nk3 receptor

Pavinetant (MLE-4901) is an orally available neurokinin-3 receptor (NK3R) antagonist used to improve menopausal symptoms.

Fezolinetant (ESN-364) is a neurokinin-3 receptor antagonist that is being investigated for menopausal hot flashes.

Scyliorhinin II acetate is a selective agonist of the neurokinin-3 (NK3) receptor (Ki = 2.5 nM) in rat cerebral cortex.

CS-003 free base (CS-003) is a triple tachykinin receptor antagonist with high affinity for human (neurokinin) NK1, NK2 and NK3 receptors, with Ki values of 2.3 nM and 0.54 nM, respectively And 0.74 nM. CS-003 free base (CS-003) has therapeutic effects on

Osanetant produces anxiolytic- and antidepressant-like effects. Osanetant is a selective NK3 receptor antagonist. It is researched for schizophrenia.

SB-222200 is a selective, reversible, and competitive antagonist of the human NK-3 receptor(Ki=4.4 nM).

GR 94800 acetate is a potent and selective neurokinin 2(NK-2) antagonist.

SB 218795 is an effective and selective antagonist of NK3 with a Ki 13 nM for hNK3 which is about 90-fold and 7000-fold selectivity over hNK2 and hNK1.

NK3 receptor antagonist

MEN 10207 is an antagonist of tachykinin.

GSK172981 is a non-peptide tachykinin NK3 receptor antagonist with a high affinity for the recombinant human (PK (I) value 7.7) and native guinea pig (PK (I) value 7.8) tachykinin NK3 receptor. In vitro, the functional evaluation showed that GSK172981 was

Elinzanetant is a dual antagonist of neurokinin (NK) receptors 1 and 3 and modulates reproductive hormone secretion.

Talnetant (SB 223412) hydrochloride is a selective NK3 receptor antagonist with a Ki of 1.4 nM in hNK-3-CHO cells. It is 100 times more selective for the hNK-3 receptor than the hNK-2 receptor and shows no affinity for hNK-1 at a concentration of 100 μM.

RO4583298 is a highly potent dual NK1 NK3 receptor antagonist with in vivo activity.

Nolpitantium Free Base is a highly selective nonpeptide antagonist of neurokinin-1 (NK1) receptor. Nolpitantium potently, selectively and competitively inhibited substance P binding to NK1 receptors from various animal species, including humans. In vitro, it was a potent antagonist in functional assays for NK1 receptors such as [Sar9, Met(O2)11]substance P-induced endothelium-dependent relaxation of rabbit pulmonary artery and contraction of guinea-pig ileum. Up to 1 mkM, Nolpitantium had no effect in bioassays for NK2 and NK3 receptors. The antagonism exerted by Nolpitantium toward NK1 receptors was apparently non-competitive, with pD2' values between 9.65 and 10.16 in the different assays. Nolpitantium also blocked in vitro [Sar9, Met(O2)11]substance P-induced release of acetylcholine from rat striatum. In vivo, Nolpitantium exerted highly potent antagonism toward [Sar9, Met(O2)11]substance P-induced hypotension in dogs, bronchoconstriction in guinea-pig) and plasma extrava......

(S)-Osanetant, the S-enantiomer of Osanetant (SR142801), is a selective NK3 receptor antagonist known for its anxiolytic- and antidepressant-like effects. It is currently under investigation for potential use in treating schizophrenia [1].

Talnetant (SB 223412) is a selective, competitive NK3 receptor antagonist that penetrates the brain and modulates mesolimbic and mesocortical dopaminergic neurotransmission.

Hemokinin 1, human TFA acts as a selective full agonist at the tachykinin neurokinin 1 (NK1) receptor, while also being a full agonist at NK2 and NK3 receptors. It is capable of inducing opioid-independent analgesia [1] [2].

GR 94800 TFA is a potent, selective antagonist of the NK 2 receptor peptide, demonstrating pK B values of 9.6 for NK 2, 6.4 for NK 1, and 6.0 for NK 3 receptors, respectively [1] [2].

GR 64349 is a potent and highly selective NK2 receptor peptide antagonist with an EC50 of 3.7 nM in rat colon, exhibiting over 1000-fold selectivity against NK1 receptors and over 300-fold selectivity against NK3 receptors, ensuring targeted action [1] [2].

Senktide is an agonist of tachykinin NK3 receptor.

Senktide acetate (Senktide acetate(106128-89-6 free base)) is a selective tachykinin NK3 receptor agonist that promotes the consolidation or expression of ELM for the study of Alzheimer's disease.

Fosnetupitant chloride monohydrochloride (Pro-netupitant chloride monohydrochloride) is a selective NK1 antagonist exhibiting high affinity for the human NK1 receptor with a pK i value of 9.5, and a lower affinity for the NK3 receptor with a pK i of 6.1. It serves as a methylene phosphate prodrug of Netupitant [1].

Eledoisin (Eledone peptide) is an undecapeptide of mollusk origin in the tachykinin family of neuropeptides, serving as a specific agonist of NK2 and NK3 receptors.