{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,1,15]],"date-time":"2026-01-15T03:33:03Z","timestamp":1768447983470,"version":"3.49.0"},"reference-count":55,"publisher":"Wiley","issue":"6","license":[{"start":{"date-parts":[[2009,8,26]],"date-time":"2009-08-26T00:00:00Z","timestamp":1251244800000},"content-version":"vor","delay-in-days":5036,"URL":"http:\/\/onlinelibrary.wiley.com\/termsAndConditions#vor"}],"content-domain":{"domain":["onlinelibrary.wiley.com"],"crossmark-restriction":true},"short-container-title":["Fundamemntal Clinical Pharma"],"published-print":{"date-parts":[[1995,11,12]]},"abstract":"<jats:p><jats:bold>Summary\u2014<\/jats:bold>Neurotensin, an endogenous peptide widely distributed throughout the brain, fulfils neurotransmitter criteria. When administered centrally, neurotensin induces various effects and modulates the activity of the mesolimbic dopamine system. It antagonizes the behavioural action of dopamine in a manner similar, but not identical, to antipsychotic drugs. Neurotensin is even considered to be an endogenous neuroleptic. In fact, microinjection of neurotensin elicits different effects depending on both the dose and the cerebral structures into which the injection is made. Our work on the development of orally\u2010active neurotensin antagonists has led to the identification of SR 48692, the first non\u2010peptide antagonist of the neurotensin receptor, and some analogues. This small molecule reveals a surprising neuropharmacological profile. It antagonizes turning behaviour induced in mice and rats (after striatal or ventral tegmental area administration of neurotensin, respectively), hypolocomotion induced by intracerebroventricular injection of neurotensin in rats, and reverses the inhibitory effect of neurotensin (nucleus accumbens injection) on amphetamine\u2010induced hyperlocomotion in rats. However, SR 48692 cannot reverse either dopamine release in the nucleus accumbens evoked by neurotensin injection in ventral tegmental area, or hypothermia and analgesia induced by intracerebroventricular injection of neurotensin. As direct and indirect dopamine agonists have been reported to promote neurotensin release in the cortex, behavioural studies were performed using injection of apomorphine. In these experiments, SR 48692 inhibited only turning and yawning. It did not antagonize other apomorphine\u2010dependent effects such as climbing, hypothermia, hypo\u2010 or hyperlocomotion, penile erection and stereotypies. All together, these data raise the question of the existence of neurotensin receptor subtypes and confirm that the nature of neurotensin and dopamine interactions depends on the brain structures considered.<\/jats:p>","DOI":"10.1111\/j.1472-8206.1995.tb00528.x","type":"journal-article","created":{"date-parts":[[2009,8,26]],"date-time":"2009-08-26T17:21:27Z","timestamp":1251307287000},"page":"513-521","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":27,"title":["Neuropharmacological profile of non\u2010peptide neurotensin antagonists"],"prefix":"10.1111","volume":"9","author":[{"given":"D.","family":"Gully","sequence":"first","affiliation":[]},{"given":"F.","family":"Jeanjean","sequence":"additional","affiliation":[]},{"given":"M.","family":"Poncelet","sequence":"additional","affiliation":[]},{"given":"R.","family":"Steinberg","sequence":"additional","affiliation":[]},{"given":"P.","family":"Soubri\u00e9","sequence":"additional","affiliation":[]},{"given":"G Le","family":"Fur","sequence":"additional","affiliation":[]},{"given":"JP","family":"Maffrand","sequence":"additional","affiliation":[]}],"member":"311","published-online":{"date-parts":[[2009,8,26]]},"reference":[{"key":"e_1_2_1_2_1","doi-asserted-by":"publisher","DOI":"10.1016\/0006-8993(91)90139-M"},{"key":"e_1_2_1_3_1","doi-asserted-by":"publisher","DOI":"10.1016\/0014-5793(86)80565-8"},{"key":"e_1_2_1_4_1","doi-asserted-by":"publisher","DOI":"10.1016\/0006-291X(85)91411-1"},{"key":"e_1_2_1_5_1","doi-asserted-by":"publisher","DOI":"10.1016\/0304-3940(94)90671-8"},{"key":"e_1_2_1_6_1","doi-asserted-by":"crossref","first-page":"489","DOI":"10.1016\/S0026-895X(25)10277-0","article-title":"Neurotensin\u2010mediated inhibition of cyclic AMP formation in neuroblastoma N1E\u2010115 cells: involvement of the inhibitory GTP\u2010binding component of adenylate cyclase","volume":"29","author":"Bozou JC","year":"1986","journal-title":"Mol Pharmacol"},{"key":"e_1_2_1_7_1","doi-asserted-by":"publisher","DOI":"10.1016\/0014-2999(94)90204-6"},{"key":"e_1_2_1_8_1","doi-asserted-by":"publisher","DOI":"10.1046\/j.1471-4159.1994.63010019.x"},{"key":"e_1_2_1_9_1","unstructured":"ChakravartyPKet al.Comm. in 206th ACS Natl Meet (August 22\u201327 Chicago IL)1993; Abstract MEDI 198."},{"key":"e_1_2_1_10_1","first-page":"7","article-title":"Inhibition of neurotensin (NT)\u2010stimulated mast cell histamine secretion by NT\u2010receptor (NT\u2010R) antagonist and by pertussis toxin (PT): evidence for a NT\u2010R on the rat mast cell","volume":"8","author":"Cochrane DE","year":"1994","journal-title":"Faseb J"},{"key":"e_1_2_1_11_1","doi-asserted-by":"crossref","first-page":"1036","DOI":"10.1016\/S0026-895X(25)13264-1","article-title":"Pharmacological studies on novel neurotensin mimetics: discovery of a pharmacologically unique agent exhibiting concentration\u2010dependent dual effects as antagonist and agonist","volume":"44","author":"Cusack B.","year":"1993","journal-title":"Mol Pharmacol"},{"key":"e_1_2_1_12_1","doi-asserted-by":"publisher","DOI":"10.1111\/j.1476-5381.1994.tb13077.x"},{"key":"e_1_2_1_13_1","doi-asserted-by":"publisher","DOI":"10.1016\/0278-5846(88)90073-5"},{"key":"e_1_2_1_14_1","doi-asserted-by":"publisher","DOI":"10.1038\/291073a0"},{"key":"e_1_2_1_15_1","doi-asserted-by":"publisher","DOI":"10.1176\/ajp.148.4.484"},{"key":"e_1_2_1_16_1","doi-asserted-by":"publisher","DOI":"10.1016\/0014-2999(84)90248-6"},{"key":"e_1_2_1_17_1","doi-asserted-by":"publisher","DOI":"10.1073\/pnas.90.1.65"},{"key":"e_1_2_1_18_1","doi-asserted-by":"publisher","DOI":"10.1016\/0006-2952(94)90440-5"},{"key":"e_1_2_1_19_1","doi-asserted-by":"publisher","DOI":"10.1016\/0143-4179(84)90090-8"},{"key":"e_1_2_1_20_1","doi-asserted-by":"publisher","DOI":"10.1016\/0361-9230(93)90295-M"},{"key":"e_1_2_1_21_1","doi-asserted-by":"publisher","DOI":"10.1016\/0306-4522(83)90195-1"},{"key":"e_1_2_1_22_1","doi-asserted-by":"publisher","DOI":"10.1111\/j.1471-4159.1986.tb13061.x"},{"key":"e_1_2_1_23_1","unstructured":"KestenSR AkunneH. 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