The pharmacology of neurotensin analogues on neurones in the rat substantia nigra, pars compacta in vitro. 1994

K D Keegan, and G N Woodruff, and R D Pinnock
Parke-Davis Neuroscience Research Centre, Addenbrookes Hospital Site, Cambridge, UK.

The effects of neurotensin and neurotensin analogues on dopamine neurones were studied in an in vitro slice preparation of rat substantia nigra, pars compacta using extracellular and intracellular recording techniques. Neurotensin had an EC50 of 13 nM in these experiments. This study showed that the C-terminal 5 amino acids of neurorotensin in neurotensin-(9-13) retained agonist activity on substantia nigra neurones. The naturally occurring neurotensin analogues neuromedin N and avian neurotensin were also active whilst kinetensin was inactive. Kinetensin differs from the C-terminal neurotensin 5-amino acids by two amino acids. The difference between the activity of neurotensin and the inactivity of kinetensin was investigated using synthetic peptides which contained single amino acid substitutions. These results show that position 12 of neurotensin is important for agonist activity in the substantia nigra.

UI MeSH Term Description Entries
D008297 Male Males
D009474 Neurons The basic cellular units of nervous tissue. Each neuron consists of a body, an axon, and dendrites. Their purpose is to receive, conduct, and transmit impulses in the NERVOUS SYSTEM. Nerve Cells,Cell, Nerve,Cells, Nerve,Nerve Cell,Neuron
D009496 Neurotensin A biologically active tridecapeptide isolated from the hypothalamus. It has been shown to induce hypotension in the rat, to stimulate contraction of guinea pig ileum and rat uterus, and to cause relaxation of rat duodenum. There is also evidence that it acts as both a peripheral and a central nervous system neurotransmitter.
D009842 Oligopeptides Peptides composed of between two and twelve amino acids. Oligopeptide
D010446 Peptide Fragments Partial proteins formed by partial hydrolysis of complete proteins or generated through PROTEIN ENGINEERING techniques. Peptide Fragment,Fragment, Peptide,Fragments, Peptide
D004298 Dopamine One of the catecholamine NEUROTRANSMITTERS in the brain. It is derived from TYROSINE and is the precursor to NOREPINEPHRINE and EPINEPHRINE. Dopamine is a major transmitter in the extrapyramidal system of the brain, and important in regulating movement. A family of receptors (RECEPTORS, DOPAMINE) mediate its action. Hydroxytyramine,3,4-Dihydroxyphenethylamine,4-(2-Aminoethyl)-1,2-benzenediol,Dopamine Hydrochloride,Intropin,3,4 Dihydroxyphenethylamine,Hydrochloride, Dopamine
D004594 Electrophysiology The study of the generation and behavior of electrical charges in living organisms particularly the nervous system and the effects of electricity on living organisms.
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D001717 Birds Warm-blooded VERTEBRATES possessing FEATHERS and belonging to the class Aves. Aves,Bird
D013329 Structure-Activity Relationship The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups. Relationship, Structure-Activity,Relationships, Structure-Activity,Structure Activity Relationship,Structure-Activity Relationships

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