SR 48692-sensitive neurotensin receptors modulate acetylcholine release in the rat striatum

Steinberg, R.; Rodier, Daniel; Mons, G.; Gully, Danielle; Fur, G. Le; Soubrié, Philippe

doi:10.1016/0143-4179(95)90053-5

Cited by 17 publications

(7 citation statements)

References 18 publications

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“…Taken together, these results support that at least the acute effects of SR 48692 and SR 48527 on A10 cell population response are mediated through blockade of high affinity NT receptors. It is worth noting that the effects of SR 48692 on A10 cell population response are produced by doses somewhat higher than those which antagonize the effects of exogenous NT in mice and rats (Poncelet et al, 1994a;Steinberg et al, 1995), suggesting that such electrophysiological changes require a higher level of NT receptor blockade.…”

Section: Discussionmentioning

confidence: 98%

Involvement of cortical neurotensin in the regulation of rat meso-cortico-limbic dopamine neurons: Evidence from changes in the number of spontaneously active A10 cells after neurotensin receptor blockade

Santucci

Gueudet

Steinberg

et al. 1997

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In order to further assess the role of endogenous neurotensin on midbrain dopaminergic neuronal function, the effects of the selective neurotensin receptor antagonists SR 48692 and SR 48527 were investigated on the number of spontaneously active A9 and A10 dopaminergic neurons in rats. Single intraperitoneal administration of SR 48692 (0.1-3 mg/kg) dose-dependently increased the number of active A10, but not A9 cells. SR 48527 (1 mg/kg) had a similar profile, but not SR 49711, its low affinity R-enantiomer, indicating that the effects observed were mediated through neurotensin receptor blockade. Five-week treatment with SR 48692 (3 mg/kg/day) produced a significant decrease of the number of active A10, but not A9 cells, which was reversed by apomorphine, suggesting that these cells were under depolarization block. Single co-administration of inactive doses of SR 48692 (0.1 mg/kg) and haloperidol (0.0625 mg/kg) significantly increased the number of active A10 cells. Conversely, co-administered active doses of SR 48692 or SR 48527 and haloperidol (1 and 0.25 mg/kg, respectively) induced an apomorphine-sensitive decrease of the number of A10 active cells. Finally, SR 48692 (10 mg/kg) modified neither accumbal nor cortical basal DA release. Local micro-injection of SR 48692 (10[-11]-10[-9] M), but not that of SR 49711 (10[-9] M), into the prefrontal cortex, increased the number of active A10 cells in a concentration-dependent manner. These results suggest that neurotensin receptor blockade counteracts a tonic inhibitory regulation by endogenous neurotensin of mesolimbic dopaminergic function and indicate that the prefrontal cortex is critically involved in this regulation.

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Section: Discussionmentioning

confidence: 98%

Involvement of cortical neurotensin in the regulation of rat meso-cortico-limbic dopamine neurons: Evidence from changes in the number of spontaneously active A10 cells after neurotensin receptor blockade

Santucci

Gueudet

Steinberg

et al. 1997

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“…The novel non‐peptide compounds SR 142948 and SR 48692 appear to be selective and potent antagonists of NT receptors in vitro and in vivo ( Gully et al ., 1993 ; 1997 ; Dubuc et al ., 1994 ; Steinberg et al ., 1994a , 1994b ; 1995 Schaeffer et al ., 1998 ), although, as already mentioned, they may act as agonists under given experimental conditions (CHO cells transfected with rodent NT 2 ‐receptors; Yamada et al ., 1998 ). Differences in receptor structure and functional responses were observed within species ( Gully et al ., 1997 ); in these studies, SR 142948 was generally more potent than SR 48692.…”

Section: Discussionmentioning

confidence: 99%

“…The heterogeneity of NT receptors has been suggested on functional grounds by in vivo rodent studies showing that SR 48692 antagonized some of the neuropeptide's effects (i.e. hypomotility and behavioural excitation), but not its ability to lower body temperature, raise pain threshold and produce some neurochemical changes ( Dubuc et al ., 1994 ; Steinberg et al ., 1995 ). The cloning of rodent ( Tanaka et al ., 1990 ) and human NT‐receptors from the HT 29 cell line ( Vita et al ., 1993 ) resulted in sites with high‐affinity in vitro specific binding (NT 1 ); a low‐affinity site (NT 2 ) was also cloned from rat brain ( Chalon et al ., 1996 ) and micromolar concentrations of the histamine H 1 receptor antagonist levocabastine completely prevented binding at this site ( Gully et al ., 1993 ; 1997 ).…”

