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Restrict the search for
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Status:
Investigational
Source:
INN:flerobuterol [INN]
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
FLEROBUTEROL is a beta-adrenoceptor agonist with potential antidepressant activity.
Class (Stereo):
CHEMICAL (ACHIRAL)
FLOSATIDIL is an antihypertensive drug discontinued in Phase II for angina pectoris.
Status:
Investigational
Source:
INN:thiodiglycol [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Thiodiglycol is the organosulfur structurally similar to diethylene glycol used as a solvent in a variety of applications ranging from dyeing textiles to inks in some ballpoint pens. In chemical synthesis, it is used as a building block for protection products, dispersants, fibers, plasticizers, rubber accelerators, pesticides, dyes, and various other organic chemicals. In the manufacture of polymers, it is used as a chain transfer agent. Thiodiglycol is a precursor in the production of Sulfur mustard and it is also considered as a “Schedule 2” compound (dual-use chemicals with low to moderate commercial use and high-risk precursors) within the terms of the Chemical Weapons Convention treaty.
Class (Stereo):
CHEMICAL (RACEMIC)
KETOCAINOL is an antiarrhythmic agent, anaesthetic.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Tinofedrine is a dithienylamine derivative patented by Deutsche Gold- und Silber-Scheideanstalt vorm. Roessler for improvement of cerebral and peripheral blood flow. In anesthetized dogs, Tinofedrine causes a remarkable increase of cardiac output by positive inotropic and chronotropic stimulation of the heart and simultaneous reduction of peripheral vascular resistance. In comparison with typical beta-agonists Tinofedrine at isotropically equieffective doses, has a much weaker effect on the heart rate. In coronary circulation, Tinofedrine causes vasodilation so that in a therapeutic dose range increased workload is equalized by sufficient myocardial supply.
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Tibenzate is a thiobenzoic acid derivative disclosed in Merck & Co., Inc. patent application. Topically applied Tibenzate shows high acaricidal activity, especially against itch mites (Sarcoptes scabiei) and their eggs. Tibenzate shows some level of antimicrobial activity against S.aureus, P.aeruginosa, and C.albicans.
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Edonentan (BMS 207940) is a highly selective biphenylsulfonamide endothelin A receptor antagonist. (11)C- and (18)F-labeled analogs of edonentan were evaluated of novel PET radioligands for imaging the endothelin-A receptor. Edonentan was in clinical trials for the treatment of heart failure however its development has been discontinued.
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Conditions:
Nifenalol is the beta-receptor antagonist. It has optical isomers. The racemic mixture and the levo-isomer are active in antagonizing beta-receptors, but the dextro-isomer is inactive. The levo-isomer seems to be about twice as active in blocking beta-receptors as the racemate. Nifenalol is virtually devoid of local anesthetic properties in contrast to procaine, propranolol, and butidrine. Nifenalol exacerbated the fighting behavior in male mice by foot-shock. Nifenalol has been studied in patients with coronary artery disease. It afforded the coronary patient good protection against angina and ischemic changes in the EKG. It was further noted that nifenalol had no antiarrhythmic action and that it was devoid of evident side effects. Nifenalol possessed weak action against tremorine and oxotremorine induced tremor.
Class (Stereo):
CHEMICAL (RACEMIC)
Nardeterol (SOM-1122) was found to be a high-affinity, partial agonist for beta adrenergic receptors. SOM-1122 inhibited the binding of [125I]iodopindolol to membranes prepared from rat cerebral cortex and cerebellum. SOM-1122 bound to beta adrenergic receptors in vitro and in vivo, increased levels of cyclic AMP in slices of cerebral cortex in vitro and reduced the density of beta adrenergic receptors after chronic treatment. SOM-1122 also was found to be behaviorally active. It reduced locomotor activity
and altered behavior maintained under DRL and multiple FlFR schedules. These behavioral effects of SOM-1122 are similar
to those reported previously for other centrally acting beta
adrenergic agonists.
Status:
Investigational
Source:
NCT01100684: Phase 3 Interventional Completed Diarrhea Predominant Irritable Bowel Syndrome
(2010)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Asimadoline is an orally active, highly selective kappa-opioid receptor agonist with approximately 500-fold greater affinity for human kappa-, as compared with either delta- or mu-opioid receptors. Due to its high selectivity for the kappa-opioid receptor, asimadoline does not produce mu-opioid like side effects. It is investigated for use/treatment in irritable bowel syndrome, pruritus, postoperative ileus. A drug interaction study investigating the coadministration of asimadoline with ketoconazole was performed in healthy volunteers - a two to three-fold increase in AUC and Cmax of asimadoline was observed with concomitant administration of ketoconazole. The most common adverse events are diarrhea, nausea, sinusitis, headache and fatigue.
