dysfunction

Phentolamine mesylate (Phentolamine methanesulfonate) is a nonselective alpha-adrenergic antagonist used to treat hypertension and hypertensive emergencies, pheochromocytoma, vasospasm of [RAYNAUD DISEASE] and frostbite, clonidine withdrawal syndrome, impotence, and peripheral vascular disease.

D(+)-Galactosamine hydrochloride is a well-established experimental toxin that induces liver injury primarily by generating free radicals and depleting UTP nucleotides, and it can be used to establish lipopolysaccharide/D-Galactosamine-induced hepatitis or acute liver injury models.

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

Trimethylamine N-oxide dihydrate (TMANO dihydrate) is a gut microbiota-dependent metabolite derived from dietary choline and other trimethylamine-containing nutrients. It induces inflammation by activating the ROS/NLRP3 inflammasome and promotes fibroblast differentiation and cardiac fibrosis via the TGF-β/Smad2 signaling pathway. TMANO dihydrate can be used to establish models of cardiac hypertrophy and cardiac fibrosis.

Nerol (Neryl alcohol) is a monoterpene found in many essential oils, such as lemon balm and hop.Nerol can lessened the severity of ouabain-triggered arrhythmias in mammalian heart.

Sarcosine (Methylglycine) is a competitive inhibitor of the type I glycine transporter (GlyT1) and an N-methyl-D-aspartate receptor (NMDAR) co-agonist.

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

Isolongifolene ((-)-Isolongifolene), a tricyclic sesquiterpene isolated from Murraya koenigii, exhibits antioxidant, anti-inflammatory, anticancer, and neuroprotective properties. It mitigates Rotenone-induced oxidative stress, mitochondrial dysfunction, and apoptosis by modulating the PI3K/AKT/GSK-3β signaling pathways.

Momordin Ic (Momordin 1c) might represent a potential anticancer activity, by inducing apoptosis through oxidative stress-regulated mitochondrial dysfunction involving the MAPK and PI3K-mediated iNOS and HO-1 pathways. Also, Momordin Ic accelerates gastrointestinal transit partially by stimulating synthesis of 5-HT to act through 5-HT(2), which, in turn, increases synthesis of prostaglandins.

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

AUT1 (AUT-1) is a novel specific modulator of Kv3 channels (EC50: 4.7 and 4.9 uM for Kv3.1b and Kv3.2a).

TMPH is an inhibitor of nAChR and inhibits nAChRs lacking α5, α6, or β3 subunits. TMPH can be used in studies about nAChR dysfunction or neurological disorders.

NS-3-008 hydrochloride (NS-3-008 HCl) is a transcriptional G0/G1 switch 2 (G0s2) inhibitor( IC50 of 2.25 μM).

N-(p-Coumaroyl) Serotonin, a polyphenol isolated from the seeds of safflower, exhibits antioxidant, cardioprotective effects after ischemia, and antitumor activity. It may improve vascular distensibility and reduce cardiovascular risk. N-(p-Coumaroyl) Serotonin ameliorates atherosclerosis and distensibility of the aortic wall in vivo, and is commonly used in atherosclerosis research.

RH01386 is a small molecule that prevents ER stress-induced β cell dysfunction and death, inhibits proapoptotic gene expression, and restores ER stress-impaired glucose-stimulated insulin secretion responses, showing potential for type 2 diabetes treatment.

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.

Propafenone (Propafenonum) is only found in individuals that have used or taken this drug. It is an antiarrhythmia agent that is particularly effective in ventricular arrhythmias. It also has weak beta-blocking activity. The drug is generally well tolerated. The electrophysiological effect of propafenone manifests itself in a reduction of upstroke velocity (Phase 0) of the monophasic action potential. In Purkinje fibers, and to a lesser extent myocardial fibers, propafenone reduces the fast inward current carried by sodium ions, which is responsible for the drugs antiarrhythmic actions. Diastolic excitability threshold is increased and effective refractory period prolonged. Propafenone reduces spontaneous automaticity and depresses triggered activity. At very high concentrations in vitro, propafenone can inhibit the slow inward current carried by calcium but this calcium antagonist effect probably does not contribute to antiarrhythmic efficacy.

Cefazolin sodium (cephazolin sodium) salt binds to and inactivates penicillin-binding proteins (PBP) located on the inner membrane of the bacterial cell wall. Cefazolin sodium salt is the sodium salt of cefazolin, a beta-lactam antibiotic and first-generation cephalosporin with bactericidal activity. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity, which results in the weakening of the bacterial cell wall and cell lysis.

Propantheline bromide (Pro-Banthine) competitively antagonizes acetylcholine activity mediated by muscarinic receptors at neuroeffector sites on smooth muscle and exocrine gland cells. Propantheline Bromide is the bromide salt form of propantheline, a quaternary ammonium compound structurally related to belladonna alkaloids. An aspartic acid residue present in the N-terminal portion of the third transmembrane helix of the muscarinic receptor is believed to form an ionic bond with the tertiary or quaternary nitrogen of the antagonist. Antagonism leads to a reduction of exocrine glands secretions and to relax the bronchial muscle and reduce tone and motility of intestinal smooth muscle.

Parecoxib (SC 69124) is an effective and selective COX-2 inhibitor.

Avanafil (TA1790) is a selective inhibitor of phosphodiesterase type 5 (PDE5) and is used as therapy of erectile dysfunction.

Mirodenafil is a PDE-5 inhibitor developed for the treatment of erectile dysfunction.

Enclomiphene citrate (trans-Clomiphene citrate) is a non-steroidal estrogen receptor antagonist,with antioestrogenic property

Phentolamine mesylate is an alpha-1 and alpha-2 selective adrenergic receptor antagonist