoparasitic Infestations/veterinary , Lice Infestations/veterinary , Phthiraptera/classification , Vertebrates/parasitology , Animals , Bird Diseases/parasitology , Birds , Ectoparasitic Infestations/parasitology , Host-Parasite Interactions , Lice Infestations/parasitology , Phylogeny , Rodent Diseases/parasitology , Rodentia
15.
Orv Hetil ; 132(50): 2785-8, 1991 Dec 15.
Article in Hungarian | MEDLINE | ID: mdl-1823100

ABSTRACT

Blood flow velocity of 24 patients in state of the brain death were examined by transcranial Doppler sonography. Authors expound the characteristic velocity-pulse graphs recorded in progressively increasing intracranial pressure and their chronology as well. The different forms of the oscillating flow and their successive development are described. The oscillating flow, the systolic spikes and the so called "zero Flow" are the transcranial Doppler signs of the ceased cerebral blood flow, and these signs can be used as one of the evidence of the brain death.


Subject(s)
Brain Death/diagnostic imaging , Cerebrovascular Disorders/diagnostic imaging , Intracranial Pressure , Adolescent , Adult , Aged , Cerebrovascular Circulation , Child , Female , Humans , Infant , Male , Middle Aged , Pseudotumor Cerebri/diagnostic imaging , Ultrasonography
16.
Acta Neurochir (Wien) ; 112(3-4): 113-7, 1991.
Article in English | MEDLINE | ID: mdl-1776512

ABSTRACT

In a total of 90 patients with intracranial hypertension and subsequent intracranial circulatory arrest, the cerebral basal arteries were examined with transcranial Doppler ultrasonography. In order to explain the development of the various forms of oscillating flow, a blood-pressure cuff was placed on the distal forearm of 25 healthy subjects to investigate the flow spectra in the proximal arteries in the presence of increasing stream resistance. With raising the pressure of the cuff, the changes in the Doppler sonographic flow spectra were simulated as in case of increasing intracranial pressure. As intracranial pressure increases at constant systemic blood pressure values, the flow velocity spectrum changes in a typical manner. At the stage of oscillating flow, characteristic changes in the flow spectra can be observed. Investigations showed that compliance is reduced in a distal to proximal direction. This means that a different frequency spectrum can be recorded in distal branches of the middle cerebral artery than in the proximal carotid artery at the same point in time. By examining the flow velocity spectra from the brachial artery, it was possible to understand better the typical course of an intracranial circulatory arrest resulting from increased stream resistance.


Subject(s)
Blood Flow Velocity , Brain Death/diagnostic imaging , Cerebral Arteries/diagnostic imaging , Cerebrovascular Circulation , Adolescent , Adult , Aged , Brachial Artery/diagnostic imaging , Child , Child, Preschool , Female , Humans , Intracranial Pressure , Male , Middle Aged , Ultrasonography , Vascular Resistance
17.
Ophthalmologica ; 200(3): 128-32, 1990.
Article in English | MEDLINE | ID: mdl-2189085

ABSTRACT

The authors report a case of Hippel's angiomatosis successfully treated with contact beta irradiation. The area of the multiplex retinal angioma and the accompanying retinal detachment was irradiated with a 106Ru/106Rh radioactive applicator. Hemodynamic changes due to irradiation were followed up in the ipsilateral ophthalmic artery with transcranial Doppler sonography. Scarring was also demonstrated by fluorescein angiography and A- and B-scan ultrasonography. Irradiation caused the narrowing and later the occlusion of the precapillaries and capillaries (i.e. the resistance vessels) and that of the shunts inside the angioma; consequently, vascular resistance increased. Transcranial Doppler sonographic recordings showed a decrease in blood flow velocity as compared to pathologically increased blood flow velocity in angiomas, and a gradual increase in vascular resistance which was lower before treatment.


