A potent, orally active, dual NK1 receptor antagonist (IC50=0.5 nM) and SERT inhibitor (IC50=5.2 nM).

A potent, selective and competitive NK1 receptor antagonist with IC50 of 2.3 nM.

A potent, selective, non-peptide NK1 receptor antagonist with Ki of 0.74 nM, IC50 of 1.6 nM.

Fosaprepitant (MK-0517, L-758,298) is a water-soluble phosphoryl prodrug for Aprepitant which is a NK1 antagonist.

Fosaprepitant (MK-0517, L-758,298) is a water-soluble phosphoryl prodrug for Aprepitant which is a NK1 antagonist.

Maropitant is a neurokinin (NK1) receptor antagonist.

NKP608 is a non-peptidic derivative of 4-aminopiperidine which acts as a selective, specific and potent antagonist at the neurokinin-1 (NK-1) receptor both in vitro(IC50=2.6 nM) and in vivo.

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

Substance P antagonists (SPA).

Rolapitant (SCH619734) is a potent, selective and orally active neurokinin NK1 receptor antagonist with a Ki of 0.66 nM.

Orvepitant maleate (GW823296 maleate) is potent, selective, orally active and well-tolerated neurokinin-1 receptor (NK-1) antagonist with a pKi of 10.2 for human neurokinin-1 receptor. Orvepitant maleate can across the blood-brain barrier. Orvepitant maleate has the potential for depressive disorder and chronic refractory cough (CRC) treatment.

Osanetant (SR142801) is a selective NK3 receptor antagonist. Osanetant produces anxiolytic- and antidepressant-like effects and is researched for schizophrenia.

MDL 29913, a cyclic pseudopeptide, is a competitive NK2 tachykinin receptor selective antagonist, with a pA2 of 8.66.

Spantide I, a substance P analog, is a selective NK1 receptor antagonist, with Ki values of 230 nM and 8150 nM for NK1 and NK2 receptor, respectively. Spantide I provides an approach to reduce type 1 and enhance the type 2 cytokine IL-10 in the infected cornea, leading to a significant reduction in corneal perforation.

Spantide I TFA, a substance P analog, is a selective NK1 receptor antagonist, with Ki values of 230 nM and 8150 nM for NK1 and NK2 receptor, respectively. Spantide I provides an approach to reduce type 1 and enhance the type 2 cytokine IL-10 in the infected cornea, leading to a significant reduction in corneal perforation.

Hemokinin 1, human is a selective tachykinin neurokinin 1 (NK1) receptor full agonist. Hemokinin 1, human is a full agonist at NK2 and NK3 receptor. Hemokinin 1, human can produces an opioid-independent analgesia.

Hemokinin 1, human TFA is a selective tachykinin neurokinin 1 (NK1) receptor full agonist. Hemokinin 1, human TFA is a full agonist at NK2 and NK3 receptor. Hemokinin 1, human TFA can produces an opioid-independent analgesia.

GR 94800 is a potent and selective NK2 receptor peptide antagonist, with pKB values of 9.6, 6.4 and 6.0 for NK2, NK1 and NK3 receptors, respectively.

GR 94800 TFA is a potent and selective NK2 receptor peptide antagonist, with pKB values of 9.6, 6.4 and 6.0 for NK2, NK1 and NK3 receptors, respectively.

GR 64349 is a potent and highly selective NK2 receptor peptide antagonist, with an EC50 of 3.7 nM in rat colon. GR 64349 exhibits selectivity >1000 and >300-fold with respect to NK1 and NK3 receptors, respectively.

[Lys5,MeLeu9,Nle10]-NKA(4-10) is a highly selective and potent NK2 receptor agonist, with an IC50 of 6.1 nM.

[Lys5,MeLeu9,Nle10]-NKA(4-10) TFA is a highly selective and potent NK2 receptor agonist, with an IC50 of 6.1 nM.

Biotin-Substance P is the biotin tagged Substance P. Substance P (Neurokinin P) is a neuropeptide, acting as a neurotransmitter and as a neuromodulator in the CNS. The endogenous receptor for substance P is neurokinin 1 receptor (NK1-receptor, NK1R).

Neurokinin A TFA (Substance K TFA), a peptide neurotransmitter of the tachykinin family, acts via the NK-2 receptor. Neurokinin A acts as a major mediator in human airway and gastrointestinal tissues.

Hemokinin 1 (mouse) is a selective agonist of neurokinin-1 receptor, with Ki of 0.175 nM and 560 nM for human NK1 receptor and human NK2 receptor, respectively.

SB 218795 is a potent and selective non-peptide NK3 receptor antagonist, with a Ki 13 nM for hNK3. SB 218795 shows about 90-fold and 7000-fold selectivity for hNK3 over hNK2 and hNK1, respectively. SB 218795 can inhibit NK3 receptor-mediated pupillary constriction of the rabbit.

Imnopitant is a NK1 receptor antagonist (WO2020132716, compound 1) .

Elinzanetant is a neurokinin receptors antagonist used for the research of Schizophrenia.

Benzomalvin B is the less active analogs of Benzomalvin A. Benzomalvin B is weakly active against substance P.

Imnopitant dihydrochloride is a neurokinin NK1 receptor antagonist.

L-760735 is a high affinity, selective and orally active NK1 receptor antagonist with an IC50 of 0.19 nM for human NK1 receptors. L-760735 exhibits anxiolytic and antidepressant-like effects.

Rolapitant (SCH619734) hydrochloride is a potent, selective, long-acting and orally active neurokinin 1 (NK1) receptor antagonist with a Ki of 0.66 nM. Rolapitant hydrochloride does not interact with CYP3A4. Rolapitant hydrochloride shows potent anti-emetic activity in a ferret emesis model.

Septide ((Pyr6,Pro9)-Substance P) is a potent NK1 receptor agonist with a Kd value of 0.55 nM.

MEN 10207 is a selective NK-2 tachykinin receptor (Neurokinin Receptor) antagonist. MEN 10207 has pA2 values of 5.2, 7.9 and 4.9 in three monoreceptor in vitro assays for NK-1, NK-2 and NK-3 tachykinin receptors, respectively.

FR 113680 is a tripeptide substance P antagonist that interacts selectively with the NK1 neurokinin receptor.