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Biomedical subjects

M Bienert

Publications and source records attributed to M Bienert.

At least 91 records · Page 5Linked to original sources
PubMed1983

Modulation of locomotor activity by substance P in rats.

The effects of intraperitoneally or intracerebrally (DA A-10 area) administered substance P (SP) on locomotor activity of rats were studied in an exact 12-h light/12-h dark cycle changing from dark to light at 6 a.m. SP was administered either at 11 a.m. (light phase, minimal locomotor activity) or at 7 p.m. (dark phase, maximal locomotor activity). The effects of 12.5 micrograms/kg SP intracerebral and 125 micrograms/kg SP intraperitoneal were very similar. In the light phase SP produces excitation but inhibition of locomotion in darkness. Hence, the effect of SP depends on the internal mechanisms controlling motor activity and tends to level off the spontaneous circadian oscillation. We found a long lasting SP effect during both the light and dark period. The present experiments led us to the conclusion that SP has a levelling effect on locomotor activity. Probably this effect might be explained as SP's action on the dopaminergic pathway or dopamine metabolism, because the dopamine content in neurons also has a circadian rhythm.

Animals↗
PubMed1983

Some observations indicating a low brain uptake of [3H]Nle11-Substance P.

The studies concerning the problem of whether an exogenous neuropeptide is able to enter the brain tissue were extended to the undecapeptide Substance P (SP). The amount of radioactivity 15 s after intracarotid injection of [3H] Nle11-SP or [14C] inulin was determined in 18 brain regions and the anterior pituitary of male rats. As compared to the reference [14C] inulin (mean +/- SD: 0.143 +/- 0.009% of the injected radioactivity per g tissue wet weight), the amount of radioactivity was higher after [3H]Nle11-SP injection (0.233 +/- 0.039%, p less than 0.001). Statistically significant differences could be found particularly in cortical and caudal areas as well as in the circumventricular organs studied. These observations do not refute the assumption that a low brain uptake of the labelled neuropeptide occurred due to an accumulation within structures of the blood-brain barrier and/or a penetration of the barrier system.

Animals↗
PubMed1982

Protection of methionine in peptides during iodination by sulfonium salt formation.

A method for the prevention of methionine oxidation during iodination of tyrosine containing peptides is reported. The methionine containing peptide is converted into the corresponding S-tert.-butylsulfonium derivative, which is iodinated using iodine monochloride. After removal of the S-tert.-butyl group and purification, sulfoxide-free 3,5 diiodotyrosine (Dit) peptides were obtained. Dit8-substance P, Dit8-physalaemin 6-11 and Dit1, Met5-enkephalin were synthesized by this route. Tritium labeling of Dit1, Met5-enkephalin yielded 3H-enkephalin with a specific radioactivity of 38 Ci/mmol.

Enkephalin, Methionine↗
PubMed1982

[On the role of substance P in thermoregulation of normotensive and spontaneously hypertensive rats (author's transl)].

Various peptides have been shown to alter body temperature. Intraperitoneal administration of substance P (SP) in doses of 25 and 250 micrograms/kg produces a significant hypothermic response in normotensive rats under cold exposure at 4 degrees C, whereas a dose of 2.5 micrograms/kg causes an increase in body temperature. Pretreatment with naloxone (4 mg/kg, 30 min before SP) suppresses the hypothermic effect. In spontaneously hypertensive rats (SHR), however, SP does not alter the body temperature. This result points to an altered thermoregulation in SHR based on changes in endorphin systems.

Animals↗
PubMed1981

Tritium labeling of gonadotropin releasing hormone in its proline and histidine residues.

3,4-dehydroproline9-GnRH prepared by solid phase peptide synthesis was tritiated catalytically under various conditions yielding 3H-GnRH with specific radioactivities in the range from 35-60 Ci/mmol and full LH releasing activity in vitro. Using palladium/alumina catalyst, the tritiation of the double bond occurs within ten minutes. Investigation of the tritium distribution between the amino acid residues showed a remarkably high incorporation of tritium into the histidine residue (11 to 37%). On the basis of this observation, the tritium labeling of GnRH and angiotensin I by direct catalytic hydrogen-tritium exchange was found to be useful for the labeling of these peptides at remarkably high specific radioactivity.

