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

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Showing 281 - 290 of 816 results

Status:
US Previously Marketed
Source:
Mytolon Chloride by Winthrop
(1951)
Source URL:
First approved in 1951
Source:
Mytolon Chloride by Winthrop
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Diphemanil methylsulfate (Prantal), a quarternary amine, is a highly specific parasympathetic blocking agent.
Edrophonium is a short and rapid-acting cholinergic drug. Chemically, edrophonium is ethyl (m-hydroxyphenyl) dimethylammonium. Edrophonium is used for the differential diagnosis of myasthenia gravis and as an adjunct in the evaluation of treatment requirements in this disease. It may also be used for evaluating emergency treatment in myasthenic crises. Because of its brief duration of action, it is not recommended for maintenance therapy in myasthenia gravis. It is also useful whenever a curare antagonist is needed to reverse the neuromuscular block produced by curare, tubocurarine, gallamine triethiodide or dimethyl-tubocurarine. It is not effective against decamethonium bromide and succinylcholine chloride. It may be used adjunctively in the treatment of respiratory depression caused by curare overdosage.
Status:
US Previously Marketed
Source:
HEXAMETHONIUM CHLORIDE HEXAMETHONIUM CHLORIDE by NYSCO
(1961)
Source URL:
First approved in 1951
Source:
Hexameton by Burroughs
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Hexamethonium is a nicotinic cholinergic antagonist. It was used to treat hypertension, but has never been approved and was discontinued because of the non-specified treatment. When this drug tried to use in medical study via inhalation, one of the volunteer died, the death has been described as “particularly disturbing ”because it was a healthy volunteer who had no thing to gain by taking part in the study. This volunteer participated in a study designed to provoke a mild asthma attack in order to help doctors discover the reflex that protects the lungs of healthy people against asthma attacks. Hexamethonium is poorly absorbed from the gastrointestinal tract and does not cross the blood-brain barrier. Now it is widely used a research tool.
Status:
US Previously Marketed
First approved in 1950

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Decamethylene disquaternary salts, with a ten-carbon (C10) chain between the quaternary groups, had the most potent curariform action in the series of polymethylene bisquaternaries. Decamethonium was used clinically as a neuromuscular blocking drug for a short time. Decamethonium was different from d-tubocurarine and that it produced a transient augmentation of contraction. C10 produces neuromuscular block by initiating some active response in the endplate or muscle fibre. Unlike d-tubocurare, decamethonium was not reversed by anticholinesterase agents.
Status:
US Previously Marketed
Source:
Panparnit HCl by Geigy
(1949)
Source URL:
First approved in 1949
Source:
Panparnit HCl by Geigy
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Caramiphen is a muscarinic M1 acetylcholine receptor antagonist, which was used for the treatment of Parkinson Disease and cough, but then there using were discontinued. Caramiphen is also used in local anesthesia, and effect could be achieved through the suppression of voltage-gated Na⁺ currents.
Status:
US Previously Marketed
Source:
Etamon Chloride by Parke-Davis
(1947)
Source URL:
First approved in 1947
Source:
Etamon Chloride by Parke-Davis
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Tetraethylammonium is an experimental drug with no approved indication or marketed formulation. Tetraethylammonium blocks of apamin-sensitive and insensitive Ca2(+)-activated K+ channels. It is a weak agonist of the nicotinic receptor. Tetraethylammonium produces transient reductions in blood pressure. Tetraethylammonium hydroxide is used as a soluble source of hydroxide ions and in the synthesis of ionic organic compounds.
Tubocurarine, a naturally occurring alkaloid, is used to treat smoking withdrawl syndrom. Tubocurarine, the chief alkaloid in tobacco products, binds stereo-selectively to nicotinic-cholinergic receptors at the autonomic ganglia, in the adrenal medulla, at neuromuscular junctions, and in the brain. Two types of central nervous system effects are believed to be the basis of Tubocurarine's positively reinforcing properties. A stimulating effect is exerted mainly in the cortex via the locus ceruleus and a reward effect is exerted in the limbic system. At low doses the stimulant effects predominate while at high doses the reward effects predominate. Intermittent intravenous administration of Tubocurarine activates neurohormonal pathways, releasing acetylcholine, norepinephrine, dopamine, serotonin, vasopressin, beta-endorphin, growth hormone, and ACTH. Tubocurarine competes with acetylcholine for post-synaptic nicotinic NM receptors and blocks them.
Status:
US Previously Marketed
Source:
GUANIDINE HYDROCHLORIDE by MERCK SHARP DOHME
(1939)
Source URL:
First approved in 1939
Source:
GUANIDINE HYDROCHLORIDE by MERCK SHARP DOHME
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Guanidine is a small basic compound. Guanidine stimulates the neuromuscular junction presynaptically by inhibiting voltage-gated potassium (Kv) channels, leading to the enhanced release of acetylcholine in the synaptic cleft. This stimulatory effect of guanidine underlies its use in the therapy for the neuromuscular diseases. The hydrochloride salt of guanidine was approved by FDA for the reduction of the symptoms of muscle weakness and easy fatigability associated with the myasthenic syndrome of Eaton-Lambert.
Adiphenine is a ternary amino ligand. It is used as a local anesthetic that reduces the frequency of acetylcholine-induced single-channel currents. It was originally introduced as a spasmolytic agent. Adiphenine reduced the muscle tone of the gastrointestinal tract, bile duct and gallbladder, bronchi, bladder. It affects the tone of the muscles of the eye, causing the pupil dilated (mydriasis), increased intraocular pressure, and paralysis of accommodation. Influences on the cardiovascular system, causing tachycardia and improving AV-conduction. Adiphenine side effects are: nausea, vomiting, heartburn, dizziness, headache. Adiphenine has not been widely used clinically.

Showing 281 - 290 of 816 results