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

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Showing 81 - 90 of 162 results

Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)



SB-273005 is one in a series of orally active nonpeptide vitronectin αvβ3 inhibitors. SB-273005 had been in phase I clinical trials by GlaxoSmithKline for the treatment of postmenopausal osteoporosis and rheumatoid arthritis (RA). However, this research has been discontinued.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

AMG-517, a potent and selective vanilloid receptor (VR1) antagonist, was in clinical trials with Amgen for the treatment of pain. AMG 517 inhibits CAP- (500 nM), acid- (pH 5.0), or heat-(45 °C) induced 45Ca2+ influx into human TRPV1-expressing CHO Cells with IC50 of 0.76 nM, 0.62 nM and 1.3 nM. AMG-517 blocks capsaicin-, proton-, and heat-induced inward currents in TRPV1-expressing cells similarly. AMG-517 inhibits native TRPV1 activation by capsaicin in rat dorsal root ganglion neurons with an IC50 value of 0.68 nM. Oral administration of AMG-517 produces a dose-dependent increase in plasma concentrations, it also produces a dose-dependent decrease in the number of flinches induced by capsaicin treatment. The minimally effective dose (MED), based on a statistically significant difference in number of flinches from the vehicle versus capsaicin-administered group, is 0.3 mg/kg for AMG 517. The corresponding plasma concentrations are 90 to 100 ng/mL for AMG-517. AMG-517 (3 mg/kg) exhibits significant reductions in capsaicin-induced flinch up to 24 h after dosing. AMG 517 blocks thermal hyperalgesia in CFA model of pain. Unfortunately, clinical studies of AMG-517 were discontinued due to the hyperthermia observed after exposure to single and multiple doses.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

6-amino-penicillanic acid is a common parent amine of various penicillins. 6-amino-penicillinic acid possesses definite antibacterial properties but these are much lower order than these of benzylpenicillin. It is destroyed by penicillinase (Beta-lactamase). The first penicillins to appear as derivatives of 6-APA were in fact phenethicillin and propicillin.
Status:
US Previously Marketed
Source:
Allercur by Roerig (Pfizer)
(1960)
Source URL:
First approved in 1960
Source:
Allercur by Roerig (Pfizer)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Clemizole is a drug in clinical development for the treatment of hepatitis C virus (HCV) infection. Clemizole is a novel inhibitor of TRPC5 channels. Clemizole is an H1 antagonist. Clemizole, an antihistamine drug that was once widely used for treatment of allergic disease, was recently discovered to be a potent inhibitor (IC50, 24 nM) of the interaction between an HCV protein (NS4B) and HCV RNA. Although clemizole was widely used during the 1950s and 1960s, this was before contemporary regulatory requirements were established for new drug development, and there is very minimal information about its pharmacokinetics and metabolism.
Status:
US Previously Marketed
Source:
Compocillin-V by Abbott
(1954)
Source URL:
First approved in 1954
Source:
Compocillin-V by Abbott
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


PENICILLIN V HYDRABAMINE, a semi-synthetic antibiotic, is used for the treatment of mild to moderately severe infections (e.g. dental infection, infections in the heart, middle ear infections, rheumatic fever, scarlet fever, skin infections, upper and lower respiratory tract infections) caused by susceptible, usually gram-positive, organisms.
Status:
US Previously Marketed
Source:
Compocillin by Abbott
(1954)
Source URL:
First approved in 1954
Source:
Compocillin by Abbott
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


PENICILLIN G HYDRABAMINE, a semi-synthetic antibiotic, is used for the treatment of infections caused by susceptible, usually gram-positive, organisms.
Status:
US Previously Marketed
Source:
Pabalate by Robins
(1949)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



AMINOBENZOATE SODIUM is a salt of Aminobenzoic acid. Aminobenzoic acid is an intermediate in the synthesis of folate by bacteria, plants, and fungi. Many bacteria, including those found in the human intestinal tract such as E. coli, generate Aminobenzoic acid from chorismate by the combined action of the enzymes 4-amino-4-deoxychorismate synthase and 4-amino-4-deoxychorismate lyase. Plants produce Aminobenzoic acid in their chloroplasts, and store it as a glucose ester (pABA-Glc) in their tissues. Humans lack the enzymes to convert Aminobenzoic acid to folate, so require folate from dietary sources such as green leafy vegetables. In humans, Aminobenzoic acid is considered nonessential and, although it has been referred to historically as "vitamin Bx", is no longer recognized as a vitamin, because most people have colon bacteria that generate Aminobenzoic acid. The potassium salt is used as a drug against fibrotic skin disorders, such as Peyronie's disease, under the trade name Potaba.
Procaine is an anesthetic agent indicated for production of local or regional anesthesia, particularly for oral surgery. Procaine (like cocaine) has the advantage of constricting blood vessels which reduces bleeding, unlike other local anesthetics like lidocaine. Procaine is an ester anesthetic. It is metabolized in the plasma by the enzyme pseudocholinesterase through hydrolysis into para-aminobenzoic acid (PABA), which is then excreted by the kidneys into the urine. Procaine acts mainly by inhibiting sodium influx through voltage gated sodium channels in the neuronal cell membrane of peripheral nerves. When the influx of sodium is interrupted, an action potential cannot arise and signal conduction is thus inhibited. The receptor site is thought to be located at the cytoplasmic (inner) portion of the sodium channel. Procaine has also been shown to bind or antagonize the function of N-methyl-D-aspartate (NMDA) receptors as well as nicotinic acetylcholine receptors and the serotonin receptor-ion channel complex.
Status:
US Previously Marketed
Source:
55 FR 33254 corn/callus remover phenoxyacetic acid
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Phenoxyacetic acid is found in cocoa and cocoa products. Phenoxyacetic acid is a flavouring ingredient. Phenoxyacetic acid is on the FDA list of approved food additives (PART 172 - FOOD ADDITIVES PERMITTED FOR DIRECT ADDITION TO FOOD FOR HUMAN CONSUMPTION; Subpart F--Flavoring Agents and Related Substances Sec. 172.515 Synthetic flavoring substances and adjuvants.). Research has shown that Phenoxyacetic acid induced hematopoietic cell proliferation, providing potential for oral therapeutics which stimulate proliferation of hematopoietic cells of multiple lineages, as well as inducing fetal globin, important for therapy of hemoglobinopathies.