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

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Showing 381 - 390 of 420 results

Iproniazid is a non-selective, irreversible monoamine oxidase inhibitor (MAO) of the hydrazine class. It was originally developed for the treatment of Tuberculosis, but in 1952, its antidepressant properties were discovered when researchers noted that patients given isoniazid became inappropriately happy. Iproniazid is no longer clinically prescribed and has been withdrawn due to incidences of hepatotoxicity.
Status:
US Previously Marketed
Source:
Ilidar by Hoffmann-La Roche
(1954)
Source URL:
First approved in 1954
Source:
Ilidar by Hoffmann-La Roche
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


AZAPETINE, a benzazepine derivative, is an alpha-1 adrenoceptor antagonist. It is a potent arterial vasodilator in the treatment of peripheral vascular diseases.
Status:
US Previously Marketed
Source:
CO-PYRONIL PYRROBUTAMINE NAPHTHALENE DISULFONATE by DISTA PRODUCTS
(1961)
Source URL:
First approved in 1952
Source:
Pyronil by Lilly
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

PYRROBUTAMINE is a potent H1-antihistamine. H1-antihistamines interfere with the agonist action of histamine at the H1 receptor and are administered to attenuate the inflammatory process in order to treat conditions such as allergic rhinitis, allergic conjunctivitis, and urticaria.
Status:
US Previously Marketed
First approved in 1951
Source:
Paveril Phosphate by Lilly
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Dimoxyline is the synthetic analogue of papaverine, Acute toxicity studies show it to be less toxic than papaverine. No analgesic action and no tolerance development in experimental animals by repeated administration. But Dimoxyline does not appear to be as potent as papaverine in comparable dosage. Dimoxyline is indicated for the treatment of patients with angina pectoris. Also, significant amount of benefit was claimed in patients with acute or chronic phlebitis, arterial thrombosis or embolism, Raynaud’s phenomena and early thromboangiitis obliterans or arteriosclerosis obliterans. Detected adverse events are: nausea or abdominal cramps.
Status:
US Previously Marketed
First approved in 1950
Source:
PIG SWIGFOR SWINE AND POULTRY by LeGear Animal Health
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Piperazine, a six membered nitrogen containing heterocycle, is of great significance to the rational design of drugs. This moiety can be found in a plethora of well-known drugs with various therapeutic uses, such as antipsychotic, antihistamine, antianginal, antidepressant, anticancer, antiviral, cardio protectors, anti-inflammatory, and imaging agents. Slight modification to the substitution pattern on the piperazine nucleus facilitates a recognizable difference in the medicinal potential of the resultant molecules. Piperazine has been used as an antihelmintic drug. Piperazine works by paralyzing the worms. They are then passed in the stool.
Status:
US Previously Marketed
Source:
My-B-Den by Bischoff (Dome)
(1949)
Source URL:
First approved in 1949
Source:
My-B-Den by Bischoff (Dome)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Adenosine monophosphate (AMP) is a nucleotide, consisting of a phosphate group, the sugar ribose, and the nucleobase adenine. AMP is an activator of several enzymes in the tissues. In the glycolytic pathway, the enzyme phosphofructokinase is inhibited by ATP but the inhibition is reversed by AMP, the deciding factor for the reaction being the ratio between ATP and AMP. In medicine, AMP is used mainly as an alternative to adenosine for treatment of ischemia and as a tool compound to measure hyperresponsiveness of airways.
Status:
US Previously Marketed
Source:
My-B-Den by Bischoff (Dome)
(1949)
Source URL:
First approved in 1949
Source:
My-B-Den by Bischoff (Dome)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Adenosine monophosphate (AMP) is a nucleotide, consisting of a phosphate group, the sugar ribose, and the nucleobase adenine. AMP is an activator of several enzymes in the tissues. In the glycolytic pathway, the enzyme phosphofructokinase is inhibited by ATP but the inhibition is reversed by AMP, the deciding factor for the reaction being the ratio between ATP and AMP. In medicine, AMP is used mainly as an alternative to adenosine for treatment of ischemia and as a tool compound to measure hyperresponsiveness of airways.
Status:
US Previously Marketed
First approved in 1948
Source:
Antistine Phosphate by Ciba
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Antazoline is an antagonist of histamine H1 receptors. It selectively bind to but does not activate histamine H1 receptors, thereby blocking the actions of endogenous histamine, which subsequently leads to temporary relief of the negative symptoms brought on by histamine. Antazoline in combination with naphazoline (VASOCON-A®) is indicated to relieve the symptoms of allergic conjunctivitis.
Status:
US Previously Marketed
Source:
Oralator by Smith Kline & French
(1946)
Source URL:
First approved in 1946
Source:
Oralator by Smith Kline & French
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Octodrine is a stimulant that is structurally similar to amphetamine and is included in several so-called “pre-workout” and “fat-burning” supplements. Octodrine, has a history of use as a pharmaceutical drug. It was originally developed in the United States as an aerosolized treatment for bronchitis, laryngitis and other conditions Initially approved by the FDA in 1946 as Eskay’s Oralator, this inhaler appeared only in the 1949 edition of the Physicians’ Desk Reference. Octodrine was combined with several other medications, including theophylline, 3-octopamine, and adenosine, in multi-ingredient tablets sold between the early 1960s through the mid-2000s under the trade names Ambredin, Ordinal, Ordinal Retard and Ordinal Forte. Some proponents say octodrine is a safer alternative to other stimulants like ephedra and Dimethylamylamine (DMAA), but there is no scientific information to support this claim. Originally developed in the early 1950’s as a remedy to nasal congestion and as a possible anti-tumor drug, Octodrine has resurfaced as a key ingredient in dietary supplements for its stimulant and thermogenic benefits.
Status:
US Previously Marketed
Source:
Strychnine U.S.P.
(1921)
Source URL:
First marketed in 1921
Source:
Strychnine U.S.P.
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Strychnine is an indole alkaloid obtained from the seeds of the Indian tree Strychnos nux-vomica. It gets its scientific name “strychnos” from Carl Linnaeus, who classified it back in 1753, but it was known to the population of India way before then. Nux vomica originates in India. Strychnine-containing baits are currently labelled for below-ground use and are intended for the control of pocket gophers. Their use as indoor pesticides has been eliminated since 1989. In the past, strychnine has been used as a pesticide to control rats, moles, gophers, and coyotes. Strychnine is highly toxic to most domestic animals. Strychnine is a competitive antagonist at glycine receptors and thus a convulsant. It has been used as an analeptic, in the treatment of nonketotic hyperglycinemia and sleep apnea.

Showing 381 - 390 of 420 results