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

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Showing 13391 - 13400 of 14117 results

Methaqualone is a depressant that modulates the activity of the GABA receptors in the brain and nervous system. It promotes relaxation, sleepiness and sometimes a feeling of euphoria. It causes a drop in blood pressure and slows the pulse rate. These properties are the reason why it was initially thought to be a useful sedative and anxiolytic. Common side effects of Methaqualone include dizziness, nausea, vomiting, diarrhea, abdominal cramps, fatigue, itching, rashes, sweating, dry mouth, tingling sensation in arms and legs, seizures and its depressant effects include reduced heart rate and respiration. The drug became banned in many countries and was withdrawn from many markets in the early 1980s.
Methysergide is an oral, synthetic ergot alkaloid, structurally related to the oxytocic agent methylergonovine and to the potent hallucinogen LSD. Methysergide is used prophylactically to reduce the frequency and intensity of severe vascular headaches. Although methysergide is an ergot alkaloid, it is a weak vasoconstrictor and oxytocic. Methysergide is a more potent antagonist of peripheral serotonin receptors than other ergot alkaloids. Methysergide is not just a 5HT2 antagonist, it is also a 5HT1 agonist. Although methysergide and sumatriptan both stimulate serotonin receptors centrally, methysergide is intended for prophylaxis while sumatriptan is indicated for treatment of an acute attack. Methysergide was approved by the FDA in 1962. Methysergide was formerly used for prophylaxis of cluster headaches/migraine headaches, but is no longer recommended due to retroperitoneal/retropulmonary fibrosis.
Methysergide is an oral, synthetic ergot alkaloid, structurally related to the oxytocic agent methylergonovine and to the potent hallucinogen LSD. Methysergide is used prophylactically to reduce the frequency and intensity of severe vascular headaches. Although methysergide is an ergot alkaloid, it is a weak vasoconstrictor and oxytocic. Methysergide is a more potent antagonist of peripheral serotonin receptors than other ergot alkaloids. Methysergide is not just a 5HT2 antagonist, it is also a 5HT1 agonist. Although methysergide and sumatriptan both stimulate serotonin receptors centrally, methysergide is intended for prophylaxis while sumatriptan is indicated for treatment of an acute attack. Methysergide was approved by the FDA in 1962. Methysergide was formerly used for prophylaxis of cluster headaches/migraine headaches, but is no longer recommended due to retroperitoneal/retropulmonary fibrosis.
Status:
US Previously Marketed
Source:
ISOETHARINE HYDROCHLORIDE by ASTRAZENECA
(1984)
Source URL:
First approved in 1961
Source:
Bronkosol by Sterling
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Isoetharine is a beta-2 adrenergic receptor agonist, which was developed by Max Bockmuhl, Gustav Erhart and Leonhard Stein at the Hochst laboratories of I.G. Farbenindustrie in 1934. By binding to beta-2 adrenergic receptors on bronchial cell membranes, isoetharine increases the level of cAMP and thus stimulates the relaxation of smooth-muscle cells, stabilizes mast cells and inhibits histamine release. Isoetharine was approved by FDA for the symptomatic relief of bronchiospasms in patients with chronic bronchitis or emphysema (aerosol and solution for inhalation), however, later on the drug was discontinued.
Status:
US Previously Marketed
Source:
ISOETHARINE HYDROCHLORIDE by ASTRAZENECA
(1984)
Source URL:
First approved in 1961
Source:
Bronkosol by Sterling
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Isoetharine is a beta-2 adrenergic receptor agonist, which was developed by Max Bockmuhl, Gustav Erhart and Leonhard Stein at the Hochst laboratories of I.G. Farbenindustrie in 1934. By binding to beta-2 adrenergic receptors on bronchial cell membranes, isoetharine increases the level of cAMP and thus stimulates the relaxation of smooth-muscle cells, stabilizes mast cells and inhibits histamine release. Isoetharine was approved by FDA for the symptomatic relief of bronchiospasms in patients with chronic bronchitis or emphysema (aerosol and solution for inhalation), however, later on the drug was discontinued.
Status:
US Previously Marketed
Source:
ISOETHARINE HYDROCHLORIDE by ASTRAZENECA
(1984)
Source URL:
First approved in 1961
Source:
Bronkosol by Sterling
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Isoetharine is a beta-2 adrenergic receptor agonist, which was developed by Max Bockmuhl, Gustav Erhart and Leonhard Stein at the Hochst laboratories of I.G. Farbenindustrie in 1934. By binding to beta-2 adrenergic receptors on bronchial cell membranes, isoetharine increases the level of cAMP and thus stimulates the relaxation of smooth-muscle cells, stabilizes mast cells and inhibits histamine release. Isoetharine was approved by FDA for the symptomatic relief of bronchiospasms in patients with chronic bronchitis or emphysema (aerosol and solution for inhalation), however, later on the drug was discontinued.
Status:
US Previously Marketed
Source:
ISOETHARINE HYDROCHLORIDE by ASTRAZENECA
(1984)
Source URL:
First approved in 1961
Source:
Bronkosol by Sterling
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Isoetharine is a beta-2 adrenergic receptor agonist, which was developed by Max Bockmuhl, Gustav Erhart and Leonhard Stein at the Hochst laboratories of I.G. Farbenindustrie in 1934. By binding to beta-2 adrenergic receptors on bronchial cell membranes, isoetharine increases the level of cAMP and thus stimulates the relaxation of smooth-muscle cells, stabilizes mast cells and inhibits histamine release. Isoetharine was approved by FDA for the symptomatic relief of bronchiospasms in patients with chronic bronchitis or emphysema (aerosol and solution for inhalation), however, later on the drug was discontinued.
Status:
US Previously Marketed
First approved in 1961

Class (Stereo):
CHEMICAL (ABSOLUTE)



Dromostanolone Propionate (known by the brand names Masteron and Drolban) was invented by Syntex in 1959. About 10 years later it was released on the American market by Lilly as brand name Drolban. The drug was first approved in the USA for use as a treatment of female breast cancer. However, the profile of side-effects included pronouncement of male characteristics in women and when more effective breast cancer treatments came to market drostanolone was gradually phased out. No longer used clinically dromostanolone propionate became very popular in the bodybuilding community. Today dromostanolone propionate remains on the list of approved medications, but it is not being manufactured or sold by pharmaceutical companies. It is still produced illegally by underground labs for use in the bodybuilding community.
Status:
US Previously Marketed
Source:
Oxaine by Wyeth
(1960)
Source URL:
First approved in 1960
Source:
Oxaine by Wyeth
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Oxethazaine is a potent local anesthetic. It is administered orally (usually in combination with an antacid) for the relief of pain associated with peptic ulcer disease or esophagitis. Its effectiveness at the acidity of the gastric environment is due to the fact that oxethazaine, a weak base, is relatively non-ionized at pH 1. It is also used topically in the management of hemorrhoid pain. Oral oxetacaine preparations are available in several countries, including India, South Africa and Brazil, but not the United States. It is marketed under the name Strocain in Japan.
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 (ABSOLUTE)



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.

Showing 13391 - 13400 of 14117 results