NK1 Receptors

The neurokinin 1 (NK1) receptor is a member of the tachykinin family of G-protein-coupled receptors which also includes NK2 and NK3 receptors. The NK1 receptor is localized in high concentrations in the CNS (particularly the striatum and amygdala) and peripheral tissues.

Products
Background
Literature
Gene Data

Agonists

Cat No Product Name / Activity
1939 C14TKL-1
Endogenous NK1 agonist
1669 GR 73632
Potent, selective NK1 agonist
2576 Hemokinin 1 (human)
Endogenous, selective NK1 agonist
1535 Hemokinin 1 (mouse)
Endogenous, high affinity, selective NK1 agonist
1178 [Sar9,Met(O2)11]-Substance P
Potent, selective NK1 agonist

Antagonists

Cat No Product Name / Activity
2893 CP 96345
Potent and selective NK1 antagonist
3417 CP 99994 dihydrochloride
High affinity NK1 antagonist
2400 FK 888
High affinity NK1 receptor antagonist
1670 GR 82334
Tachykinin NK1 receptor antagonist
4013 L 760735
High affinity NK1 receptor antagonist
0868 L-732,138
Potent, selective NK1 antagonist
1145 L-733,060 hydrochloride
Potent NK1 antagonist
1635 RP 67580
Potent and selective NK1 antagonist
2394 SDZ NKT 343
Highly selective, human NK1 antagonist
1784 Spantide I
Selective NK1 antagonist
4012 SR 140333
Potent NK1 receptor antagonist

The neurokinin 1 (NK1) receptor is a member of the tachykinin family of G-protein-coupled receptors which also includes NK2 and NK3 receptors. The NK1 receptor is localized in high concentrations in the CNS (particularly the striatum, amygdala and some hypothalamic and thalamic nuclei) and peripheral tissues.

NK1 receptors are thought to mediate central stress reactions, mood control, excitatory neurotransmission, immune modulation and airway and lung function. The receptor displays greater potency for the endogenous agonist substance P than Neurokinin A and Neurokinin B (SP > NKA > NKB). The human gene encoding the NK1 receptor has been localized on chromosome 2 (2p13.1-p12).

External sources of pharmacological information for NK1 Receptors :

Literature for NK1 Receptors

GPCR

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Peptide Hormone Receptors

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Peptides Involved in Appetite Modulation

Peptides Involved in Appetite Modulation Scientific Review

Written by Sonia Tucci, Lynsay Kobelis and Tim Kirkham, this review provides a synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis; putative roles of the major peptides are outlined and compounds available from Tocris are listed.

Cardiovascular

Cardiovascular Poster

Cardiovascular disease remains one of the major causes of morbidity and mortality in the Western world and therefore this therapeutic area continues to be of great interest to researchers. This poster highlights the key GPCRs regulating vascular reactivity.

Depression

Depression Poster

Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.

NK1 Receptor Gene Data

Species Gene Symbol Gene Accession No. Protein Accession No.
Human TACR1 NM_001058 P25103
Mouse Tacr1 NM_009313 P30548
Rat Tacr1 NM_012585 P14600