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Restrict the search for
methyl salicylate
to a specific field?
Status:
Investigational
Class (Stereo):
CHEMICAL (RACEMIC)
Daledalin is a norepinephrine reuptake inhibitor, developed in the 1970s by Pfizer. In animal models, daledalin potentiates the action of catecholamines, reverses the hypothermia induced by noradrenaline or noradnamine injected into the cerebral ventricles of mice. Daledalin potentiates amphetamine-induced excitation in rats and antagonizes reserpine-hypothermia in mice, tetrabenazine-sedation in rats and reserpine- and tetrabenazine-induced ptosis in mice. It inhibits noradrenaline and 5-hydroxytryptamine uptake by rat brain slices in vitro. In a clinical trial on patients with a depressive illness, no difference in efficacy between daledalin and amitriptyline was found.
Class (Stereo):
CHEMICAL (ACHIRAL)
Barucainide, an IB anti-arrhythmic agent, was evaluated in patients with coronary artery disease. Its antiarrhythmic effect was studied in patients with markedly depressed left-ventricular function. Barucainide was in phase II clinical trials to treat the patients with arrhythmias but the development of the drug was discontinued.
Status:
Investigational
Source:
INN:milipertine [INN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Milipertine was studied in patients with severe schizophrenia. Information about the current use of the drug is not available.
Status:
Investigational
Source:
NCT04439188: Phase 2 Interventional Active, not recruiting Advanced Lymphoma
(2016)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
GSK-2636771 is a potent, orally bioavailable, PI3Kβ-selective inhibitor, sensitive to PTEN null cell lines. GSK-2636771 shows selectively inhibitory activity in PTEN null cell lines (human prostate adenocarcinoma PC-3 and breast cancer HCC70) with EC50 of 36 nM and 72 nM, respectively. GSK-2636771 significantly decreases cell viability in p110β-reliant PTEN-deficient PC3 prostate and BT549 and HCC70 breast cancer cell lines, and leads to a marked decrease of AKT phosphorylation only in the control prostate and breast cancer cell lines. On April 1 2016 GlaxoSmithKine completes a phase-I/II trial for Solid tumours (Late-stage disease) in USA, United Kingdom and South Korea (NCT01458067).
Status:
Investigational
Source:
INN:pyrrolifene [INN]
Source URL:
Class (Stereo):
CHEMICAL (UNKNOWN)
Pyrroliphene is a dialkylaminodiphenylbutanol ester with antitussive and analgesic activities. In clinical trials the major side effect of Pyrroliphene was sedation, and the other side effect liabilities were similar to those of morphine.
Class (Stereo):
CHEMICAL (ACHIRAL)
Tiamenidine (also known as HOE 440) is a diazacycloalkene derivative patented by Farbwerke Hoechst A.-G. as 2 alpha-sympathomimetic antihypertensive agents. In preclinical models, tiamenidine induces hypotension and bradycardia in renal hypertensive cats and rats and in normal rats and dogs. Furthermore, Tiamenidine inhibits the liberation of norepinephrine from nerves leading to the heart and suppress sympathetic circulatory reflexes in dogs. In clinical trials, Tiamenidine exerts favor influences on systolic and diastolic blood pressure, and reduces plasma noradrenaline and adrenaline levels and suppresses plasma renin activity. Unfortunately, during the withdrawal of Tiamenidine, there is a rebound of blood pressure and plasma noradrenaline and adrenaline, overshooting baseline levels.
Status:
Investigational
Source:
Zhonghua Er Ke Za Zhi. Aug 2011;49(8):572-6.: Not Applicable Human clinical trial Completed Tourette Syndrome
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Tiapamil (also known as Ro 11-1781) is a dithiane derivative patented by Hoffmann-La Roche, F., und Co., A.-G. as calcium-channel antagonist useful for myocardial infarction treatment. Tiapamil, like verapamil, inhibited in a concentration-dependent manner Ca2+-induced contractions in isolated, K+-depolarized preparations of rat renal artery, dog coronary artery and rabbit main pulmonary artery. The inhibitory effects of Tiapamil can be overcome by raising the Ca2+ concentration of the bath fluid. In the rabbit main pulmonary artery, Tiapamil reduces 45Ca influx into the K+-depolarized vascular smooth muscle cells. Tiapamil inhibits the slow potentials in partially depolarized guinea-pig papillary muscles. Tiapamil decreases contractile force in isolated guinea-pig atria and papillary muscles, as well as in isolated cat hearts. Tiapamil also reduces heart rate and increases coronary flow in these preparations. Tiapamil doubled coronary artery blood flow in the coronary sinus blood without producing major changes in blood pressure and heart rate in anesthetized dogs. Tiapamil did not affect contractions of isolated guinea-pig ileum, rat stomach strips or rat vas deferens in response to various stimulants. Tiapamil have no major effects on renal water and electrolyte excretion, on autonomic nerves and receptors, on pain perception and on the central nervous system. Acute, subacute, and chronic toxicity studies demonstrate low toxicity for Tiapamil with no tendency for accumulation. In clinical trials, Tiapamil effectively lowers systolic and diastolic blood pressure, but have no effects on heart rate
Class (Stereo):
CHEMICAL (ABSOLUTE)
Sergolexole [LY 281067] is an ergoline ester similar in structure to amesergide [LY 237733], with potent and highly selective antagonist activity at serotonin 2. The preclinical pharmacologic activity of LY 281067 shows it to be a potent and highly selective serotonergic (5-HT2) receptor antagonist. Based upon binding studies with 5-HT2 receptors in brain cortical membranes and block of 5-HT-induced contractions in the rat jugular vein, LY 281067 showed high affinity at 5-HT2 receptors with a dissociation constant of approximately 1 nM. LY 281067 was a highly selective 5-HT2 receptor antagonist without appreciably binding to 5-HT1, D1 or D2 receptors or interacting with histamine (H1), cholinergic, beta adrenergic or alpha-1 adrenergic receptors in smooth muscle. LY 281067 had modest affinity at alpha-2 receptors with a dissociation constant of approximately 100 nM. Oral bioavailability of LY 281067 in spontaneously hypertensive rats was excellent with an oral to i.v. dose ratio approximating 4. Sergolexole was undergoing phase II clinical trials with Eli Lilly in the USA as a potential treatment for migraine and anxiety, but development of this compound, but development of this compound has been discontinued.
Class (Stereo):
CHEMICAL (ACHIRAL)
Quindecamine (also known as UCL-1407) is quinaldine derivative with antibiotic and fungicidal activity. Treatment of rats and mice with Quindecamine (250 mg/kg/ day) each day for 4 weeks followed by 500 mg/kg/day for 2 more weeks reduced spontaneous motility and body weight but produced no pathological abnormalities of the various organs studied. In vitro, the drug showed very good activity against Staphylococcus aureus, Streptococcus hemolyticus, Candida albicans, Trichophyton mentagrophytes, and T. vaginalis. The drug had very good activity in 180 human subjects with various bacterial and mycotic diseases of the skin and mucosa when applied as a 1% salve.
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Deterenol is a beta-adrenoceptor agonist. It is an effective nonmydriatic and nonmiotic hypotensive agent, which can be used in antiglaucoma treatment.
