U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 411 - 420 of 575 results

1-(2-methoxyphenyl)piperazine is an effective blocker of striatal dopaminergic receptors in rat brain and is apparently the simplest chemical structure known to exert dopaminergic blocking activity. It is exhibited pronounced antihypertensive and weak sympatholytic activities in experimental animals. Blood pressure was also lowered in hypertensive patients and this effect was sometimes accompanied by a strong sedation, and after large repeated doses, by disorientation and stupor. In a filter paper bioassay 1-(2-methoxyphenyl)piperazine demonstrated acaricidal activity. 1-(2-methoxyphenyl)piperazine is a building block of many serotonergic and dopaminergic agents. Some of them have antidepressant activity.
1-(2-methoxyphenyl)piperazine is an effective blocker of striatal dopaminergic receptors in rat brain and is apparently the simplest chemical structure known to exert dopaminergic blocking activity. It is exhibited pronounced antihypertensive and weak sympatholytic activities in experimental animals. Blood pressure was also lowered in hypertensive patients and this effect was sometimes accompanied by a strong sedation, and after large repeated doses, by disorientation and stupor. In a filter paper bioassay 1-(2-methoxyphenyl)piperazine demonstrated acaricidal activity. 1-(2-methoxyphenyl)piperazine is a building block of many serotonergic and dopaminergic agents. Some of them have antidepressant activity.
1-(2-methoxyphenyl)piperazine is an effective blocker of striatal dopaminergic receptors in rat brain and is apparently the simplest chemical structure known to exert dopaminergic blocking activity. It is exhibited pronounced antihypertensive and weak sympatholytic activities in experimental animals. Blood pressure was also lowered in hypertensive patients and this effect was sometimes accompanied by a strong sedation, and after large repeated doses, by disorientation and stupor. In a filter paper bioassay 1-(2-methoxyphenyl)piperazine demonstrated acaricidal activity. 1-(2-methoxyphenyl)piperazine is a building block of many serotonergic and dopaminergic agents. Some of them have antidepressant activity.
1-(2-methoxyphenyl)piperazine is an effective blocker of striatal dopaminergic receptors in rat brain and is apparently the simplest chemical structure known to exert dopaminergic blocking activity. It is exhibited pronounced antihypertensive and weak sympatholytic activities in experimental animals. Blood pressure was also lowered in hypertensive patients and this effect was sometimes accompanied by a strong sedation, and after large repeated doses, by disorientation and stupor. In a filter paper bioassay 1-(2-methoxyphenyl)piperazine demonstrated acaricidal activity. 1-(2-methoxyphenyl)piperazine is a building block of many serotonergic and dopaminergic agents. Some of them have antidepressant activity.
1-(2-methoxyphenyl)piperazine is an effective blocker of striatal dopaminergic receptors in rat brain and is apparently the simplest chemical structure known to exert dopaminergic blocking activity. It is exhibited pronounced antihypertensive and weak sympatholytic activities in experimental animals. Blood pressure was also lowered in hypertensive patients and this effect was sometimes accompanied by a strong sedation, and after large repeated doses, by disorientation and stupor. In a filter paper bioassay 1-(2-methoxyphenyl)piperazine demonstrated acaricidal activity. 1-(2-methoxyphenyl)piperazine is a building block of many serotonergic and dopaminergic agents. Some of them have antidepressant activity.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)



(R)-Alprenolol is a less active stereoisomer of antihypertensive beta-blocker alprenolol. Its activity against beta-adrenoreceptor is 100 times lower than the activity of (S)-alprenolol. In a model of ventricular arrhythmias produced by ligation of the left coronary artery, (R)-alprenolol was effective at 15.5 mg/kg, whereas (S)-alprenolol abolished the ventricular arrhythmia by cumulative dose of 7.5 mg/kg.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)



Benzamil is a derivative of amiloride, a potassium sparing diuretic, and is an inhibitor of Na /H and Na /Ca channels. Amiloride works by directly blocking the epithelial sodium channel (ENaC) thereby inhibiting sodium reabsorption in the distal convoluted tubules and collecting ducts in the kidneys (this mechanism is the same for triamterene). This promotes the loss of sodium and water from the body, but without depleting potassium. Benzamil has being shown to attenuate the development of hypertension in Dahl salt-sensitive rats. Benzamil has been studied as a possible treatment for cystic fibrosis. Benzamil was suggested to be a useful sodium channel blocker for the long-term treatment of the biochemical defect in the lungs of patients with cystic fibrosis.
SDZ-WAG-994 is a potent and selective A1 receptor agonist, discovered by Sandoz. SDZ-WAG-994 was able to induce a dose-related and sustained fall in blood pressure and heart rate in spontaneously hypertensive rats. The compound was investigated in patients with heart failure symptoms and moderate left ventricular systolic dysfunction, where it produced no effect. In patients with patients with permanent atrial fibrillation, SDZ-WAG-994 was able to limit the increase in mean heart rate during exercise. The compound was also tested for treatment of postoperative dental pain, but for all efficacy measures, SDZ-WAG-994 was not significantly different from placebo.
Veratridine (VTD), an alkaloid derived from the Liliaceae plant shows anti-tumor effects. Veratridine is also an agent that opens voltage dependent Na+ channels, blocks Na+ channel activation, and induces Ca2+ influx. The compound has been observed to be an alkaloid neurotoxin used to amplify sodium permeability. Studies report that Veratridine can trigger exocytosis and induce Ca2+ oscillations. Furthermore, Veratridine has been shown to effect the mitochondrial respiratory chain complexes, induce release of noradrenaline, and increase superoxide anion production. Veratridine competes with BTX binding in a mutually exclusive manner. However, the pharmacological effects of veratridine on Na+ channels are quite different from those of BTX. First, veratridine reduces the single Na+ channel conductance drastically whereas BTX does not. Veratridine therefore is regarded as a partial agonist and BTX as a full agonist of Na+ channels. Second, under voltage clamp conditions BTX binds practically irreversibly to Na+ channels whereas veratridine readily dissociates from its binding site. Both of these drugs, however, bind preferentially to the open state of Na+ channels. The BTX resistant Na+ channels in Phyllobates frogs remain sensitive to veratridine. The ceveratrum alkaloids, including Veratridine, have a characteristic hypotensive effect not directly involving the CNS. They slow the heart and lower arterial blood pressure by reflexly stimulating medullary vasomotor centers without decreasing cardiac output (Bezold–Jarisch effect). These agents were introduced in the 1950s as antihypertensive agents; however, they were found to have a narrow therapeutic index and their use was discontinued.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

C-curarine-III chloride (Methvin) is a short-acting selective sympathetic ganglioblocker with weak antagonist activity on the nicotinic receptor at the neuromuscular junction; hypotensive. In test animals the drug produces a well-marked and short-term (easily controllable) hypotensive effect, without causing any histamine-like and direct vasodilation action. When used in relatively high doses methvin blocks the neuro-muscular conduction, potentiates the action of major muscle relaxants. A study of methvin in clinical conditions confirmed its high gangliolytic activity previously revealed in experiments.

Showing 411 - 420 of 575 results