(D-Tyr11)-Neurotensin
(D-Tyr11)-Neurotensin is an agonist of neurotensin receptor (Neurotensin Receptor) and an inhibitor of glutamatergic neurotransmission. Activation of NTR1 in the VTA by (D-Tyr11)-Neurotensin enhances glutamatergic inputs to non-dopaminergic neurons, mediating reward and dopamine efflux; meanwhile, activation of NTR2 reduces glutamatergic excitatory postsynaptic currents (EPSC) in dopaminergic neurons. (D-Tyr11)-Neurotensin can be used in studies related to schizophrenia.
For research use only. We do not sell to patients.
- CAS No.: 64088-62-6
- Formula: C78H121N21O20
- Molecular Weight:1672.92
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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NTR1 |
NTR2 |
(D-Tyr11)-Neurotensin (0.01-0.5 μM; 7 min) dose-dependently attenuates glutamatergic EPSCs in VTA Ih+ neurons, producing a maximum mean decrease of 47% at 0.5 μM[1].
(D-Tyr11)-Neurotensin (0.01 μM; 7 min co-incubation with 0.1 μM antagonist) has its glutamatergic EPSC-attenuating effect in VTA Ih+ neurons blocked by 0.1 μM SR142948 but not 0.1 μM SR48692[1].
(D-Tyr11)-Neurotensin (0.01 μM; 7 min co-incubation with 0.1 μM antagonist) has its glutamatergic EPSC-enhancing effect in VTA Iₕ− neurons blocked by both 0.1 μM SR142948 and 0.1 μM SR48692[1].
(D-Tyr11)-Neurotensin (10-6 M) enhances potassium-evoked [3H]dopamine release from rat nucleus accumbens slices by 79%[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
(D-Tyr11)-Neurotensin (i.c.) exhibits higher potency than native neurotensin in inducing hypothermia following intracerebral injection in rats[2].
(D-Tyr11)-Neurotensin (100 pg-10 ng; uni. intra-VTA; single administration; 60 min monitoring) exerts an effect of increasing ipsilateral nucleus accumbens dopamine efflux in urethane (HY-B1207)-anesthetized male rat models[3].
(D-Tyr11)-Neurotensin (40-320 ng; uni. intra-VTA; single administration; observation for 30 min) exerts a strong dose-dependent contralateral rotational behavior-inducing effect in male rat models[3].
(D-Tyr11)-Neurotensin (0.1 nM-1 mM; uni. intra-VTA; single administration of 130 nl over 40 s; 60 min monitoring) alters extracellular dopamine concentrations in a region- and dose-dependent manner in urethane-anesthetized male rat models, producing differential effects in the prefrontal cortex, caudal nucleus accumbens, and rostral nucleus accumbens, including sustained elevation, delayed response, and reduced efflux depending on the brain region and concentration used[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Long-Evans (male, adult, 280-320 g, stereotaxic surgery with VTA guide cannulae implantation for CPP conditioning)[1]
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Dosage:1.5 nM, 3 nM
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Administration:bilateral intra-VTA
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Result:Induced a conditioned place preference attenuated by co-injection with 1.2 nM SR142948 (1.5 nM dose).
Induced a conditioned place preference blocked by co-injection with 1.2 nM SR48692 (3 nM dose).
Did not alter locomotor activity (horizontal and stereotypy-like movements) compared to control groups.
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Animal Model:Sprague-Dawley (male, 260-330 g, anaesthetized with urethane)[3]
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Dosage:100 pg, 1 ng, 10 ng
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Administration:uni. intra-VTA; single bolus ejection of 65 nl over 20 s
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Result:Produced a dose-dependent increase in dopamine efflux in the nucleus accumbens.
Required approximately 630 pg for half-maximal effect.
Caused peak effects 5-10 minutes after ejection depending on dose.
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Animal Model:Sprague-Dawley (male, 260-330 g, anaesthetized with chloral hydrate, implanted with unilateral guide cannula over VTA, 1 week recovery)[3]
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Dosage:40 ng, 80 ng, 160 ng, 320 ng
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Administration:uni. intra-VTA; single dose; 0.5 μl over 1 minute
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Result:Induced dose-dependent contralateral circling.
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Animal Model:Sprague-Dawley (male, 280-310 g)[4]
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Dosage:0.1 nM, 10 nM, 1 mM
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Administration:uni. intra-VTA; single administration of 130 nl over 40 s; 60 min monitoring
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Result:Induced an increase in extracellular dopamine concentration with a longer duration than native neurotensin or neurotensin.
Showed no effect on dopamine efflux in the prefrontal cortex at 10 nM.
Induced a significant decreasing phase followed by an increase of greater amplitude from 40 to 60 minutes in the caudal nucleus accumbens at 1 mM.
Induced an onset of smaller amplitude at t=2 min followed by a sustained increase from t=16 to 60 minutes in the caudal nucleus accumbens at 10 nM.
Induced an increase that began significantly later, from t=14 to 60 minutes in the caudal nucleus accumbens at 0.1 nM.
Induced a multiphasic effect: a short-lasting increase at t=4 min followed by a decreasing phase below baseline from t=10 to 30 minutes in the rostral nucleus accumbens at 1 mM.
Induced only a decreasing effect from t=4 to 40 minutes in the rostral nucleus accumbens at 10 nM, with a longer duration of the decreasing phase than native neurotensin.
Evoked a slight but non-significant increase in the rostral nucleus accumbens at 0.1 nM.
Chemical Information
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CAS No. 64088-62-6
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Molecular Weight 1672.92
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Formula C78H121N21O20
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SMILES
OC(C=C1)=CC=C1C[C@H](C(N[C@@H]([C@@H](C)CC)C(N[C@H](C(O)=O)CC(C)C)=O)=O)NC([C@H]2N(CCC2)C([C@H](CCCNC(N)=N)NC([C@H](CCCNC(N)=N)NC([C@H]3N(CCC3)C([C@H](CCCCN)NC([C@H](CC(N)=O)NC([C@H](CCC(O)=O)NC([C@@H](NC([C@H](CC(C)C)NC([C@H]4NC(CC4)=O)=O)=O)CC5=CC=C(C=C5)O)=O)=O)=O)=O)=O)=O)=O)=O
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Sequence
{Pyr}-Leu-Tyr-Glu-Asn-Lys-Pro-Arg-Arg-Pro-{d-Tyr}-Ile-Leu
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Sequence Shortening
{Pyr}-LYENKPRRP-{d-Tyr}-IL
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Rouibi K, et al. Ventral Midbrain NTS1 Receptors Mediate Conditioned Reward Induced by the Neurotensin Analog, D-Tyr[11]neurotensin. Frontiers in neuroscience. 2015;9:470.
[4]. Sotty F, et al. Comparative effects of neurotensin, neurotensin(8-13) and [D-Tyr(11)]neurotensin applied into the ventral tegmental area on extracellular dopamine in the rat prefrontal cortex and nucleus accumbens. Neuroscience. 2000;98(3):485-92. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
(D-Tyr11)-Neurotensin Related Classifications
HY-P0234A Related Classifications
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