h1 receptor antagonist

Y1 receptor antagonist 1 (H 409-22 isomer) is the active isomer of H-409/22, a neuropeptide Y (NPY) Y1 receptor antagonist that dose-dependently antagonizes the vascular response to exogenous and endogenous NPY in pigs. lagodeoxycholic acid (H 409-22 isomer) is the active isomer of H-409/22, an antagonist of neuropeptide Y (NPY) Y1 receptor.

Adenosine antagonist-1 acts as an adenosine A3 receptor (AA3R) antagonist.

Edg-2 receptor inhibitor 1 (SAR-100842) is an Edg-2 receptor inhibitor extracted (IC50: <0.1 μM).

CGRP antagonist 1 is a potent CGRP receptor antagonist with Ki values of 35 nM and IC50 values of 57 nM, respectively.CGRP antagonist 1 can be used for the study of cardiovascular and neurovascular diseases.

Adenosine receptor A1 antagonist 5 acts as an adenosine antagonist, is an oxypurine, acts as an insecticide and pest control agent, and has an inhibitory effect on elevated blood pressure.

Hepcidin antagonist-1 is an iron-modulating antagonist.Hepcidin antagonist-1 can be used to study metabolic disorders such as iron-deficiency diseases and anemia.

h-NTPDase8-IN-1 is a specific aminosulfonylbenzamide inhibitor of h-NTPDases8 (IC 50 = 0.28 ± 0.07 μM). h-NTPDase8-IN-1 can be used to study diseases brought about by aberrant h -NTPDase expression.

5-HT6 7 antagonist 1 is a dual 5-HT6 7 2A and D2 receptor antagonist for the study of dementia and Alzheimer's disease.

EP1-antagonist-1 (EP1 antagonist 1) is an EP1 antagonist (pKi: 7.54; pIC50: 8.5).

AMPA receptor modulator-1 can be activated by glutamate, thereby modulating ion channels.

LPA1 receptor antagonist 1(LPA1 R antagonist 1) is a selective and potent lysophosphatidic acid (LPA1) receptor antagonist (IC50 : 25 nM) for the study of idiopathic pulmonary fibrosis.

Estrogen receptor antagonist 8 acts as an estrogen receptor (ER) antagonist with anti-uterine activity and potential anti-tumorigenic activity and can be used to study ovarian dysfunction.

ORL1 antagonist 1 is an o antagonist of pioid receptor-like 1 (ORL1) (IC50 of 61 nM).

A2B receptor antagonist 1 (EXAMPLE 9B) is a potent A2B adenosine receptor antagonist.

GLP-1 receptor agonist 9 citrate is an agonist of GLP-1.

Protease-Activated Receptor-1, PAR-1 Agonist acetate is a selective proteinase-activated receptor1 (PAR-1) agonist peptide. Protease-Activated Receptor-1, PAR-1 Agonist acetate corresponds to PAR1 tethered ligand and which can selectively mimic theactions of thrombin via this receptor[1][2].

AMPA receptor antagonist-3 is an AMPA receptor antagonist.

A2B receptor antagonist 2 hydrochloride is an antagonist of adenosine receptor A2B (Ki = 2.30 μM for rA1, 6.8 μM for rA2A, 3.44 μM for hA2B).

AMPA receptor antagonist-2 is an AMPA receptor antagonist.

CRTh2 antagonist 1 is a CRTh2 antagonist (IC50: 89 nM).

5-HT2 antagonist 1 is a potent 5-HT2 receptor antagonist, has weak α1 adrenoceptor blocking activity.

AR antagonist 1 is a potent antagonist of the androgen receptor. It binds to E3 ligase ligands with weak binding affinities to VHL protein in the synthesis of PROTAC ARD-266.

5-HT2A antagonist 1 is a 5-HT2A antagonist. It may be useful in the treatment of gastrointestinal disorders circulatory disorders.

A2A receptor antagonist 1 (CPI-444 analog) is an antagonist of both adenosine A2A receptor and A1 receptor with Kis of 4 and 264 nM, respectively.

Dopamine D2 Receptor Antagonist-1 functions as a negative allosteric modulator (NAM) of the dopamine D2 receptor (D2R), demonstrating sub-millimolar affinity.

Sigma-1 receptor antagonist 2 is a potent and selective antagonist of sigma 1 receptor (σ1 R) (σ1 and σ2 receptor with Kis of 3.88 and 1288 nM , respectively).

Glucocorticoid receptor agonist-1 is a potent glucocorticoid receptor agonist with an IC50 of 2.8 nM[1].

Androgen receptor antagonist 1 is an orally available full androgen receptor antagonist (IC50: 59 nM). It can be used in the synthesis of PROTAC AR degraders, which results in 24% and 47 % AR protein degradation in LNCaP cells at 1 μM and 10 μM, respectively.

5-HT4 antagonist 1 is an antagonist of 5-HT4 (pKi = 9.6).

