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Restrict the search for
phenyl aminosalicylate
to a specific field?
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Bepridil (trade name Vascor) is an amine calcium channel blocker used to treat angina. Bepridil is a calcium channel blocker that has well characterized anti-anginal properties and known but poorly characterized type 1 anti-arrhythmic and anti-hypertensive properties. It is not related chemically to other calcium channel blockers such as diltiazem hydrochloride, nifedipine and verapamil hydrochloride. Bepridil has inhibitory effects on both the slow calcium (L-type) and fast sodium inward currents in myocardial and vascular smooth muscle, interferes with calcium binding to calmodulin, and blocks both voltage and receptor operated calcium channels. Bepridil inhibits the transmembrane influx of calcium ions into cardiac and vascular smooth muscle. This has been demonstrated in isolated myocardial and vascular smooth muscle preparations in which both the slope of the calcium dose response curve and the maximum calcium-induced inotropic response were significantly reduced by bepridil. In cardiac myocytes in vitro, bepridil was shown to be tightly bound to actin. Bepridil regularly reduces heart rate and arterial pressure at rest and at a given level of exercise by dilating peripheral arterioles and reducing total peripheral resistance (afterload) against which the heart works. Bepridil is no longer sold in the United States, but it is still marketed in other countries. Bepridil has antihypertensive and selective anti-arrhythmia activities and acts as a calmodulin antagonist. Although, it contains one chiral center, it is generally administered as a racemates. The drug bepridil is a racemic mixture of two enantiomers for the 2R as CID 16048570 and 2S as CID 445143. (R)-isomer of bepridil is more active than (-S)- isomer, in certain cases. In the retrogradely perfused, paced rat heart the higher activity was found for the ( )-enantiomer, which
was 4.27 times more potent in increasing coronary flow than the (-)-isomer. The two enantiomers of bepridil showed a lower activity on maximum systolic left ventricular
pressure (MSLVP) than on coronary flow, and a similar 3-4 fold
stereoselectivity with both parameters.
Status:
Possibly Marketed Outside US
Source:
Loftran by Beecham
Source URL:
Class (Stereo):
CHEMICAL (UNKNOWN)
KETAZOLAM, a benzodiazepine with an additional d-face-fused heterocyclic ring, possesses anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties. It is used for the treatment of anxiety and spasticity.
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Epalrestat is an aldose reductase inhibitor that is approved in Japan for the improvement of subjective neuropathy symptoms, abnormality of vibration sense, and abnormal changes in heart beat associated with diabetic peripheral neuropathy.
Status:
Possibly Marketed Outside US
Source:
NCT02020408: Phase 4 Interventional Completed Eating Disorder
(2011)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
3-amino-4-(2[11C]methylaminomethylphenylsulfanyl)benzonitrile (DASB C-11) exhibits excellent in vitro and in vivo properties toward the serotonin transporter. Parametric imaging of serotonin transporters (SERT) with DASB C-11 PET is a useful data analysis tool. DASB C-11 is a suitable PET radioligand for measuring drug occupancy of the SERT in vivo and has potential for monitoring in vivo changes in serotonin levels. Studies in humans showed that the regional distribution of DASB C-11 uptake was concordant with the known densities of SERT sites in the brain. The highest levels of radioactivity were observed in the hypothalamus, intermediate levels were observed in the thalamus and striatum, whereas modest to low levels of radioactivity were observed in the cortical regions and cerebellum, respectively.
Status:
Possibly Marketed Outside US
Source:
Medrylamine
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Medrylamine is an antihistamine agent. It was used topically. Medrylamine offers sure relief from allergic manifestations of varied and unknown etiologies
Status:
Possibly Marketed Outside US
Source:
NCT00325936: Phase 4 Interventional Completed Hypertension
(2005)
Source URL:
Class (Stereo):
CHEMICAL (UNKNOWN)
Targets:
Conditions:
Cilnidipine (FRC-8653) is a dihydropyridine (DHP) type of calcium channel antagonist. The L-type Ca2+ channel blockade by cilnidipine affects predominantly vascular smooth muscle, thereby producing vasodilation of peripheral resistance vessels and coronary arteries. The blockade of N-type Ca2+ channels affects predominantly peripheral nerve endings of sympathetic neurons, thereby dilating blood vessels by lowering plasma catecholamine levels. Furthermore, renoprotective and neuroprotective effects as well as cardioprotective action of cilnidipine have been demonstrated in clinical practice or animal examinations. Cilnidipine was originated by Fuji & Rebio Pharmaceutical Co., Ltd. and developed jointly with Ajinomoto for the treatment of hypertension. Cilnidipine has been launched in Japan.
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:
Palerol by Novartis
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Piperylone is a non-narcotic analgesic and antispasmodic agent.
Status:
Possibly Marketed Outside US
Source:
NCT01595516: Phase 4 Interventional Completed Prehypertension
(2012)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Bradykinin, a pro-inflammatory mediator is also a neuromediator and regulator of several vascular and renal functions. Bradykinin can act as a vasoactive substance along with histamine in inflammation and swelling as it is a potent vasodilator. In addition, it triggers the release of other mediators such as nitric oxide in inflammatory and cancer tissues. Bradykinin acts via specific cell surface receptors: bradykinin receptor, B1 and B2 that are G-protein coupled receptors of the seven-transmembrane domain family. It was shown that increased plasma levels of bradykinin lead to the angioedema as the common major clinical manifestation. Bradykinin was also studied in heart transplant recipients and in obesity patients, but these studies were terminated or withdrawn for different reasons. Bradykinin is also an important growth factor for many cancers. Bradykinin antagonists showed higher potency than standard anti-cancer drugs, without evident toxicity to the hosts, that is why they have great promise for the development of new anti-cancer drugs.
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (RACEMIC)
Trimethyldiphenylpropylamine (Recipavrin) is a methadon analog with antispasmodic properties. It exerts both musculotropic (antibarium) and anticholinergic action, relieves smooth muscle spasms, e.g. dysmenorrhea and pains associated with gallstones. It was marketed in Sweden in the 1960s as a spasmolytic drug under tradename Recipavrin.
