Details
| Stereochemistry | UNKNOWN |
| Molecular Formula | C19H25NO2 |
| Molecular Weight | 299.4073 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 0 / 3 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CC(CCC1=CC=CC=C1)NC(C)C(O)C2=CC=C(O)C=C2
InChI
InChIKey=PTGXAUBQBSGPKF-UHFFFAOYSA-N
InChI=1S/C19H25NO2/c1-14(8-9-16-6-4-3-5-7-16)20-15(2)19(22)17-10-12-18(21)13-11-17/h3-7,10-15,19-22H,8-9H2,1-2H3
DescriptionSources: https://www.drugs.com/cons/nylidrin.htmlCurator's Comment: Description was created based on several sources, including http://eci2012.net/product/arlidin/
Sources: https://www.drugs.com/cons/nylidrin.html
Curator's Comment: Description was created based on several sources, including http://eci2012.net/product/arlidin/
Nylidrin (Buphenine, Arlidin) is a beta-adrenergic agonist. Nylidrin causes peripheral vasodilation, a positive inotropic effect, and increased gastric volume of gastric juice. It is used in the treatment of peripheral vascular disorders and premature labor. In peripheral vascular disorders, Arlidin (nylidrin HCl) increases walking ability and promotes healing of trophic ulcers. Nylidrin hydrochloride acts predominantly by beta-receptor stimulation. Beta stimulation with nylidrin has been demonstrated in a variety of isolated tissues from rabbits, guinea pigs and dogs. It has been shown to dilate arterioles in skeletal muscle and to increase cardiac output in the anesthetized dog and cat and in unanesthetized man. An increase in cerebral blood flow and a decrease in vascular resistance has also been reported. The result of this combination of actions is a greater blood supply to ischemic tissues, with usually minimal change in blood pressure. Arlidin may be of benefit in elderly patients with mild to moderate symptoms that are commonly associated with organic mental disorders. Short-term (3 months’ duration) and long-term (12 months’ duration) clinical studies have demonstrated a modest improvement in ability to perform general activities of daily living, self-care and in a capability for social interactions. The mechanism whereby nylidrin may provide relief of selected symptoms in some elderly patients with organic brain disorders is not known.
Originator
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL2096666 Sources: http://www.ncbi.nlm.nih.gov/pubmed/9430414 |
0.18 µM [IC50] | ||
Target ID: CHEMBL2096680 Sources: http://www.ncbi.nlm.nih.gov/pubmed/9430414 |
32.0 µM [IC50] | ||
Target ID: CHEMBL2096911 Sources: http://www.ncbi.nlm.nih.gov/pubmed/9430414 |
42.0 µM [IC50] | ||
Target ID: CHEMBL1907610 Sources: http://www.ncbi.nlm.nih.gov/pubmed/2997229 |
7.1 nM [Kd] | ||
Target ID: CHEMBL210 Sources: http://www.genome.jp/dbget-bin/www_bget?dr:D01543 |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | Arlidin Approved UseMay be of benefit in elderly patients with mild to moderate symptoms that are commonly associated with organic mental disorders. |
|||
| Primary | Arlidin Approved UsePeripheral vascular disease, intermittant claudication, thrombophlebitis, TAO, frost bite, nocturnal leg cramps. |
Doses
| Dose | Population | Adverse events |
|---|---|---|
120 mg single, oral Overdose |
unknown, 14 years |
Other AEs: Chest pain, Headache... Other AEs: Chest pain (1 patient) Sources: Headache (1 patient) Flushing (1 patient) Shortness of breath (1 patient) |
6 mg 2 times / day multiple, oral Dose: 6 mg, 2 times / day Route: oral Route: multiple Dose: 6 mg, 2 times / day Sources: |
unhealthy, 32 years |
|
50 mg/min multiple, intravenous Dose: 50 mg/min Route: intravenous Route: multiple Dose: 50 mg/min Sources: |
pregnant |
AEs
| AE | Significance | Dose | Population |
|---|---|---|---|
| Chest pain | 1 patient | 120 mg single, oral Overdose |
unknown, 14 years |
| Flushing | 1 patient | 120 mg single, oral Overdose |
unknown, 14 years |
| Headache | 1 patient | 120 mg single, oral Overdose |
unknown, 14 years |
| Shortness of breath | 1 patient | 120 mg single, oral Overdose |
unknown, 14 years |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Profiling of a prescription drug library for potential renal drug-drug interactions mediated by the organic cation transporter 2. | 2011-07-14 |
|
| Age-related macular degeneration and nutritional supplementation: a review of randomised controlled trials. | 2003-09 |
|
| Development and use of a computer program to detect potentially inappropriate prescribing in older adults residing in Canadian long-term care facilities. | 2002-10-14 |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: http://www.medbroadcast.com/Drug/GetDrug/Arlidin
The recommended dose of nylidrin is 12 mg to 24 mg daily in 3 or 4 divided doses for certain types of mental disorders. For blood vessel disorders of the legs, the recommended adult dose is 12 mg to 48 mg daily in 3 to 4 divided doses.
Route of Administration:
Oral
In Vitro Use Guide
Sources: http://www.ncbi.nlm.nih.gov/pubmed/9430414
Nylidrin was a potent (IC50 = 0.18 uM) antagonist of rat NR1A/2B receptors expressed in Xenopus oocytes
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ACTIVE MOIETY