Neurotensin receptors are transmembrane receptors that bind the
neurotransmitter neurotensin
Neurotensin is a 13 amino acid neuropeptide that is implicated in the regulation of luteinizing hormone and prolactin release and has significant interaction with the dopaminergic system. Neurotensin was first isolated from extracts of bovine ...
.
Two of the receptors encoded by the and genes contain seven transmembrane helices and are
G protein coupled. Numerous crystal structures have been reported for the neurotensin receptor 1 (NTS
1).
The third receptor has a single transmembrane domain and is encoded by the gene.
Ligands
Agonists
;Peptide
* Beta-lactotensin (NTS
2)
* JMV-449
*
Neurotensin
Neurotensin is a 13 amino acid neuropeptide that is implicated in the regulation of luteinizing hormone and prolactin release and has significant interaction with the dopaminergic system. Neurotensin was first isolated from extracts of bovine ...
*
Neuromedin N (NTS
1 selective)
* PD-149,163 (NTS
1 selective, reduced amide bond 8-13 fragment of neurotensin)
;Non-peptide
* NTS
1 full agonist SRI-9829
* Partial agonists derived from
SR-48692
Antagonists
*
Levocabastine
Levocabastine (trade name Livostin or Livocab, depending on the region) is a selective second-generation H1 receptor antagonist which was discovered at Janssen Pharmaceutica in 1979. It is used for allergic conjunctivitis.
As well as acting as ...
(NTS
2 selective, also H
1 histamine antagonist)
*
SR-48692 (NTS
1 selective)
*
SR-142948 (unselective, CAS# 184162-64-9)
Biophysical Investigation
Unusually for GPCRs, NTS1 can be expressed in an active form in the bacteria ''E. coli''.
It can be purified and analysed ''in vitro'' and has been analysed by a number of biophysical techniques such as surface plasmon resonance,
FRET
and cryo-electron microscopy.
Furthermore, high-resolution crystal structures of NTS
1 have been determined in complex with the peptide full agonist NT8-13, the non-peptide full agonist SRI-9829, the partial agonist RTI-3a, and the antagonists / inverse agonists SR-48692 and SR-142948, as well as in the ligand-free apo state
References
External links
*
*
G protein-coupled receptors
{{transmembranereceptor-stub