Aluminum Oxide↗
PubMed1980

Circular dichroism studies of substance P and its C-terminal sequences. CD spectra in aqueous solution and effects of hydrogen ion concentration.

CD spectra of substance P (SP) and its C-terminal partial sequences have been measured in diluted aqueous solution including variation of hydrogen ion concentration. In the far u.v. region there is an overlapping of the amide CD absorption by the CD of the phenylalanine residue aromatic side chains (217-220 nm). This complex CD absorption is reduced during changes from acidic to alkaline pH, especially in those cases where a phenylalanine residue is at the N-terminus of the peptide chain. These CD changes dependent on pH are due more to charge effects on the aromatic chromophores than to substantial conformational changes. However, solvation effects on the conformational features of SP peptides caused by the deprotonation of the amino groups have to be taken into account. CD and potentiometric titrations indicate that the N-terminal alpha-amino groups of the SP peptides in general are freely accessible to the solvent. Our studies did not give any evidence of the occurrence of ordered structures of SP peptides in diluted aqueous solution.

Amino Acid Sequence↗
PubMed1978

Effect of substance P on mechanical and myoelectrical activities of stomach and small intestines in conscious dog.

The effect of Substance P (SP) on the intestine in situ of the dog was investigated. Five female dogs were used. At the same time, mechanographic recordings, using balloon kymography, were taken, while the myoelectric activity was recorded by means of electrography. Differences in SP action on the mechanogram and electromyogram of the stomach and the small intestines were reflected in the following phenomena: (a) SP in the doses used was less active on the ileum than on the stomach; (b) SP increased basal tonus but inhibited peristaltic contraction; (c) SP acted predominantly on spike discharges in the electromyogram. These results are likely to support the assumption that SP acts as a physiological modulator of smooth muscle activity.

Animals↗
PubMed1977

[Inhibition of 3-H-noradrenalin uptake in synaptosomes by substance P].

The uptake kinetics of DL-[3H]-norepinephrine into synaptosomes from rat brain hypothalamus can be described as a two stage process with uptake constants of Km = 0.9 micron and Km = 0.06 micron, respectively. Substance P exerts an inhibiting influence on both uptakes. The possible importance of this inhibition for the regulation of noradrenergic transmission is discussed.

Animals↗
PubMed1975

[Studies on the mechanism of action of peptide attacking smooth muscle. II. Differentiation of biologic activity of tachykinins in affinity and intrinsic efficacy].

Under the condition of receptor blockade produced by continuous presence of an agonist in the organ bath, it was attempted to determine the dissociation constants for C-terminal partial sequences of the substance P at an isolated guinea pig ileum, by analogy with the method involving irreversible antagonists, and to compare them with the biological activity at the guinea pig ileum and the rat colon (ED50 values). Differentiation of the biological activity at the guinea pig ileum into affinity and "intrinsic efficacy" allows one to explain quantitative differences in determining the biological value on both isolated organs, and to reveal the contribution of the individual amino acids to affinity and "intrinsic efficacy".

Amino Acids↗
PubMed1975

[Studies on the mechanism of action of peptides attacking smooth muscles. III. The effect of N-azylation on the activity of C-terminal partial sequences of eledoisin, physalaemin and substance P on the guinea pig ileum].

C-terminal pentapeptides of eledoisin, physalaemin, and the substance P, when N-substituted with acetyl, halogenacetyl and other acyl residues, are increased in their action more than 100fold, reaching the activity of acylated hexa- and heptapeptides. The effect found with a number of compounds is interpreted as the influence of predominantly hydrophobic substituents upon the peptide sequence essential for the action. Polar groups in the acylic residue seem to cause additional increase in action.

Animals↗