neurokinin b

Neurokinin B (NKB) belongs in the family of tachykinin peptides. Neurokinin B is implicated in a variety of human functions and pathways such as the secretion of gonadotropin-releasing hormone.

Neurokinin B TFA, a member of the tachykinin family, binds to a series of GPCRs, including neurokinin receptors 1 (NK1R), NK2R, and NK3R, to modulate their biological effects.

(D-Pro2,D-Trp6,8,Nle10)-Neurokinin B 是 Neurokinin B(Neurokinin Receptor) 的竞争性拮抗剂，pA2 为 5.5，对 Substance P 或 Neurokinin A 没有影响。

Tyr0-Neurokinin B (Tyr-NKB)为Neurokinin B的类似物，具有引发膀胱收缩的生物活性。

[MePhe7]-Neurokinin B为NK-3受体(NK3R)激动剂，具有3 nM的IC50值。通过激活神经激肽3受体，[MePhe7]-Neurokinin B能够调节脉冲促性腺激素释放激素(GnRH)的分泌，成为调控该过程的潜在调节剂。

Neurokinin B acetate(86933-75-7 free base) 是属于速激肽家族的神经激肽 B 的醋酸盐形式。神经激肽与神经激肽受体 1 (NK1R)、nk2r 和 NK3R 结合，并介导其生物学效应。

SB-222200 是一种选择性口服活性的，具有血脑屏障渗透性的 NK-3 受体拮抗剂，用于中枢神经系统疾病的研究。

L 363851 is a neurokinin B agonist.

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)

Benzomalvin B is a fungal metabolite originally isolated from Penicillium. It acts as an antagonist of neurokinin-1 (NK1) receptors, inhibiting binding of substance P by 24% in vitro when used at a concentration of 100 μg ml.

Benzomalvin C is a weak antagonist of the neurokinin-1 (NK1) receptor inhibiting binding of substance P by 46% when used at 100 μg ml in vitro. It is also a weak inhibitor of indolamine 2,3-dioxygenase (IDO) with an IC50 value of 130 μM for recombinant IDO. It was isolated from Penicillium and contains an epoxide group at C-19 and C-20, which is not present in benzomalvins A, B, or E.

GR 83074 是一种有效的选择性 NK-2(Neurokinin Receptor) 拮抗剂，pKB 为 8.23。GR 83074 对 NK-3 没有活性，并表现出 340 倍的 NK-2 NK-1 选择性。