neurokinin-3

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.

L-732138 is a potent and competitive antagonist of neurokinin-1 (NK-1) receptor(IC50 : 2.3 nM)

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

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.

SB 235375 is a potent and selective antagonist of the neurokinin-3 receptor with low penetrance in the central nervous system (CNS).

GSK256471 is a potent selective NK(3) antagonist that shows a high affinity for recombinant human (PK (I) value 8.9) and native guinea pig (PK (I) value 8.4) tachykinin NK(3) receptors. In vitro functional assessment showed that GSK256471 reduced the E(Ma

D-Lysine lactam is a chiral building block.1,2It has been used in the synthesis of a chiral antibiotic synthetic intermediate, as well as in the stereoselective synthesis of neurokinin (NK) receptor antagonists. 1.Kumar, A., Bhashkar, B., Bhavsar, J., et al.Catalytic reduction: Efficient synthesis of chiral key intermediate of besifloxacin hydrochlorideDer Pharma Chemica7(9)297-3000(2015) 2.Gerspacher, M., Lewis, C., Ball, H.A., et al.Stereoselective preparation of N-[(R,R)-(E)-1-(3,4-dichlorobenzyl)-3- (2-oxoazepan-3-yl)carbamoyl]allyl-N-methyl-3,5-bis(trifluoromethyl)benzamide, a potent and orally active dual neurokinin NK(1)/NK(2) receptor antagonistJ. Med. Chem.46(16)3508-3513(2003)

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

Osanetant HCl is the (R)-enantiomer; neurokinin-3 receptor antagonist

[Glp5,(Me)Phe8,Sar9] Substance P (5-11) (DiMe-C7) is an analogue of Substance P that acts on the neurokinin 1 receptor (NK1R) in rat brain, similarly to Substance P but with a significantly extended duration of action. This compound selectively enhances dopamine metabolism within the mesencephalon and midbrain cortex, increases motor activity, and facilitates the resumption of addictive agent-seeking behavior in rats [1] [2] [3].

[D-Trp2,7,9] Substance P is a tachykinin (Neurokinin Receptor) antagonist with inhibitory affinities (K_i values) of 1 μM for NK-1, 1.3 μM for NK-2, and approximately 9 μM for NK-3 receptors [1].

[Lys5,MeLeu9,Nle10]Neurokinin A(4-10) (LMN-NKA), a Neurokinin A analogue, is a selective and potent NK2 receptor (NK2R) agonist with prokinetic activity, making it valuable for researching smooth muscle contractions across various tissues through NK-2 receptor engagement [1][2][3].

GR 83074 is a potent and selective antagonist of the NK-2 (Neurokinin Receptor) with a 340-fold selectivity over NK-1 and a pK_B value of 8.23. It does not act as an antagonist for NK-3, affirming its specificity [1].

[MePhe7]-Neurokinin B is a neurokinin NK-3 receptor (NK3R) agonist, exhibiting a potent agonistic activity with an IC50 value of 3 nM. It acts as a potential regulator of pulsatile gonadotropin-releasing hormone (GnRH) secretion through the activation of NK3R [1].

(Trp7,β-Ala8)-Neurokinin A (4-10) is a potent neurokinin-3 (NK3) antagonist [1].

Men 10376 TFA(135306-85-3,free) (Neurokinin-2 receptor antagonist TFA) is an effective and selective tachykinin nk-2 receptor antagonist with a K I value of 4.4 M for the nk-2 receptor in the small intestine of rats.