A small library of Fmoc-protected 3-arylated tyrosines was created by radical arylation. The new building blocks were successfully applied in the synthesis of two novel neurotensin receptor ligands. Both isomers showed high affinity for the human NTS2 receptor with K(i) values in the nanomolar range. Interestingly, subtype selectivity strongly depends on the configuration of the peptide in posi...

Cloned cDNAs encoding neurotensin were isolated from a cDNA library derived from primary cultures of canine enteric mucosa cells. Nucleotide sequence analysis has revealed the primary structure of a 170-amino acid precursor protein that encodes both neurotensin and the neurotensin-like peptide neuromedin N. The peptide-coding domains are located in tandem near the carboxyl terminus of the precu...

Using a radioimmunoassay toward the COOH-terminal region of neurotensin, an immunoreactive and biologically active neurotensin-related peptide (NRP) has been isolated from pepsin-treated fractions of bovine, canine, human, and rat plasma. Bovine NRP was identified as H-Ile-Ala-Arg-Arg-His-Pro-Tyr-Phe-Leu-OH, which is similar in structure to both neurotensin and angiotensin I. Canine and human N...

Parkinsonism, a common unwanted side effect of typical antipsychotic (neuroleptic) drugs, is induced by the blockade of striatal dopamine D2 receptors. In rats with hemi-parkinsonism induced by unilateral lesion of dopaminergic nigrostriatal neurons with 6-hydroxydopamine, D2 antagonists inhibit contralateral turning induced by D2 agonists and augment the levels of neurotensin mRNA in dopaminer...

STUDY DESIGN Controlled, repeated-measures, single-blind randomized study. OBJECTIVES To determine the effect of cervical or thoracic manipulation on neurotensin, oxytocin, orexin A, and cortisol levels. BACKGROUND Previous studies have researched the effect of spinal manipulation on pain modulation and/or range of movement. However, there is little knowledge of the biochemical process that...

The human placenta exhibits unique structural and multifunctional features. It is known to have the capacity to synthesize, store and secrete hormones of the hypothalamohypophyseal axis, but the existence of neurotransmitters and neuropeptides in the human placenta has attracted a great deal of attention. This is especially important when it is considered that the placenta is a non-innervated o...

BACKGROUND Excitatory interneurons account for the majority of neurons in laminae I-III, but their functions are poorly understood. Several neurochemical markers are largely restricted to excitatory interneuron populations, but we have limited knowledge about the size of these populations or their overlap. The present study was designed to investigate this issue by quantifying the neuronal popu...

The effects of intraocular injection of kainic acid and acrylamide upon retinal neuropeptides and high affinity binding sites have been determined in the chick. Kainic acid causes a sharp reduction in Met-enkephalin and somatostatin while neurotensin levels are unchanged. This treatment also lowers the extent of cholinergic muscarinic but not of [3H]naloxone or [3H]spiroperidol binding. In cont...

We tested whether Ca(2+)-mobilizing neuropeptides can function as growth factors for small cell lung carcinoma cells. The neuropeptides bradykinin, neurotensin, cholecystokinin, and vasopressin at nanomolar concentrations stimulated a rapid and transient increase in the intracellular concentration of Ca2+. Crucially, these peptides in the same concentration range also caused a marked increase i...