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Restrict the search for
telotristat ethyl
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Status:
Possibly Marketed Outside US
Source:
Bururalol hydrochloride
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Bufuralol is a non-cardioselective beta-adrenergic blocker with high intrinsic sympathomimetic activity. It has affinity for both β1 and β2-adrenergic receptors. It acts as a potent β-adrenoceptor antagonist with partial agonist activity. Bufuralol is primarily metabolized by cytochrome P450 (CYP) isoform CYP2D6, with CYP1A2 and CYP2C19. Activity of bufuralol has been shown to yield antianginal and antihypertensive effects. It appears to have a higher incidence of adverse eflects than with other beta blockers. Bufuralol has been in phase III clinical trials for the treatment of hypertension. However, this research has been discontinued.
Status:
Possibly Marketed Outside US
Source:
Zoniclezole hydrochloride
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Class (Stereo):
CHEMICAL (RACEMIC)
Zoniclezole was proven to have anticonvulsant profile. It is representative of a novel class of water-soluble agents being developed for the treatment of epilepsy. Zoniclezole has been shown to be a potential antagonist of electroshock-induced seizures in animals, and to some degree, pentylenetetrazol-induced seizures. In preclinical studies the compound had prolonged efficacy at relatively low doses. Zoniclezole is glutamate receptor antagonist.
Status:
Possibly Marketed Outside US
Source:
Vatensol by Pfizer
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Guanoclor is an anti-hypertensive agent developed by
Pfizer Ltd. (U.K.). It seems to be effective in various types of hypertension
(unknown aetiology, renal, and malignant). It affects both
systolic blood-pressure and diastolic blood-pressure. It is an
adrenergic neurone-blocking agent, which also interferes with
noradrenaline synthesis by inhibition of the enzyme dopamine
beta-hydroxylase. Clinical use of the compound was first
reported by Lawrie et al. (1964), who achieved satisfactory
blood-pressure control in 60% of their cases with guanoclor
alone, and in a further 18% with the addition of a thiazide
diuretic. They also noted a significant reduction in urinary
noradrenaline levels during guanoclor administration. Guanochlor has an affinity for the Na+/H+ exchanger ranging between 0.5 uM and 6 uM in different systems and is more potent than amiloride in all systems studied. It is suggested that guanochlor recognizes a binding site on the Na+/H+ exchanger that is distinct from the amiloride binding site.
Status:
Possibly Marketed Outside US
Source:
ZATEBRADINE HYDROCHLORIDE
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Zatebradine is a bradycardic compound that blocks hyperpolarization-activated inward current (If) through cyclic nucleotide-gated cation (HCN) channels in sinoatrial node cells. Additionally, it can block voltage-gated outward K+ (IK) currents and related neuronal hyperpolarization-activated inward current (Ih) channels but exhibits little or no activity for L-type Ca2+ (ICa) currents. When assessed through telemetric ECG recording in mice, zatebradine reduced heart rate from 600 to 200 beats per minute with an ED50 value of 1.8 mg/kg and induced increasing arrhythmia at concentrations >10 mg/kg.
Status:
Possibly Marketed Outside US
Source:
LESHCUTAN
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Methylbenzethonium chloride is a quaternary ammonium with antimicrobial activity, which is used in combination with aminoglycoside antibiotic, paromomycin (brand name LESHCUTAN) for the topical treatment of cutaneous leishmaniasis.
Status:
Possibly Marketed Outside US
Source:
LESHCUTAN
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Methylbenzethonium chloride is a quaternary ammonium with antimicrobial activity, which is used in combination with aminoglycoside antibiotic, paromomycin (brand name LESHCUTAN) for the topical treatment of cutaneous leishmaniasis.
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (ACHIRAL)
Dihexyverine (Metaspas, Spasmodex) is an anticholinergic and direct smooth muscle relaxant (spasmolytic). Dihexyverine is sold in France under the brand name Spasmodex. It is indicated for the treatment of the gastrointestinal tract disorders. Dihexyverine is a muscarinic acetylcholine receptor antagonist.
Status:
Possibly Marketed Outside US
Source:
Trandate by Allen & Hanburys
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Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Dilevalol, the RR-stereoisomer of labetalol, is a non-cardioselective β-adrenoceptor antagonist with substantial partial β2-agonist and negligible α1-blocking activity. Reduction in blood pressure during dilevalol administration is associated with peripheral vasodilatation, and heart rate remains essentially unchanged. Following oral administration, dilevalol is completely absorbed. Once-daily administration is possible, due to a long elimination half-life. In vitro and in vivo animal studies and results obtained in humans reveal that dilevalol is a nonselective blocker of β1- and β2-adrenoceptors, with a similar potency to propranolol, but has negligible antagonistic activity at α1-receptors. Dilevalol, the R,R′ stereoisomer, makes up 25% of racemic labetalol, the drug, approved by FDA for the treatment of hypertension. The relaxing potency of dilevalol was approximately 4.7 times more potent than that of labetalol. Dilevalol markedly reduced the diastolic blood pressure with only a slight increase of heart rate In pithed rats, while isoproterenol and pindolol caused moderate to marked positive chronotropic effects in proportion to their hypotensive effects. These results suggest that dilevalol has more potent ISA than labetalol. In contrast to labetalol, dilevalol possesses little, if any, alpha-adrenergic blocking activity. The compound is 3 to 10 times less potent than labetalol at α1-adrenergic receptors under a variety of experimental conditions. Moreover, it is 300- to 1000-fold less potent at alpha1-adrenergic receptors compared with β1-adrenergic receptors. The pA2 values for dilevalol as an α antagonist range from 5.9 to 6.4. Because maximal plasma concentrations of the drug after administration of a 400-mg dose are approximately 0.5 pmol, it is doubtful that alpha blockade is involved in the antihypertensive response to dilevalol in humans.
Status:
Possibly Marketed Outside US
Source:
Surheme by Spemsa [Italy]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Butalamine hydrochloride under the brand name Adrevil forte is an effective drug for the treatment of patients suffering from blood flow disorders of the lower extremities.
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (ACHIRAL)
Biphenamine is a local anesthetic with antibacterial and antifungal properties. It has been used in the treatment of seborrheic scalp disorders.
