rats

Ziprasidone hydrochloride (CP-88059 hydrochloride) is a united 5-HT (serotonin) and dopamine receptor antagonist which shows potent effects of antipsychotic activity.

SBC-115076 is a potent extracellular proprotein convertase subtilisin kexin type 9 (PCSK9) antagonist.

NS6180 is a potent and selective KCa3.1 channel inhibitor(IC50= 9 nM). It prevents T-cell activation and inflammation.

Raloxifene (LY139481) is a selective estrogen receptor modulator that exhibits both estrogen agonist and antagonist activities at certain sites, with antiviral activity against viruses like Ebola, influenza, and HCV, useful for studying viral infections.

Zopolrestat (CP 73850) is a potent inhibitor of aldose reductase (IC50 = 3.1 nM).

Vardenafil (Vivanza) is an oral therapy for the treatment of erectile dysfunction. It is a selective inhibitor of cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5). Penile erection is a hemodynamic process initiated by the relaxation of smooth muscle in the corpus cavernosum and its associated arterioles. During sexual stimulation, nitric oxide is released from nerve endings and endothelial cells in the corpus cavernosum. Nitric oxide activates the enzyme guanylate cyclase resulting in increased synthesis of cyclic guanosine monophosphate (cGMP) in the smooth muscle cells of the corpus cavernosum. The cGMP in turn triggers smooth muscle relaxation, allowing increased blood flow into the penis, resulting in erection. The tissue concentration of cGMP is regulated by both the rates of synthesis and degradation via phosphodiesterases (PDEs). The most abundant PDE in the human corpus cavernosum is the cGMPspecific phosphodiesterase type 5 (PDE5); therefore, the inhibition of PDE5 enhances erectile function by increasing the amount of cGMP.

N,N'-Dicyclohexylurea (AURORA KA-3582) is a soluble epoxide hydrolase (sEH) inhibitor.

Vardenafil hydrochloride trihydrate (BAY38-9456) is a new type PDE inhibitor with IC50 of 0.7 and 180 nM for PDE5 and PDE1, respectively.

Vardenafil hydrochloride is a New Phosphodiesterase Type 5(PDE5) Inhibitor, in the Treatment of Erectile Dysfunction in Men With Diabetes

VPC171 is a novel adenosine A1 receptor positive allosteric modulator (PAM).

Metyrapone (NSC-25265) is an inhibitor of the enzyme STEROID 11-BETA-MONOOXYGENASE. It is used as a test of the feedback hypothalamic-pituitary mechanism in the diagnosis of CUSHING SYNDROME.

BMY 7378 dihydrochloride (BMY7378 HCl) , α1D-adrenergic receptor antagonist, is a weak partial agonist/antagonist of 5-HT1A receptor.

RO 46-8443 is the first non-peptide endothelin ETB receptor selective antagonist. RO 46-8443 displays up to 2000-fold selectivity for ETB receptors both in terms of binding inhibitory potency and functional inhibition.

Vardenafil dihydrochloride (Levitra) is a new type PDE inhibitor with IC50 of 0.7 and 180 nM for PDE5 and PDE1, respectively.

SPHINX31 is a potent inhibitor of serine/arginine-rich protein kinase 1 (SRPK1; IC50: 5.9 nM).

Trandolapril is an orally administered angiotensin converting enzyme (ACE) inhibitor that is hydrolysed to the active diacid trandolaprilat.

Lerisetron is an antagonist of serotonin type 3 (5-HT3) receptor, with antiemetic activity.

Ampreloxetine hydrochloride (TD-9855 HCl) has anti-inflammatory activity and is a potential compound for the treatment of depression and Alzheimer's disease.

NKP608 is a selective and highly effective neurokinin-1 (NK-1) receptor antagonist with anticancer and antianxiety activities, inhibiting the proliferation of human colorectal cancer cells through the Wnt signaling pathway.

The ED50 of J-2156 in rats for the relief of mechanical allodynia and mechanical hyperalgesia in the ipsilateral hindpaws was 3.7 and 8.0 mg/kg, respectively. J-2156 is a high potent, selective somatostatin receptor type 4 (SST4 receptor) agonist with IC5

KGA-2727 is a potent and selective SGLT1 inhibitor, with Kis of 97.4 nM and 43.5 nM for human and rat SGLT1, respectively. The selectivity ratios (Ki for SGLT2/Ki for SGLT1) of KGA-2727 are 140 (human) and 390 (rat). KGA-2727 for the treatment of diabete.

Men 10376 is a selective antagonist of tachykinin NK-2 receptor. It has a Ki of 4.4 μM for rat small intestine NK-2 receptor.

trans-AUCB (t-AUCB) is an effective and selective soluble epoxide hydrolase inhibitor, with IC50 values of 1.3 nM for hsEH, 8 nM for mouse sEH, and 8 nM for rat sEH.

DPCPX (PD 116948) is an A1 adenosine receptor antagonist