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Biomedical subjects

E Eichenberger

Publications and source records attributed to E Eichenberger.

At least 19 recordsLinked to original sources
PubMed1984

Pharmacology of fluperlapine compared with clozapine.

3-Fluoro-6-(4-methyl-piperazinyl)- 11H -dibenz [b,e]azepine ( fluperlapine , NB 106-689) resembles clozapine qualitatively and quantitatively in that it causes sedation, muscle relaxation, anticholinergic effects, no catalepsy, has little effect on apomorphine- and amphetamine-induced behaviour, does not induce apomorphine supersensitivity, and increases dozing and spindle activity in the rat's EEG. In the striatum of rats, it binds less to dopamine (DA) D2-receptor sites, but it enhances DA-turnover more than clozapine. Like clozapine and unlike haloperidol, it is equally active in the striatum, the nucl . accumbens and the cortex. Unlike clozapine, it does not significantly enhance norepinephrine (noradrenaline, NA)- or 5-hydroxytryptamine turnover and it does not increase prolactin blood levels significantly. Of the two compounds, only fluperlapine has some effects in common with antidepressants, i.e. tetrabenazine-antagonism and NA-uptake inhibition in slices of rat brain in vitro and ex vivo.

Animals↗
PubMed1980

The pharmacology of 5-chloro-4-(2-imidazolin-2-yl-amino)-2,1,3-benzothiadiazole (DS 103-282), a novel myotonolytic agent.

5-Chloro-4-(2-imidazolin-2-yl-amino)-2,1,3-benzothiadiazole (DS 103-282) is a centrally acting agent with a novel chemical structure and a pharmacological profile different from that of myotonolytic drugs in current use such as diazepam, baclofen and dantrolene. It inhibits alpha- and gamma-rigidity in rats, reflex muscle tone in rabbits and the linguomandibular reflex in cats at low doses, but has little or no effect on gross spinal reflexes or electrically-induced segmental reflexes in cats. The mechanism underlying the muscle relaxation is unknown. Effects on convulsions induced by impaired GABA-transmission and by strychnine suggest a possible influence on glycine-mediated neurotransmission. In muscle-relaxing doses, DS 103-282 is without appreciable sedative, haemodynamic or neurochemical effects. Clinical investigations have confirmed the pharmacological predictions with regard to both the myotonolytic activity and the low propensity to produce side-effects.

Analgesics↗
PubMed1976

[The course of blood pressure and organ changes in rats with DOCA-hypertension].

In 45 control rats and 47 nephrectomized, DOCA-implanted, hypertensive rats (hypertensive phase), blood pressure, weight gain, development of pathologic-anatomical histological changes as well as changes in the myocardial enzyme pattern were studied over 24 weeks and after absorption of the DOCA tablet the return of the animals to normal conditions (follow-up phase) for another 14 weeks. During the hypertensive phase, blood pressure rose to 233 mm Hg on the average within 10 weeks and remained constant up to the 22nd week. In the follow-up phase, it dropped sharply, at first, and then slowly returned to normal. Weight gain was the same in DOCA and control rats. Relative weights of heart, kidneys and liver were elevated in the hypertensive phase but fell again in the follow-up phase. The pathologic-histological changes formed in the hypertensive phase, such as myocardial hypertrophy, glomerular hyalinization, tubular dilation and perivascular fibrosis, were remitted in part. Unchanged, however, the enhanced heart score persisted evidencing a proliferative vasoconstriction. Except for a pronounced, reversible increase in MAO activity, the cardial enzyme pattern remained unchanged during the experiment.

Animals↗
PubMed1975

Clozapine and the dopamine hypothesis of schizophrenia, a critical appraisal.

This paper discusses some of the pharmacological and neurochemical properties of clozapine, and the special attributes that differentiate clozapine from the classical neuroleptics. The question as to whether or not clozapine blocks DA-receptors--a crucial point in regard to the dopamine hypothesis of schizophrenia--has received particular attention. Neurochemical, neuropharmacological, and endocrinological evidence is presented which speaks against a DA-receptor blockade by clozapine in pharmacologically relevant doses. These findings are difficult to reconcile with the dopamine hypothesis which proposes a direct relationship between antipsychotic effect and DA-receptor blockade.

Animals↗
PubMed1975

Pharmacological actions of the antihypertensive agent N-amidino-2-(2,6-dichlorophenyl)acetamide hydrochloride (BS 100-141).

Pharmacological properties characterizing N-amidino-2-(2,6-dichlorophenyl)acetamide hydrochloride (BS 100-141) as a centrally acting antihypertensive agent are described. Its action resembles that of clonidine in many respects but with important differences which are discussed. In DOCA-NaCl--hypertensive conscious rats, BS 100-141 lowers systemic blood pressure with oral doses of 0.3-5 mg/kg. Evidence for a central site of action is provided by the following findings. Infusion of BS 100-141 into the vertebral artery of anaesthetized dogs reduces blood pressure, the same dose being ineffective by i.v. route. Injection into the lateral cerebral ventricle of anaesthetized cats causes a marked reduction in blood pressure and heart rate, the same dose being ineffective when given i.v. The effects of intraventricular injection are inhibited by phentolamine administered by the same route. Intravenous administration of BS 100-141 induces dose-dependent reductions in the splanchnic (sympathetic) nerve activity in the cat. BS 100-141 reduces noradrenaline turnover in the brain stem of the rat as a result of central alpha-adrenoceptor stimulation. Doses which are effective in the hypertensive rat do not reduce dopamine turnover in the corpus striatum. The peripheral, direct alpha-sympathomimetic action of BS 100-141 was demonstrated by the transient increases in blood pressure observed in rats. These increases were unaffected by pretreatment with reserpine, but were antagonized by phentolamine. BS 100-141 was shown to induce contractions of isolated veins and arteries which were competitively inhibited by phentolamine. It stimulates presynaptic cardiac sympathetic alpha-adrenoceptors, thus inhibiting transmitter release to the heart. The sedative effects of BS 100-141 observed in dogs were slight compared to those of clonidine.

Animals↗