Section: Introductionmentioning

confidence: 99%

In vitro functional evidence of different neurotensin‐receptors modulating the motor response of human colonic muscle strips

Croci

Aureggi

Guagnini

et al. 1999

British J Pharmacology

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1 The newly developed non-peptide neurotensin (NT)-receptor antagonists SR 48692 and SR 142948 were used to challenge NT responses of human colonic circular smooth muscle strips in vitro. The presence of NT 1 and NT 2 receptor transcripts in this tissue was tested by reverse transcriptase polymerase chain reaction (RT ± PCR) analysis. 2 NT potently and dose-dependently contracted muscle strips, with signi®cant regional di erences in potency and e cacy between the transverse and distal colon: EC 50 , 3.6 and 7.5 nM; the maximal e ect was 70 and 55% of 0.1 mM carbachol. Colonic responses to NT in both segments were virtually the same in the presence of atropine (1 mM), levocabastine (10 mM) or tetrodotoxin (1 mM). 3 SR 142948 (10 nM ± 1 mM) competitively antagonized NT responses in the transverse and distal colon with similar a nities: pA 2 values 8.71 and 8.45, slopes 0.98 and 0.99. SR 48692 (10 nM ± 10 mM) antagonized the NT response competitively in the distal colon (pA 2 6.55, slope 0.79) and non-competitively in the transverse colon (pA 2 8.0, slope 0.51). Neither compound had any agonist e ect. 4 The fact that the speci®c antagonists prevented NT-evoked atropine-and tetrodotoxin-insensitive mechanical responses of colonic muscle strips is highly consistent with the presence in these tissues of non-neuronal NT receptors, whose heterogeneity in the transverse segment is supported by the non-competitive antagonism of SR 48692. The ®nding of NT 1 receptor transcript in both transverse and distal colon suggests its identity with the lower a nity site disclosed functionally by SR 48692 in these segments.

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“…ACh levels were measured in 30-min dialysate samples (50 l) by using a high-performance liquid chromatography system (Waters, Milford, MA) as previously described by Steinberg et al (1995) except for the electrochemical detection system (Coulochem II; ESA, Chelmsford, MA). Briefly, the analytical system for ACh included a trapping precolumn and immobilized enzyme reactor (BAS.MF-6151).…”

Section: Crf-induced Hippocampal Acetylcholine Releasementioning

confidence: 99%

4-(2-Chloro-4-methoxy-5-methylphenyl)-N-[(1 S)-2-cyclopropyl-1-(3-fluoro-4-methylphenyl)ethyl]5-methyl-N-(2-propynyl)-1,3-thiazol-2-amine Hydrochloride (SSR125543A): A Potent and Selective Corticotrophin-Releasing Factor1 Receptor Antagonist. I. Biochemical and Pharmacological Characterization

Gully

Geslin²,

Serva³

et al. 2002

The Journal of Pharmacology and Experimental Therapeutics

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SR 48692-sensitive neurotensin receptors modulate acetylcholine release in the rat striatum

Cited by 17 publications

References 18 publications

Involvement of cortical neurotensin in the regulation of rat meso-cortico-limbic dopamine neurons: Evidence from changes in the number of spontaneously active A10 cells after neurotensin receptor blockade

Involvement of cortical neurotensin in the regulation of rat meso-cortico-limbic dopamine neurons: Evidence from changes in the number of spontaneously active A10 cells after neurotensin receptor blockade

In vitro functional evidence of different neurotensin‐receptors modulating the motor response of human colonic muscle strips

4-(2-Chloro-4-methoxy-5-methylphenyl)-N-[(1 S)-2-cyclopropyl-1-(3-fluoro-4-methylphenyl)ethyl]5-methyl-N-(2-propynyl)-1,3-thiazol-2-amine Hydrochloride (SSR125543A): A Potent and Selective Corticotrophin-Releasing Factor1 Receptor Antagonist. I. Biochemical and Pharmacological Characterization

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