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

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Showing 61 - 70 of 171 results

Ifenprodil (marketed under the brands Vadilex; Dilvax; Creocral; Cerocral) is a selective NMDA receptor (glutamate) antagonist. Additionally, ifenprodil inhibits GIRK channels, and interacts with alpha1 adrenergic, serotonin, and sigma receptors. Ifenprodil acts as a vasodilator. Ifenprodil is a medicine available in a number of countries worldwide, but not in US.
Status:
Possibly Marketed Outside US
Source:
Pirroksan by All-Union Scientific-Research Chemical-Pharmaceutical Institute
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Proroxan is a non-selective а-adrenoblocker. Proroxan was found to prevent the development of hypertensive crises and improve cerebral bioelectrical parameters in most of hypertensive patients. Proroxan has been used as an antihypertensive and in the treatment of Ménière’s disease, motion sickness, and allergic dermatitis.
Status:
Possibly Marketed Outside US
Source:
Unknown by Kowa
Source URL:

Class (Stereo):
CHEMICAL (UNKNOWN)



Nipradilol is a beta blocker and nitric oxide donor. It was launched in Japan in 1988. This medicine lowers intraocular pressure by suppressing aqueous production and increasing fluid drainage from the eye. It is usually used to treat glaucoma and intraocular hypertension. The most commonly reported adverse reactions include conjunctival congestion, superficial keratitis, eye irritation, bloodshot eyes, itch and headache. If any of these symptoms occur, consult with your doctor or pharmacist.
Status:
Possibly Marketed Outside US
Source:
Lofexidine by Nattermann & Cie
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Levlofexidine is R-enantiomer of a α2A adrenergic receptor agonist Lofexidine. Levlofexidine (as a component of Lofexidine) can be used as a short-acting anti-hypertensive but is mostly used to help relieve symptoms of heroin or opiate withdrawal in opiate dependency. Lofexidine is approved in the United Kingdom but is still undergoing clinical trials in the United States. Levlofexidine showed an approximately 9-fold higher affinity than Dexlofexidine for the alpha 2-adrenoceptor-like binding sites in rat brain membranes identified by [3H]-clonidine and was 4 times more potent at displacing [3H]-prazosin from alpha 1-adrenoceptors. The possibility of using lofexidine to treat alcohol addiction withdrawal symptoms has been investigated and has not yet been shown to be an effective treatment.
Status:
Possibly Marketed Outside US
Source:
Nevadral Retard
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Norfenefrine or meta-octopamine, also known as 3,β-dihydroxyphenethylamine, is an adrenergic agent used as a sympathomimetic drug which is marketed in Europe, Japan, and Mexico. Along with its structural isomer p-octopamine and the tyramines, norfenefrine is a naturally occurring, endogenous trace amine and plays a role as a minor neurotransmitter in the brain. Norfenefrine controls blood pressure in acute hypotensive states eg pheochromocytomectomy, sympathectomy, poliomyelitis, spinal anesth, MI, septicemia, blood transfusion and drug reactions. Adjunct in treatment of cardiac arrest and hypotension.
Status:
Possibly Marketed Outside US
Source:
NCT02307396: Phase 4 Interventional Completed Schizophrenia
(2015)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Zuclopenthixol is indicated the management of the manifestations of schizophrenia and other mental illnesses with disturbances in thinking, emotional reactions and behaviour. It is also used to treat the manic phase of manic depressive illness. Zuclopenthixol, a thioxanthene derivative, has high affinity for both dopamine D1 receptors and dopamine D2 receptors. Zuclopenthixol also has high affinity for α1-adrenergic and 5-HT2 receptors. Zuclopenthixol (CLOPIXOL®) is avavilable in the form of tablets and solution for intramuscular injections.
Flupenthixol is a thioxanthene antipsychotic used in the treatment of schizophrenia and other psychoses, with the exception of mania and psychomotor hyperactivity due to an activating effect associated with this drug. It may also be employed as an antidepressant. Flupenthixol has a wide range of pharmacological actions. Flupenthixol blocks dopaminergic receptors, thus interfering with dopaminergic transmission in the brain. Flupenthixol also inhibits serotonin 5-HT, histamine H1, muscarinic and alpha-1 adrenergic receptors.
The Rauwolfia alkaloid, raubasine (ajmalicine), has been found to have broad application in the treatment of circulatory diseases, especially in the relief of obstruction of normal cerebral blood flow. In combination with other Rauwolfia alkaloids it has been used to lower high blood pressure. Raubasine is an antihypertensive drug used in the treatment of high blood pressure. It has been marketed under numerous brand names including Card-Lamuran, Circolene, Cristanyl, Duxil, Duxor, Hydroxysarpon, Iskedyl, Isosarpan, Isquebral, Lamuran, Melanex, Saltucin Co, Salvalion, and Sarpan. Raubasine acts as a α1-adrenergic receptor antagonist.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)



Adrafinil (CRL 40028) was synthesized by Louis Lafon Laboratories. The proprietary name of adrafinil is Olmifon®; its chemical name is (diphenylmethyl )sulfinyl-2-acetohydroxamic acid. Adrafinil is metabolized to modafinil. Adrafinil and modafinil both serve as α1-adrenergic–receptor agonists. The evidence in support of this hypothesis, however, is weak, and other mechanisms of action are probable. Adrafinil may modify the intracerebral release of amino acids (both GABA and glutamate) and adrafinil may increase cerebral metabolism. Olmifon ® tablets, 300 mg (adrafinil) were indicated for the treatment of disorders of vigilance, attention, and ideo-motor slowing in the elderly. It has been marketed in France since September 19, 1985. Cephalon announced their intent to stop marketing the drug, and has discontinued production and marketing of Olmifon in September 2011. Adrafinil is marketing as nootropic supplement to improve cognitive functions.
Status:
First approved in 1997

Class (Stereo):
CHEMICAL (ABSOLUTE)



Tamsulosin, a sulfamoylphenethylamine-derivative alpha-adrenoceptor blocker with enhanced specificity for the alpha-adrenoceptors of the prostate, is commonly used to treat benign prostatic hyperplasia (BPH). The drug is commercially available in a racemic mixture of 2 isomers, and is pharmacologically related to doxazocin, prazosin, and terazosin. However, unlike these drugs, tamsulosin has a higher affinity for the alpha-1A- adrenergic receptors, which are located in vascular smooth muscle. Studies show that tamsulosin has about 12 times greater affinity for alpha-1 adrenergic receptors in the prostate than those in the aorta, which may result in a reduced incidence of adverse cardiovascular effects. Tamsulosin is sold under the trade name Flomax.