Neurotensin receptors

Overview

Neurotensin receptors are activated by the endogenous tridecapeptide neurotensin (pGlu-Leu-Tyr-Glu-Asn-Lys-Pro-Arg-Arg-Pro-Tyr-Ile-Leu) derived from a precursor (NTS, 30990), which also generates neuromedin N, an agonist at the NTS2 receptor. [3H]neurotensin (human, mouse, rat) and [125I]neurotensin (human, mouse, rat) may be used to label NTS1 and NTS2 receptors at 0.1-0.3 and 3-5 nM concentrations respectively.
Excerpt from IUPHAR/BPS Guide to Pharmacology
Species
Family
Panel
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Species
Receptor
Family
Assays
Human
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Human non-orphan GPCRs
Oncology
Psychiatry
à la carte
Reference agonist:
neurotensin
EC50:
180 pM
Human
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Human non-orphan GPCRs
à la carte
Reference agonist:
SR48692
EC50:
83 nM
Mouse
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Mouse non-orphan GPCRs
à la carte
Reference agonist:
neurotensin
EC50:
74 pM
Mouse
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Mouse non-orphan GPCRs
à la carte
Reference agonist:
SR48692
EC50:
13 nM