U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 21 - 30 of 35 results

Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)



Ginsenoside Rb1 is a triterpene saponin originally found in species of Panax that exhibits antioxidative, anti-inflammatory, neuroprotective, orexigenic, and stimulatory activities. In animal models, ginsenoside Rb1 increases motor activity, food intake, and skeletal muscle ATP content, improving energy metabolism. Ginsenoside Rb1 also downregulates expression of toll-like receptor 4 (TLR4) and TNF-α in animal models of sepsis, protecting against liver and lung damage. Additionally, ginsenoside Rb1 inhibits glucose-induced neurotoxicity by preventing GSK-3β-stimulated CHOP induction. This compound also activates Nrf2 and increases expression of heme oxygenase 1 (HO-1), suppressing oxidative stress in vitro. Ginsenoside Rb1 improves learning and memory, increases Bmax of M-cholinergic receptors, and accelerates cerebral protein and ACh biosynthesis. Ginsenoside Rb1 is a component of Korean Red Ginseng, marketed in Korea. Korean ginseng (Panax ginseng Meyer, Araliaceae) is traditionally used as an important herbal medicine in Far East Asia. Korean Red Ginseng is possibly effective for:
Status:
Possibly Marketed Outside US
Source:
Unknown
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Loganin was found in parts of some trees and shrubs including bark of Mastixia arborea (Cornaceae family), Corni fructus and A. boonei (Apocynaceae), a West African herbal medicinal plant traditionally used for its antimalarial, aphrodisiac, antidiabetic, antimicrobial properties. A key intermediate in the biosynthesis of indole alkaloids loganin was synthesized in 1971 by carboxyl group methylation of loganic acid. It has been shown, that loganin possesses anti-shock effects, anti-oxidant, glucose-lowering and neuroprotective properties. Loganin exhibits an anti-inflammatory effect in cases of acute pancreatitis and its pulmonary complications through inhibition of NF-κB activation. It is an active ingredient of a new herbal formula KBMSI-2 which has been through Phase 4 clinical trial for the efficacy and safety in the treatment of Erectile Dysfunction. Loganin inhibits β-secretase in vitro and increases performance in Morris water maze and Y-maze tests in vivo, suggesting potential benefit in memory impairment and Alzheimer’s disease. In addition, it also modulates ERK signaling to decrease connective tissue growth factor (CTGF) and downregulates expression of MCP-1, NF-κB, and iNOS in animal models. Inhibition of CTGF may be a potential target in diabetic nephropathy (DN) therapy, which highlights the possibility of using loganin to treat DN.
Status:
Possibly Marketed Outside US
Source:
Mvix by SK Chemicals
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



The inhibition of cyclic nucleotide Phosphodiesterase type 5 (PDE5) has been clinically validated as an effective treatment for erectile dysfunction. One of them is mirodenafil (formerly known as SK-3530) approved only in Korea. This drug was developed by SK Chemicals and marketed under the trade name Mvix.
Protodioscin is a steroidal saponin compound found in a number of plant species, most notably in the Tribulus, Trigonella and Dioscorea families. Extracts from T. terrestris standardised have been demonstrated to produce proerectile effects in isolated tissues and aphrodisiac action in several animal species. Protodioscin have shown cytotoxic effects against a number of leukemia and solid tumors cell lines.
Status:

Class (Stereo):
CHEMICAL (ACHIRAL)



Vardenafil (Levitra) 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.
Status:

Class (Stereo):
CHEMICAL (ACHIRAL)



Vardenafil (Levitra) 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.
Status:

Class (Stereo):
CHEMICAL (ACHIRAL)



Vardenafil (Levitra) 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.
Sildenafil (Viagra, Revatio) is a PDE5 inhibitor which was approved by FDA for the treatment of erectile disfunction and adults with pulmonary arterial hypertension. Upon administration sildenafil inhibits PDE5 and results in elevated level of cyclic guanosine monophosphate and smooth muscle relaxation.
Sildenafil (Viagra, Revatio) is a PDE5 inhibitor which was approved by FDA for the treatment of erectile disfunction and adults with pulmonary arterial hypertension. Upon administration sildenafil inhibits PDE5 and results in elevated level of cyclic guanosine monophosphate and smooth muscle relaxation.
SAR407899 is a potent, ATP-competitive Rho kinase inhibitor. It antihypertensive action in animals. Sanofi is developing SAR 407899 for the treatment of microvascular angina (Syndrome X). It was previously being developed in clinical trials for the treatment of diabetic neuropathies, diabetic nephropathies, erectile dysfunction, pulmonary hypertension, hypertension and kidney disorders, but development was discontinued for those indications.

Showing 21 - 30 of 35 results