WIN 62577 is a species-selective tachykinin NK1 receptor antagonist. WIN 62577 is also an allosteric enhancer with micromolar potency at M3 receptors. WIN 62577 exhibits potent antiviral activity against SARS-CoV-2.

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

CP 122721 is an orally active NK1 receptor antagonist. CP 122721 attenuates cisplatin-induced vomiting in ferrets (ID50: 0.08 mg/kg). CP 122721 inhibits kainate (KA)-induced seizure activity and CA1 neuronal cell death in rats. CP 122721 is useful in the study of depression, asthma, and irritable bowel syndrome (IBS).

ASN-1377642 is a NK1 receptor antagonist with a Ki value of 251 nM. ASN-1377642 shows antitumor action in breast cancer cells with NK1R-Tr high expression.

Anthrotainin, a tetracyclic compound, is a substance P binding inhibitor with an IC50 of 3 μM.

(1R,2S,3R)-Aprepitant (Compound ent-4) is a competitive human neurokinin-1 (NK-1) receptor antagonist. (1R,2S,3R)-Aprepitant is promising for research of cancers and postoperative nausea and vomiting.

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.

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.

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.

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

Substance P antagonists (SPA).

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

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

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.

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

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.

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.

Imnopitant dihydrochloride is a neurokinin NK1 receptor antagonist.

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

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

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

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

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

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).

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

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

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.

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 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.

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.