Neuronal Signaling

SCH 50911, (+)-(S)-5,5-dimethylmorpholinyl-2-acetic acid, a selective, orally-active and competitive γ-Aminobutyric acid B GABA(B) receptor antagonist.

Prasugrel (PCR 4099) Maleic acid is a platelet inhibitor with IC50 value of 1.8 μM.

7-Chlorokynurenic acid sodium salt is a potent and selective antagonist of the glycine B coagonist site of the N-methyl-D-aspartate (NMDA) receptor (IC50=0.56 μM).

SDZ 220-581 hydrochloride is an orally active, potent, competitive NMDA receptor antagonist with pKi value of 7.7.

Rislenemdaz (CERC-301) is an orally bioavailable and selective N-methyl-D-aspartate (NMDA) receptor subunit 2B (GluN2B) antagonist with Ki and IC50 of 8.1 nM and 3.6 nM, respectively.

Biperiden(KL 373) is an antiparkinsonian agent, which is the selective central M1 cholinoreceptors blocker.

Aclidinium Bromide(LAS 34273; LAS-W 330) is a long-acting, inhaled muscarinic antagonist as a maintenance treatment for chronic obstructive pulmonary disease (COPD).

Minodronic acid (YM-529) is an antagonist of purinergic P2X2/3 receptors involved in pain.

QNZ46 is a NR2C/NR2D-selective NMDA receptor non-competitive antagonist (IC50 values are 3, 6, 229, and >300, >300 μM for NR2D, NR2C, NR2A, NR2B, and GluR1, respectively).

Benzetimide hydrochloride is a muscarinic acetylcholine receptor antagonist.

DNQX Disodium is a water-soluble form of selective non-NMDA receptor antagonist DNQX.

Gabazine free base is a specific GABA receptor antagonist. Does not affect GABA-transaminase or glutamate-decarboxylase activitites.

NSC 102533 is a potent antagonist of the purinergic P2X7 receptor, a ligand-gated ion channel involved in inflammation and immune regulation. It effectively inhibits ATP-induced dye uptake in HEK293 cells expressing human P2X7 receptors with an IC₅₀ of 22.4 nM. NSC 102533 also suppresses ATP-induced IL-1β secretion in human THP-1 monocytes and primary mouse peritoneal macrophages, with IC₅₀ values of 9.8 nM and 11.2 nM, respectively, demonstrating strong anti-inflammatory activity.

In addition to its immunomodulatory effects, NSC 102533 exhibits antivenom potential by inhibiting Bothrops atrox venom proteolysis in a concentration-dependent manner. In in vivo studies, intradermal administration of NSC 102533 (3 mg/kg) significantly reduces skin hemorrhage induced by B. atrox and B. jararaca venom and attenuates carrageenan-induced paw edema in mice at doses between 0.01 and 1 mg/kg. These properties highlight NSC 102533 as a valuable pharmacological tool for studying P2X7 receptor–mediated inflammatory responses and venom-induced pathology.

Nor-benzetimide is a major metabolite of Benzetimide. Benzetimide is a mAChR antagonist with anticholinergic activity.

α-Bungarotoxin is a competitive antagonist at nicotinic acetylcholine receptors (nAChRs). α-Bungarotoxin, a selective α7 receptor blocker, blocks α7 currents with an IC50 of 1.6 nM and has no effects on α3β4 currents at concentrations up to 3 μM.