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

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Showing 10051 - 10060 of 10251 results

Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)

Metizoline is an adrenergic agent with vasoconstrictor properties. It has been used as the active component of nasal decongestant spray (Ellsyl).
Status:
Possibly Marketed Outside US
Source:
SOFRAMYCIN by Waksman, S.A. et al.
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Framycetin is a component of neomycin that is produced by Streptomyces fradiae. Framycetin is used for the treatment of bacterial eye infections such as conjunctivitis. Framycetin is an antibiotic. It is not active against fungi, viruses and most kinds of anaerobic bacteria. Framycetin works by binding to the bacterial 30S ribosomal subunit, causing misreading of t-RNA, leaving the bacterium unable to synthesize proteins vital to its growth. Framycetin is useful primarily in infections involving aerobic bacteria bacteria. Framycetin binds to specific 30S-subunit proteins and 16S rRNA, four nucleotides of 16S rRNA and a single amino acid of protein S12. This interferes with decoding site in the vicinity of nucleotide 1400 in 16S rRNA of 30S subunit. This region interacts with the wobble base in the anticodon of tRNA. This leads to interference with the initiation complex, misreading of mRNA so incorrect amino acids are inserted into the polypeptide leading to nonfunctional or toxic peptides and the breakup of polysomes into nonfunctional monosomes. Framycetin is a component of SOFRACORT (Framycetin sulphate - Gramicidin-dexamethasone), indicated for the treatment of blepharitis and infected eczema of the eyelid; allergic, infective and rosacea conjunctivitis; rosacea keratitis; scleritis and episcleritis; iridocyclitis, and other inflammatory conditions of the anterior segment of the eye, as well as otitis externa (acute and chronic) and other inflammatory and sebhorrheic conditions of the external ear.
Amezinium is a sympathomimetic used for its vasopressor effects in the treatment of hypotensive states. Amezinium inhibited monoamine oxidase (MAO) activity. Amezinium antagonized the response to tyramine and blocked neuronal uptake of noradrenaline. Side effects revealed are: palpitation, headache, nausea/vomiting, hot flashes, high blood pressure.
Pyridoxamine (PM) is one of three natural forms of vitamin B6. It is a critical transient intermediate in catalysis of transamination reactions by vitamin B6-dependent enzymes. In preclinical or clinical trials PM has demonstrated pharmacological potential for treatment of diabetic nephropathy, diabetic retinopathy, and hyperlipidemia, and for use in kidney stone preventive therapies. Although its precise mode of action in vivo is not yet clear, it is likely that at least three mechanisms are at play: inhibition of post-Amadori steps of the Maillard reaction; scavenging of reactive carbonyl compounds; and inhibition of toxic effects of ROS. Pyridoxamine was marketed as a dietary supplement, often as the hydrochloride salt, pyridoxamine dihydrochloride. However, in the United States, the FDA ruled in January 2009 that pyridoxamine must be regulated as a pharmaceutical drug because it is the active ingredient in Pyridorin, a drug designed to prevent the progression of diabetic nephropathy.
Status:
Possibly Marketed Outside US
Source:
Alloferin by Hoffman-La Roche
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Alcuronium (diallylnortoxiferine) is a semi-synthetic substance prepared from C-toxiferine I a bis-quaternary alkaloid obtained from Strychnos toxifera. Alcuronium is a neuromuscular blocking (NMB) agent, alternatively referred to as a skeletal muscle relaxant. Alcuronium is used for endotracheal intubation and to produce muscle relaxation in general anesthesia during surgical procedures. The pharmacological action of alcuronium is readily reversed by neostigmine, and it produced little histamine release. The major disadvantage of alcuronium is that it elicits a vagolytic effect produced by a selective atropine-like blockade of cardiac muscarinic receptors.

Class (Stereo):
CHEMICAL (ACHIRAL)


Bisdequalinium (also known as R-199, trade name Solvidont) is an antibacterial agent for endodontic use. Bisdequalinium was available in three dispensing forms: an irrigation solution, a working solution, and a medication paste. They contained 0.125 %, 0.5 %, and 0.48 % Bisdequalinium respectively. The low cytotoxicity and high antimicrobial effects, detergent, and lubricating and chelating properties, all claimed in the manufacturer's brochure, make this material an appropriate candidate for clinical endodontic use.
Pyridoxamine (PM) is one of three natural forms of vitamin B6. It is a critical transient intermediate in catalysis of transamination reactions by vitamin B6-dependent enzymes. In preclinical or clinical trials PM has demonstrated pharmacological potential for treatment of diabetic nephropathy, diabetic retinopathy, and hyperlipidemia, and for use in kidney stone preventive therapies. Although its precise mode of action in vivo is not yet clear, it is likely that at least three mechanisms are at play: inhibition of post-Amadori steps of the Maillard reaction; scavenging of reactive carbonyl compounds; and inhibition of toxic effects of ROS. Pyridoxamine was marketed as a dietary supplement, often as the hydrochloride salt, pyridoxamine dihydrochloride. However, in the United States, the FDA ruled in January 2009 that pyridoxamine must be regulated as a pharmaceutical drug because it is the active ingredient in Pyridorin, a drug designed to prevent the progression of diabetic nephropathy.
Status:
Possibly Marketed Outside US
Source:
Probicromil by ZYF Pharm Chemical
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Probicromil is a Histamine H1 antagonist. It was taken to the clinic and found to be effective in exercise and antigen challenge. Probicromil inhibited Ascaris-induced bronchoconstriction and the increase in plasma histamine levels seen after Ascaris inhalation. Therapeutic efficacy in seasonal rhinitis was also demonstrated. Further clinical studies were halted because of a side-effect associated with the compound, namely a sensation of warmth (especially in the perineal region) experienced by some volunteers after inhalation.
Status:
Possibly Marketed Outside US
Source:
CAMTOBELL by Chong Kun Dang Research Institute
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Belotecan is a semisynthetic analogue of camptothecin containing a 2-(N-isopropylamino) ethyl group linkage at position C-7 of the camptothecin ring. It stabilizes the complex formed between topoisomerase I and DNA, thereby preventing the religation of DNA breaks. This leads to an inhibition of DNA replication and triggers apoptotic cell death. Belotecan was approved in Korea under the name Camtobell for the treatment of patients with ovarian and small cell lung cancers.
Dimebon (latrepirdine) is an orally available, small molecule, gamma carboline derivative that was developed and used in Russia as an over-the-counter oral antihistamine for allergy treatment since 1980s. In 1990s it was shown that Dimebon has promising potential in treating neurodegenerative diseases. In 2003, Medivation Inc acquired the rights to Dimebon. Medivation went public in December 2004, with Dimebon as the only drug in its pipeline. The product was being developed by Medivation and Pfizer as a treatment for early-stage Alzheimer's disease and Huntington's disease. However, development was discontinued by Medivation and Pfizer in early 2012. Dimebon inhibits alpha-Adrenergic receptors (alpha1A, alpha1B, alpha1D, and alpha2A), Histamine H1 and H2 receptors and Serotonin 5-HT2c, 5-HT5A, 5-HT6 receptors with high affinity. Dimebon may act by blocking NMDA receptors or voltage-gated Ca2+ channels and by preventing mitochondrial permeability pore transition.

Showing 10051 - 10060 of 10251 results