Neurotensin receptor
Encyclopedia
The neurotensin receptors are transmembrane receptors that bind the neurotransmitter
neurotensin
. Two of the receptors encoded by the and genes contain seven transmembrane helices and are G protein coupled
. The third receptor has a single transmembrane domain and is encoded by the gene.
Non-peptide
Neurotransmitter
Neurotransmitters are endogenous chemicals that transmit signals from a neuron to a target cell across a synapse. Neurotransmitters are packaged into synaptic vesicles clustered beneath the membrane on the presynaptic side of a synapse, and are released into the synaptic cleft, where they bind to...
neurotensin
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...
. Two of the receptors encoded by the and genes contain seven transmembrane helices and are G protein coupled
G protein-coupled receptor
G protein-coupled receptors , also known as seven-transmembrane domain receptors, 7TM receptors, heptahelical receptors, serpentine receptor, and G protein-linked receptors , comprise a large protein family of transmembrane receptors that sense molecules outside the cell and activate inside signal...
. The third receptor has a single transmembrane domain and is encoded by the gene.
Agonists
Peptide- Beta-lactotensin (NTS2)
- JMV-449
- NeurotensinNeurotensinNeurotensin 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...
- Neuromedin NNeuromedin NNeuromedin N is a neuropeptide derived from the same precursor polypeptide as neurotensin, and with similar but subtly distinct expression and effects....
(NTS1 selective) - PD-149,163 (NTS1 selective, reduced amide bond 8-13 fragment of neurotensin)
Non-peptide
- Partial agonists derived from SR-48692
Antagonists
- LevocabastineLevocabastineLevocabastine is a selective second-generation H1-receptor antagonist which was discovered at Janssen Pharmaceutica in 1979. It is used for allergic conjunctivitis....
(NTS2 selective, also H1 histamine antagonist) - SR-48692SR-48692SR-48692 is a drug which acts as a selective, non-peptide antagonist at the neurotensin receptor NTS1, and was the first non-peptide antagonist developed for this receptor. It is used in scientific research to explore the interaction between neurotensin and other neurotransmitters in the brain, and...
(NTS1 selective) - SR-142,948SR-142,948SR-142,948 is a drug used in scientific research which is a non-peptide antagonist selective for the neurotensin receptors, although not selective between subtypes...
(unselective, CAS# 184162-64-9)