ERRα antagonist-1 (ERR+/- antagonist-1) is a high-affinity, selective antagonist of the estrogen-related receptor α (ERRα). It effectively prevents the interaction of ERRα with both Proliferator-activated Receptor γ Coactivator-1α (PGC-1α) and PGC-1β, displaying IC50 values of 170 nM and 180 nM, respectively. Notably, ERRα antagonist-1 does not interfere with the interactions involving ERRβ or ERRγ and the PGC-1α and PGC-1β coactivators. Furthermore, it does not affect the interaction between either ERα or ERβ and PGC-1α or SRC-1.

(E)-GABAB receptor antagonist 1 is a trans-GABAB receptor antagonist 1. (E)-GABAB receptor antagonist 1 decreases GABA-induced IP3 (inositol trisphosphate) production with IC50 of 37.9 μM. GABAB receptor antagonist 1 is a selective and negative allosteric modulator of GABAB (γ-Aminobutyric acid) receptors.

H3 receptor antagonist 1 is used in the study of neurological diseases, histamine H3 receptor antagonist.

CCR3 antagonist 1 is a potent CCR3 antagonist, used for the research of inflammatory and immunologic diseases.

N-(6-chloro-5-(2-Methoxyphenoxy)-2-(pyridin-4-yl)pyriMidin-4-yl)-5-Met inhibits endothelin binding to membranes from CHO cells carrying human ETA receptor and human ETB receptor with IC50 of 268nM and 1810nM, respectively.

Sigma-1 receptor antagonist 3 is a potent and selective antagonist of Sigma-1 (σ1) receptor(Ki : 1.14 nM), has the potential for the neuropathic pain.

Cimicifugoside H1 shows the protective function to cerebral neuron during cerebral ischemia.

GP130 receptor agonist-1 (N-(4-Fluorophenyl)-4-phenyl-2-thiazolami) is a potent, brain-penetrant and orally active GP130 receptor agonist.

DB21, Galectin-1 Antagonist, is a peptidomimetic conjugated with dibenzofuran, serving as an allosteric inhibitor of galectin-1 (GAL1) interactions with glycans on cell surfaces. This compound enhances the inhibition of angiogenesis and tumor growth in melanoma, lung adenocarcinoma, and ovarian cancer models [1].

CMKLR1 antagonist 1 (compound S-26d) is a potent, orally active antagonist of the chemokine-like receptor 1 (CMKLR1), exhibiting a pIC50 of 7.44 in hCMKLR1-transfected CHO cells. It is applicable in the research of psoriasis and metabolic diseases [1].

Compound 5e, a GPR34 receptor antagonist, exhibits selective inhibition of lysophosphatidylserine-induced ERK1/2 phosphorylation in a dose-dependent manner, demonstrating an IC50 value of 0.680 μM without significant cytotoxicity. Additionally, it displays antisensory activity in a mouse neuropathic pain model [1].

Compound 21, an orally active and selective RARα antagonist, exhibits a potent inhibition of the retinoic acid receptor α with an IC50 of 4.6 nM [1].

Interferon receptor inducer-1 Used in the treatment of a disorder in which the induction of interferon is involved. is an interferon (IFN) receptor inducer.

GluR6 antagonist-1 inhibits the pY binding site of tyrosine kinase p56lck SH2 domain.

GABA receptor Antagonist 1 (compound 7w) effectively inhibits the Px RDL1 GABAR at an IC50 of 7.08 nmol/L and demonstrates insecticidal efficacy against P. xylostella, S. frugiperda, S. exigua, and S. litura with respective LC50 values of 0.09, 0.84, 0.87, and 0.68 mg/L. Moreover, this compound exhibits moderate toxicity to honeybees (48 h, ID50 = 2.22 μg/adult) and low toxicity to zebrafish (LC50: 42.4 mg/L) [1].

Histamine H4 receptor antagonist-1 is a potent antagonist of the histamine H4 receptor.

Androgen Receptor Degrader-1 (Compound 18) is a potent agent for androgen receptor degradation, applicable in cancer research [1].

EP4 receptor antagonist 3 is a highly potent and specific inhibitor of the EP4 receptor. It is intended for research purposes in studying EP4 receptor-mediated diseases such as acute and chronic pain, osteoarthritis, rheumatoid arthritis, and cancer.

RXFP1 receptor agonist-1 (Example 2), an agonist of the RXFP1 receptor, suppresses cAMP production in HEK293 cells that constitutively express the human RXFP1, exhibiting an EC50 of 300 nM [1].

mGluR5 antagonist-1 (compound 10) is a potent mGluR5 inhibitor exhibiting an IC50 of 11.5 nM and demonstrates antidepressant effects [1].

Compound 39, also known as CB2 receptor antagonist 2, is a potent CB2 antagonist exhibiting an IC50 of 0.33 μM. It engages in strong interactions with residues L17, W6.48, V6.51, and C7.42 [1].