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Restrict the search for
guanidine
to a specific field?
Class (Stereo):
CHEMICAL (ACHIRAL)
Guancydine, an antihypertensive agent which anti-angiotensin effect was not observed.
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Zaltidine (CP-57,361) is a guanidinothiazolylimidazole compound
which is a highly specific H2-receptor antagonist. It potently inhibits gastric acid secretion. Zaltidine appears to be an effective treatment of duodenal ulcer in human studies. However, the incidence of hepatic damage (8%) seems higher than with commonly used H2-receptor antagonists.
Class (Stereo):
CHEMICAL (ACHIRAL)
Tuvatidine (HUK 978) is a potent H2-antagonist. HUK 978 was shown to be devoid of activity at the histamine H1-receptor, the muscarinic receptor and the alpha and beta-adrenergic receptors. In both the guinea-pig gastric mucosa preparation and the rat perfused stomach
model, HUK 978 was a powerful inhibitor of acid secretion. HUK 978 is a highly specific H2-antagonist and inhibits acid secretion for longer periods than other competitive compounds.
Status:
Investigational
Source:
NCT00852839: Phase 2 Interventional Completed Dry Mouth Associated With Sjogren's Syndrome
(2009)
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Compound 552-02 is a potent, selective inhibitor of epithelial sodium channels that is effective in enhancing mucociliary clearance and is well tolerated when administered as a single dose by inhalation aerosol in normal healthy adult volunteers. Parion Sciences was developing 552 02 for the treatment of xerostomia, cystic fibrosis, chronic bronchitis, chronic obstructive pulmonary disease, radiation injuries. Compound 552-02 was specifically designed for aerosol delivery to the pulmonary system as a more selective, potent, long-acting ENaC blocker to promote an expansion in ASL volume, with or without hypertonic saline. Compound 552-02 was selected from a series of novel ENaC blockers to
produce a selective block on airway epithelial sodium channels, with a potency up to 2 orders of magnitude greater than
amiloride. 552-02 blocked the majority (95%) of Isc, with a calculated IC50 value of 7 nM. Drug development was discontinued.
Class (Stereo):
CHEMICAL (ACHIRAL)
Cariporide is a selective sodium-hydrogen antiporter inhibitor patented by a pharmaceutical company Hoechst A.-G. for treatment myocardial ischemia-reperfusion injury. The sodium-hydrogen exchanger is an important player in the pathophysiology of myocardial ischemia-reperfusion injury. The accumulation of hydrogen ions in the myocyte cytosol; during ischemia creates a proton gradient that promotes the efflux of hydrogen ions in exchange for the influx of sodium ions. This sodium buildup can secondary activates the sodium-calcium exchanger to operate in the reverse mode, resulting in a net calcium accumulation in myocyte cytosol, which leads to dysfunction and cell death. By inhibiting sodium-hydrogen exchange, Cariporide can prevent the accumulation of calcium in the cytosol, therefore reduce the infarct size. In clinical trials, Cariporide shows a statistically significant decline in myocardial infarction but increases mortality. Due to the increase in mortality, cariporide did not pass clinical trials.
Status:
Investigational
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Conditions:
Siguazodan is a selective inhibitor of phosphodiesterase 3. It caused significant increases in cardiac output and stroke volume. It is orally active inotropic/vasodilator agent with a sustained duration in vivo. Siguazodan has potential utility in the treatment of congestive heart failure. Siguazodan has anti-platelet actions over the same concentration range that it is an inotrope and vasodilator. Siguazodan caused bronchodilation. In combination with phosphodiesterase 4, it may be useful in the therapy of asthma.
Status:
Investigational
Source:
INN:flubrobenguane (¹⁸F) [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Tiotidine is a controversial histamine H2 receptor ligand with negligible activity against H1- and H3- receptors. It was found that tiotidine behaves as an inverse agonist in U-937 cells, diminishing basal cAMP levels. Tiotidine showed two binding sites, one with high affinity and low capacity and the other with low affinity and high capacity. Tiotidine is currently in use as a radioligand in histamine H2-receptor binding studies. Compared to cimetidine, tiotidine appears to be approximately eight times more potent on a molar basis than cimetidine as an inhibitor of acid secretion, and the tiotidine effect is more prolonged. It was developed for the treatment of peptic ulcer.
Status:
Investigational
Source:
INN:gapromidine [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Class (Stereo):
CHEMICAL (ACHIRAL)
Guanclofine was studied as an adrenergic neuron blocking agent.
