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

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

Showing 31371 - 31380 of 31824 results

Status:
Possibly Marketed Outside US
Source:
ZANIDIP by Corsini, A.|Bonfatti, M.|Quarato, P.|Accomazzo, M.R.|Raiteri, M.|Sartani, A.|Testa, R.|Nicosia, S.|Paoletti, R.|Fumagalli, R.
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



(S)-Lercanidipine is enantiomer of antihypertensive drugs Lercanidipine, that acts by blocking L-type calcium channels, allowing relaxation and opening of blood vessels. The dihydropyridine calcium antagonists promote systemic vasodilatation by a reversible blockade of voltage-dependent Ca2+ influx through L-type channels in the cell membrane. (S)-Lercanidipine has 100- to 200-fold greater affinity than the (R)-enantiomer for the L-type calcium channel. The pharmacokinetics of (S)- Lercanidipine has been evaluated in healthy volunteers, in elderly and non-elderly patients with hypertension, and in patients with renal or hepatic impairment. Patients from these studies were investigated after receiving a single 10 or 20 mg dose of [14C]-labeled rac-Lercanidipine as a solution. The maximum plasma concentrations of (S)-Lercanidipine were reached within 2–3 h and the area under the plasma concentration-time curves were not linearly related to the dose, indicating a saturable first-pass metabolism. The absorption of (S)-LER increases after the ingestion of a high-fat meal. Lercanidipine is highly bound to plasma protein (>98%) in humans. Its volume of distribution of 2–2.5 L/kg was determined in healthy volunteers after intravenous infusion of 2 mg. Lercanidipine is extensively metabolized by CYP 3A4 to inactive pyridine derivatives. A crossover study involving a single administration of either 10 mg of (R)- or (S)-LER or 20 mg of rac-LER as a solution demonstrated no in vivo enantiomer interconversion
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)

Bietamiverine is an antispasmodic agent.
Status:
Possibly Marketed Outside US
Source:
Japan:Olanexidine Hydrochloride Hydrate
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Olanexidine [1-(3,4-dichlorobenzyl)-5-octylbiguanide] (formerly OPB-2045), an antimicrobial agent exhibited antimicrobial activity against a wide range of bacteria, especially Gram-positive bacteria, was synthesized in 1997. To optimize its use as a topical antiseptic, olanexidine was converted to the gluconate salt. The resulting formulation (OPB) had more potent bactericidal activity against methicillin-resistant S. aureus and vancomycin-resistant enterococci in both in vitro and in vivo animal models than chlorhexidine and PVP-I. The mechanism of action was considered to be follows: olanexidine binds to the cell membrane, disrupts membrane integrity, and exerts its bacteriostatic and bactericidal activities by causing the irreversible leakage of intracellular components. At relatively high concentrations, olanexidine aggregates the cells through a protein-denaturing effect.
Status:
Possibly Marketed Outside US
Source:
ZANIDIP by Corsini, A.|Bonfatti, M.|Quarato, P.|Accomazzo, M.R.|Raiteri, M.|Sartani, A.|Testa, R.|Nicosia, S.|Paoletti, R.|Fumagalli, R.
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



(R)-Lercanidipine is enantiomer of antihypertensive drugs Lercanidipine, that acts by blocking L-type calcium channels, allowing relaxation and opening of blood vessels. The dihydropyridine calcium antagonists promote systemic vasodilatation by a reversible blockade of voltagedependent Ca2+ influx through L-type channels in the cell membrane. (S)-Lercanidipine has 100- to 200-fold greater affinity than the (R)-enantiomer for the L-type calcium channel. The pharmacokinectics of (S)- Lercanidipine has been evaluated in healthy volunteers, in elderly and non-elderly patients with hypertension, and in patients with renal or hepatic impairment. Patients from these studies were investigated after receiving a single 10 or 20 mgdose of [14C]-labeled rac-Lercanidipine as a solution. The maximum plasma concentrations of (S)-Lercanidipine were reached within 2–3 h and the area under the plasma concentration–time curves were not linearly related to the dose, indicating a saturable first-pass metabolism. The absorption of (S)-LER increases after the ingestion of a highfat meal. Lercanidipine is highly bound to plasma protein (>98%) in humans. Its volume of distribution of 2–2.5 L/kg was determined in healthy volunteers after intravenous infusion of 2 mg. Lercanidipine is extensively metabolized by CYP 3A4 to inactive pyridine derivatives. A crossover study involving a single administration of either 10 mg of (R)- or (S)-LER or 20 mg of rac-LER as a solution demonstrated no in vivo enantiomer interconversion
Status:
Possibly Marketed Outside US
Source:
NCT02213068: Phase 4 Interventional Completed Transplant; Failure, Kidney
(2014)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Aminopropyl racementhyl phosphate is a prodrug of menthol patented by Pacific Corporation (Korea). Upon administration, it is enzymatically decomposed into menthol and 3-aminopropylphosphoric acid, a component used for anti-aging cosmetic composition. Aminopropyl racementhyl phosphate was found to reduce the irritation of menthol while maintaining its useful effects.
Status:
Possibly Marketed Outside US
Source:
NCT03885778: Phase 4 Interventional Completed Food Effect
(2019)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

LB80380 is a prodrug of besifovir, a novel antiviral agent for the treatment of chronic hepatitis B.
Butetamate is a cough suppressant. It exerts antispasmodic, bronchodilator and anticholinergic properties.
Status:
Possibly Marketed Outside US
Source:
NCT04595916: Phase 4 Interventional Completed Acute Drug Induced Liver Injury
(2020)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Magnesium isoglycyrrhizinate is a magnesium salt form of isoglycyrrhizinate, a derivative of glycyrrhizic acid extracted from the roots of the plant Glycyrrhiza glabra. Magnesium isoglycyrrhizinate has anti-inflammatory, antioxidant and hepatoprotective activities. The drug is believed to be a free radical scavenger and to modulate the activity of hepatic enzymes. Magnesium isoglycyrrhizinate was investigated in clinical trials to restore hepatic impairments caused by chemotherapy drugs and as a treatment of chronic liver diseases.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (UNKNOWN)

Vinylbital is a barbiturate derivative. It was introduced into therapy in 1963 and used as a sedative and in the treatment of insomnia.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)

Exiproben is a choleretic drug marketed in Italy in the 1970s under the trademark of Etopalin and Droctil. When administered, exiproben potently stimulates the production of bile.

Showing 31371 - 31380 of 31824 results