acting

Erlotinib (NSC-718781) is an EGFR inhibitor (IC50: 2 nM). It is used for the treatment of non-small cell lung cancer.

(±)-Tazifylline is a selective and long-acting antagonist of histamine H1 receptor. Tazifylline shows much lower affinity for H2 receptors, α- and β-adrenoceptors, 5-hydroxytryptamine and muscarinic receptor subtypes.

DSP-0565 exhibits anti-convulsant activity and good safety margin in various models including scPTZ, 6 Hz, MES, and amygdala kindling. DSP-0565 can be used in studies about acting as a broad-spectrum anti-epileptic drug.

NUCC-390, a novel small-molecule CXCR4 receptor agonist, selectively induces CXCR4 receptor internalization while acting antagonistically to AMD3100. This compound facilitates nerve functional recovery following neurodegeneration in vivo.

TD-5471 hydrochloride is a selective and potent long-acting human β2-adrenergic receptor agonist for the treatment of chronic obstructive pulmonary disease (COPD).

Etripamil (MSP-2017) displays atrioventricular nodal conduction and prolongs atrioventricular nodal refractory periods by inhibiting calcium ion influx through the calcium slow channels in the atrioventricular node cells. Etripamil is an antagonist of short-acting L-type calcium-channel. It has a rapid onset of action designed for intranasal administration. It is also used to treat Paroxysmal Supraventricular Tachycardia.

Fluspirilene (R 6218) is a non-competitive L-type calcium channel antagonist (IC50: 0.03 μM).Fluspirilene is a long-acting antipsychotic compound used in the treatment of schizophrenia.

Pancopride(LAS 30451) is a novel, orally available, long-acting, selective 5-HT3 receptor antagonist that blocks nitrogen mustard and dacarbazine-induced vomiting.

PF-610355 is a long-acting and potent β2-adrenergic receptor agonist (EC50: 0.26 nM).PF-610355 can be used to study asthma and COPD.

Pranidipine (OPC-13340) is a novel, long-acting 1,4-dihydropyridine calcium channel blocker with antihypertensive activity. It enhances acetylcholine-induced relaxation in the presence of endothelium and nitroglycerin-induced relaxation in the absence of endothelium.

A 77636 hydrochloride is a potent, orally active, selective and long acting dopamine D1 receptor agonist (pKi=7.40; Ki=39.8 nM). A 77636 hydrochloride shows antiparkinsonian activity. A 77636 hydrochloride is functionally inactive at dopamine D2 receptor.

dopamine D1 receptor antagonist

Clopimozide (R-29764) acts as a calcium channel antagonist and inhibits [3H] nilandipine binding.Clopimozide is a novel and orally available long-acting antischizophrenic psychostatic compound.

Silperisone HCl (RGH-5002) blocks sodium and calcium channels in cells, decreases excitability and contractility of muscle cells, reduces peripheral tone, and acts as a muscle relaxant and peripheral vasodilator. Silperisone HCl is used to treat recurrent painful myoclonus due to spinal cord injury, abnormal hypertonia due to cerebrovascular disease, dystonia symptoms, cone tension syndrome, multiple sclerosis myospasm and myelitis. silperisone is a sodium channel protein type 2 alpha channel blocker. silperisone is an organosilicon similar to tolperisone, an organosilicon compound with centrally acting muscle relaxant properties.

Upacicalcet (AJT-240) is an intraventricular calcium mimetic, a SHPT available for human hemodialysis, that inhibits excessive parathyroid hormone (PTH) secretion by directly acting on parathyroid cell membrane calcium-sensitive receptors, thereby lowering blood levels of PTH.Upacicalcet is an orthosteric modulator of calcium-sensitive receptors and prevents adenine-induced secondary vascular calcification and bone disease in a rat model of adenine-induced secondary hyperparathyroidism.

Upacicalcet HCl is an intravesical calcium mimetic that inhibits excessive parathyroid hormone (PTH) secretion by directly acting on calcium-sensitive receptors in parathyroid cell membranes, thereby lowering PTH levels in the blood.Upacicalcet HCl can be used for the treatment of blood Upacicalcet HCl is a novel compound for the treatment of secondary hyperparathyroidism, targeting amino acid-binding sites of calcium-sensitive receptors. binding sites.

AZD 3043 (THRX 918661) is a variant modulator of the γ-aminobutyric acid type A receptor, a novel sedative-hypnotic and a potential short-acting anesthetic that produces hypnosis and EEG suppression in rats.AZD 3043 potentiates the γ-aminobutyric acid type A receptor and inhibits neuronal nicotinic acetylcholine receptors.

Etidocaine is an amino acidamide that acts as a local anesthetic with fast onset and long-acting properties.

Milveterol HCl is a long-acting β(2) -adrenergic receptor agonist for the potential treatment of chronic obstructive pulmonary disease (COPD).

Propanidid (Sombrevin) is a gamma-aminobutyric acid type A receptor (GABAA) agonist and a fast-acting intravenous anesthetic that lowers arterial blood pressure.

Verofylline (Verofyllinum) is an orally available, long-acting, multiacting, methylxanthine-substituted bronchodilator with inhibitory effects on PDE4 for the treatment of asthma disease research obesity.

N-0500 HCl ((-)-Propyl-9-hydroxynaphthoxazine Hydrochloride) is a very potent centrally acting DA receptor agonist. N-0500 HCl is a potent displacer of the specific [3H]DP_x0002_5,6-ADTN binding with IC50 of 3nM.

Viloxazine (Viloxazin) (Viloxazin) is a dual-action compound that functions as a norepinephrine reuptake inhibitor and exhibits potent agonistic activity towards 5-HT 2C receptors while acting as an antagonist for 5-HT 2B receptors, with respective potency values of EC 50 = 32 μM and IC 50 = 27 μM. Its primary mechanism of action involves the modulation of serotonergic and noradrenergic pathways. Viloxazine is commonly employed in depression research [1] [2].

SB-277011 hydrochloride (SB-277011A hydrochloride) is a potent, selective, and orally active dopamine D3 receptor (D3R) antagonist that crosses the blood-brain barrier, with Ki values of 10.7 nM for rodent D3R and 11.2 nM for human D3R. It is 80-100 times more selective for D3 receptors than other dopamine receptors, acting on D3 receptors (pKi: 8.0), D2 receptors (pKi: 6.0), 5-HT1B receptors (pKi < 5.2), and 5-HT1D receptors (pKi: 5.9).