Subject(s)
Angiomatosis/radiotherapy , Eye Neoplasms/radiotherapy , Hemodynamics , Retinal Diseases/radiotherapy , Ruthenium Radioisotopes/therapeutic use , von Hippel-Lindau Disease/radiotherapy , Adult , Eye Neoplasms/pathology , Eye Neoplasms/physiopathology , Female , Fluorescein Angiography , Humans , Retinal Diseases/pathology , Retinal Diseases/physiopathology , Ultrasonography , von Hippel-Lindau Disease/pathology , von Hippel-Lindau Disease/physiopathology
18.
Orv Hetil ; 130(32): 1703-6, 1989 Aug 06.
Article in Hungarian | MEDLINE | ID: mdl-2674836

ABSTRACT

The value of transcranial Doppler sonography is demonstrated in two infants with an elevation of intracranial pressure (ICP). One of them suffered from hydrocephalus and ICP increased because of her VP shunt-insufficiency. In the other case status epilepticus caused brain oedema and a rise in intracranial pressure. In both cases, transcranial Doppler sonography showed a decrease in blood flow (CBF) velocity and an increase in the Pourcelot index in the middle cerebral artery. Quick or gradual reduction of the ICP led to an increase in CBF velocity and a decrease in the Pourcelot index. On the basis of experiences of the authors, transcranial Doppler sonography is a valuable method of verifying the elevation of ICP. It is suitable for measuring the effect of treatment necessitated by the elevation of ICP. The method is non-invasive, quick and it can be freely repeated. Therefore it is applicable for monitoring the dynamic of ICP.


Subject(s)
Pseudotumor Cerebri/diagnosis , Ultrasonography , Age Factors , Humans , Infant , Infant, Newborn
19.
Orv Hetil ; 130(31): 1669-72, 1675-6, 1989 Jul 30.
Article in Hungarian | MEDLINE | ID: mdl-2771402

ABSTRACT

Transcranial Doppler Sonography. Authors publish the experiences gained by 2300 examinations with Transcranial Doppler Sonography (TDS) which is a new, noninvasive ultrasound method to examine cerebral blood flow velocity in the basal arteries. The theoretical ground and the technique of the investigation is detailed. Mean values of blood flow velocity in the middle cerebral artery of 88 healthy volunteers in different age groups are reported. Authors stress on the numerous advantages of the utilization of this technique. Different pathological alterations of blood flow velocity and characteristic types of velocity-pulse figure are accounted. At last illustrative case reports proving the importance of TDS in different pathological states are presented.


Subject(s)
Cerebrovascular Circulation , Cerebrovascular Disorders/diagnosis , Adult , Cerebral Hemorrhage/diagnosis , Cerebral Hemorrhage/etiology , Cerebrovascular Disorders/surgery , Craniocerebral Trauma/complications , Female , Hematoma, Epidural, Cranial/diagnosis , Hematoma, Epidural, Cranial/etiology , Humans , Intracranial Aneurysm/complications , Intracranial Aneurysm/diagnosis , Intracranial Aneurysm/surgery , Male , Rupture, Spontaneous , Ultrasonics
20.
Acta Biochim Biophys Hung ; 24(1-2): 129-42, 1989.
Article in English | MEDLINE | ID: mdl-2514534

ABSTRACT

A new family of tricyclic compounds, the dibenzodioxazocines were synthesized. These compounds were the following: 2-chloro-12-(2-piperidino-ethyl)-dibenzo d,g 1,3,6 dioxazocine hydrochloride: EGYT-2347, 2-chloro-12-(3-dimethylamino-2-methyl-propyl)-dibenzo [d,g] [1,3,6]-dibenzodioxazocine hydrochloride: EGYT-2509, 2-chloro-12-(3-dimethylamino-propyl)-dibenzo [d,g] [1,3,6] dioxazocine-maleate: EGYT-2474 and 2-chloro-12-2-(4-methyl-piperazino)-ethyl-dibenzo [d,g] [1,3,6]-dioxazocine-dihydrochloride: EGYT-2541. These compounds are inhibitors of both butyryl- and acetylcholinesterase to and they exhibited relatively good anticholinergic properties in receptor binding experiments. The most selective inhibitor of butyrylcholinesterase is the compound EGYT-2347 (Ki = 1.5 x 10(-7) M) which strongly binds to rat brain muscarinic cholinergic receptor (KD = 4.1 x 10(-8) M).


Subject(s)
Cholinesterase Inhibitors , Dibenzoxazepines/pharmacology , Receptors, Muscarinic/drug effects , Animals , Brain/drug effects , Brain/metabolism , Cattle , Dibenzoxazepines/chemical synthesis , Dibenzoxazepines/metabolism , Female , Guinea Pigs , Ileum/drug effects , Ileum/metabolism , In Vitro Techniques , Kinetics , Male , Rats , Receptors, Muscarinic/metabolism , Structure-Activity Relationship
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