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

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Showing 6151 - 6160 of 12702 results

Status:
Possibly Marketed Outside US
Source:
NCT04597190: Phase 4 Interventional Active, not recruiting PTSD
(2021)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Serotonin (5-hydroxytryptamine, or 5-HT) is a monoamine neurotransmitter produced by serotonergic neurons in the CNS and enterochromaffin cells in the gastrointestinal tract. Pharmacologic action of serotonin is mediated by a large and diverse range of 5-HT receptors. Serotonin plays an important part in the biochemistry of depression, migraine, bipolar disorder, and anxiety. It is also believed to be influential on sexuality and appetite. Creatinine is a product of the metabolic breakdown of creatine phosphate in muscle. Creatinine is filtered by healthy kidneys. Serotonin creatinine sulfate complex was the first isolated salt form of serotonin.
Status:
Possibly Marketed Outside US
Source:
Japan:Nilvadipine
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Nilvadipine (NIVADIL®) is a L-type calcium channel blocker for treatment of hypertension. It inhibits the influx of extracellular calcium through myocardial and vascular membrane pores by physically plugging the channel. The decrease in intracellular calcium inhibits the contractile processes of smooth muscle cells, causing dilation of the coronary and systemic arteries, increased oxygen delivery to the myocardial tissue, decreased total peripheral resistance, decreased systemic blood pressure, and decreased afterload.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)

ALONIMID, a compound which is structurally related to thalidomide, possesses sedative and hypnotic properties.
Potassium Orotate is a non-steroidal anabolic preparation with regenerating, diuretic effect. Potassium Orotate improves appetite, cardiac glycosides tolerance, stimulates regenerative and reparative processes of metabolism. Orotic acid is one of precursors the pyrimidine nucleotides which are a part of nucleic acids which participate in synthesis of protein molecules. In this regard potassium orotate is applied as substance of anabolic action at disturbances of protein metabolism, first of all at disturbance of albumin function of a liver, at the dystrophic changes in a myocardium which developed as owing to pathological process (a myocarditis, myocardial infarction), and as a result of a physical overstrain in sport as the general stimulators of metabolic processes.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)



The phenylpyrazosteroid cortivazol is a selective agonist ligand for the glucocorticoid receptor (GR), a steroid receptor member of the nuclear receptor superfamily of transcription factors. Cortivazol is an apoptotic, anti-inflammatory and immunosuppressive agent that has been used in the treatment of diskogenic radiculopathy, back pain, osteoarthritis and acute childhood lymphoblastic leukemia. Cortivazol has potent antileukemic activity in childhood ALL. Its activity is related to cell cycle arrest and induction of apoptosis. Cortivazol (Altim) is indicated in rheumatological diseases: - In intra-articular injection: inflammatory arthritis, advanced osteoarthritis. - In periarticular injection: tendinitis, bursitis. - In injection of soft tissue: talalgia, carpal tunnel syndrome, Dupuytren’s contracture. - In epidural injection: radiculalgia
Status:
Possibly Marketed Outside US
Source:
Whipcide by Merial
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Phthalofyne (3-methyl-1-pentyn-3-yl acid phthalate) is a synthetic chemical compound demonstrated to have trichuricidal activity against both Trichuris vulpis and Trichuris trichiura. It was used in veterinary medicine against dog whipworm, Trichuris vulpis, under the brand name Whipcide.
Dilevalol, the RR-stereoisomer of labetalol, is a non-cardioselective β-adrenoceptor antagonist with substantial partial β2-agonist and negligible α1-blocking activity. Reduction in blood pressure during dilevalol administration is associated with peripheral vasodilatation, and heart rate remains essentially unchanged. Following oral administration, dilevalol is completely absorbed. Once-daily administration is possible, due to a long elimination half-life. In vitro and in vivo animal studies and results obtained in humans reveal that dilevalol is a nonselective blocker of β1- and β2-adrenoceptors, with a similar potency to propranolol, but has negligible antagonistic activity at α1-receptors. Dilevalol, the R,R′ stereoisomer, makes up 25% of racemic labetalol, the drug, approved by FDA for the treatment of hypertension. The relaxing potency of dilevalol was approximately 4.7 times more potent than that of labetalol. Dilevalol markedly reduced the diastolic blood pressure with only a slight increase of heart rate In pithed rats, while isoproterenol and pindolol caused moderate to marked positive chronotropic effects in proportion to their hypotensive effects. These results suggest that dilevalol has more potent ISA than labetalol. In contrast to labetalol, dilevalol possesses little, if any, alpha-adrenergic blocking activity. The compound is 3 to 10 times less potent than labetalol at α1-adrenergic receptors under a variety of experimental conditions. Moreover, it is 300- to 1000-fold less potent at alpha1-adrenergic receptors compared with β1-adrenergic receptors. The pA2 values for dilevalol as an α antagonist range from 5.9 to 6.4. Because maximal plasma concentrations of the drug after administration of a 400-mg dose are approximately 0.5 pmol, it is doubtful that alpha blockade is involved in the antihypertensive response to dilevalol in humans.
Acivicin is a modified amino acid and structural analog of glutamine, that irreversibly inhibits glutamine-dependent amidotransferases involved in nucleotide and amino acid biosynthesis. Acivicin is a potent antitumor agent that induces apoptosis in human lymphoblastoid cells. Phase I dose-escalating studies conducted in cancer patients administered acivicin showed reversible, dose-limiting CNS toxicity, characterized by lethargy, confusion and decreased mental status.
Status:
Possibly Marketed Outside US
Source:
PMS-bezafibrate by Pharmascience Inc [Canada]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Bezafibrate is a lipid-lowering fibric acid derivative. Bezafibrate directly bound to and activated all three peroxisome proliferator-activated receptor (PPAR) subtypes respectively in PPAR binding and transactivation assays. However, from a biochemical point of view, bezafibrate is a PPAR ligand with a relatively low potency. Bezafibrate leads to considerable raising of HDL cholesterol and reduces triglycerides, improves insulin sensitivity and reduces blood glucose level, significantly lowering the incidence of cardiovascular events and new diabetes in patients with features of metabolic syndrome. It is the only pan-PPAR activator with more than a quarter of a century of therapeutic experience with a good safety profile.
Status:
Possibly Marketed Outside US
Source:
Japan:Pyrrolnitrin
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Pyrrolnitrin is an antifungal antibiotic and is most active against dermatophytic fungi, especially the species of Trichophyton. Fist, physical and chemical properties of pyrrolnitrin was described by Arima et al. It is synthesized from tryptophan, and the synthesis is probably initiated by a chloroperoxidase enzyme system acting on tryptophan. The present report deals with the mechanism of action of pyrrolnitrin. Pseudomonas pyrrocinia and other Pseudomonas species produce pyrrolnitrin from tryptophan as secondary metabolite. Pyrrolnitrin inhibits fungal growth by inhibiting the respiratory electron transport system.

Showing 6151 - 6160 of 12702 results