Melitracen HCl ia potential dopamine D1/2 receptor antagonist used to treat depression. It is often co-administered with flupenthixol as a treatment for trigeminal neuralgia. It does not effect cardiovascular function. 了解更多
Zhihua Yi, .et al. Andrographolide Inhibits Mechanical and Thermal Hyperalgesia in a Rat Model of HIV-Induced Neuropathic Pain, Front Pharmacol, 2018, 9: 593 PMID: 29950989
Tripelennamine hydrochloride, a H1-receptor antagonist, is a psychoactive drug and member of the pyridine andethylenediamine classes that is used as an antipruritic and first-generation antihistamine. 了解更多
Robert A. Volkmann, .et al. MPX-004 and MPX-007: New Pharmacological Tools to Study the Physiology of NMDA Receptors Containing the GluN2A Subunit, PLoS One, 2016, 11(2): e0148129 PMID: 26829109
Oxprenolol is an orally bioavailable β-adrenergic receptor (β-AR) antagonist (Ki = 7.10 nM in a radioligand binding assay using rat heart tissue). It is non-selective and inhibits both β1- and β2-ARs (Kds = 2.09 and 1.35 nM in isolated rat heart and uterus, respectively). Oxprenolol is selective for β-ARs over serotonin (5-HT) receptors in rat sarcolemmal membrane preparations (IC50s = 4.13 and 23,300 nM, respectively), but it binds to 5-HT1A receptors in rat hippocampus and 5-HT1B in rat striatum (Kis = 94.2 and 642 nM, respectively). 了解更多
L-isomer of cetirizine and histamine H1 receptor antagonist
Levocetirizine dihydrochloride is a L-isomer of cetirizine and histamine H1 receptor antagonist. It incrases levels of CD4+ CD25+ T cells and decreases levels of eosinophils, decreasing allergy symptoms. 了解更多
Fimasartan is a non-peptide angiotensin II receptor antagonist (ARB) used for the treatment of hypertension and heart failure. Through oral administration, fimasartan blocks angiotensin II receptor type 1 (AT1 receptors), reducing pro-hypertensive actions of angiotensin II, such as systemic vasoconstriction and water retention by the kidneys. 了解更多
Etripamil (MSP-2017) is a short-acting L-type calcium-channel antagonist with a rapid onset of action designed for intranasal administration, used to treat Paroxysmal Supraventricular Tachycardia (PSVT). Etripamil (MSP-2017) slows atrioventricular nodal conduction and prolongs atrioventricular nodal refractory periods by inhibiting calcium ion influx through the calcium slow channels in the atrioventricular node cells. 了解更多
CGP 36742 is a selective GABAB receptor antagonist that can penetrate the blood?Cbrain barrier after peripheral administration, with an IC50 of 32?μM. CGP 36742 is useful in treatment of depression. 了解更多
PF-04634817 is an orally administered CCR2 and CCR5 chemokine receptor antagonist, for the treatment of diabetic nephropathies and diabetic macular oedema. 了解更多
LY-2940094 is a potent, selective and orally available nociceptin receptor (NOP receptor) antagonist with high affinity (Ki=0.105 nM) and antagonist potency (Kb=0.166 nM). LY-2940094 reduces ethanol self-administration in animal models. 了解更多
Azilsartan medoxomil monopotassium is an orally administered angiotensin II receptor type 1 antagonist with IC50 of 0.62 nM, which used in the treatment of adults with essential hypertension. 了解更多
SB-277011 dihydrochloride (SB-277011A dihydrochloride) is a potent, selective, orally bioavailable and brain penetrate dopamine D3 receptor antagonist, with pKis of 8.0, 6.0, <5.2 and 5.9 for D3, D2, 5-HT1B, and 5-HT1D receptors, respectively. 了解更多
JNJ-37822681 dihydrochloride is a potent, specific, centrally active, fast-dissociating dopamine D2 receptor antagonist with a moderate binding affinity for the dopamine D2L receptor (Ki =158 nM), which has potential for the treatment of schizophrenia and bipolar disorder. 了解更多
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