AIMSBethanidine (BW467C60) is a newly presented strong adrenergic neuron blocking factor which has a hypotensive operation in man. SENPs are essential for maintaining a balance between SUMOylation and deSUMOylation which can be disturbed by changing the expression of (sentrin-specific proteases) SENPs. SENP1 is the most studied isoform of SENPs. Hypertrophic stimuli can increase SENP1 expression using calcium/calcineurin-NFAT3 signaling in heart. Moreover, SENP1 expression may positively relate to the expression of mitochondrial genes of the heart, and can cause the heart and mitochondrial dysfunction.MATERIALS AND METHODSIn order to inhibit SENP1 using Bethanidine, molecular docking and molecular dynamics (MD) simulation of SENP1 with Bethanidine were performed. Molecular docking showed that Bethanidine can inhibit SENP1.KEY FINDINGSMD Simulation showed that Bethanidine constitutes a stable complex with SENP1 as was evident from RMSD, RMSF, H-bond and DSSP plots. Free binding energy and the interaction patterns were obtained from molecular docking, and MD trajectory exhibited Bethanidine can be a potential drug candidate for SENP1 inhibition.SIGNIFICANCEThis study supplies enough evidences that Bethanidine is a potential inhibitor of SENP1 and can be applied for the treatment of cardiovascular diseases.

01 Nov 1994·European Journal of PharmacologyQ3 · MEDICINE

Tolerance to peripheral, but not central, effects of ropinirole, a selective dopamine D2-like receptor agonist

Q3 · MEDICINE

Article

Author: Raval, Pravin ; Parker, Stephen G. ; Eden, Roger J. ; Yeulet, Stephanie

Studies were conducted to determine possible development, and underlying mechanisms, of tolerance to the hypotensive effects of ropinirole (4-[2-(dipropylamino)ethyl]-1-3-dihydro-2H-indol-2-one HCl), a selective dopamine receptor agonist, following twice daily oral administration to cynomolgus monkeys and spontaneously hypertensive rats (SHR). Tolerance to the hypotensive effects of the compound developed in both species within one week of repeated dosing. Tolerance which developed in rats was dose-related and could not be attributed to altered plasma/drug concentrations or be overcome by increasing the i.v. challenge dose of ropinirole. Cross-tolerance was shown to the dopamine receptor agonist bromocriptine. Similar hypotensive responses to bethanidine were seen in rats treated with ropinirole or vehicle. Tolerance to hypolocomotor effects of the compound were not apparent in the same time frame. The dopamine D2 receptor antagonist, domperidone, caused hypertension in ropinirole-but not vehicle-treated rats. Results reported in this paper are not consistent with a down-regulation of peripheral dopamine D2-like receptors but suggest a compensatory increase in basal sympathetic tone.

01 Feb 1991·European Journal of PharmacologyQ3 · MEDICINE

Muscarinic receptors and parasympathetic neurotransmission in guinea-pig trachea

Q3 · MEDICINE

Article

Author: David F. Biggs ; Zhi-Jie Yang

Muscarinic receptors involved in cholinergic neurotransmission were studied in isolated innervated guinea-pig tracheas using preganglionic (nerve) and postganglionic (field) stimulation, after blocking sympathetic effects with bethanidine (5 microM). Neostigmine (10 nM) significantly increased responses to nerve and field stimulation. The M1 antagonist pirenzepine (0.1-100 nM) selectively reduced tracheal responses to nerve stimulation in control and in neostigmine-treated tissues. The M2 antagonist gallamine (0.1-100 microM) significantly increased tracheal responses to nerve and field stimulation in control and in neostigmine-treated preparations. At concentrations that increased baseline tone, oxotremorine, arecoline and pilocarpine decreased responses to nerve and field stimulation. Gallamine (30 microM) selectively reduced the inhibitory effects of these agonists on responses to nerve and field stimulation. The findings indicate that cholinergic neurotransmission in guinea-pig trachea is modulated by facilitatory M1 receptors at parasympathetic ganglia and inhibitory M2 receptors at the postganglionic nerve endings.

100 Deals associated with Bethanidine Sulfate

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KEGG	Wiki	ATC	Drug Bank
D01603	Bethanidine Sulfate	C02CC01	DBSALT000194

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