Bethanidine sulfate (Synonyms: BW 467C60)

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Bethanidine sulfate (BW 467C60) is an orally active antihypertensive agent and adrenergic neuron blocker. Bethanidine sulfate exerts its antihypertensive effect by inhibiting the release of norepinephrine from sympathetic nerve terminals. Bethanidine sulfate exhibits anti-ventricular arrhythmic activity. Bethanidine sulfate can be used in research related to hypertension, ventricular tachycardia, and ventricular fibrillation.

For research use only. We do not sell to patients.

Bethanidine sulfate Chemical Structure

CAS No. : 114-85-2

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Biological Activity
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References
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Description

In Vitro

Bethanidine sulfate (1-3 μg/mL) abolishes the inhibitory effect of neural stimulation on the pendular movement of isolated rabbit ileum^[1].
Bethanidine sulfate (1-10 μg/mL) attenuates the neurostimulatory contractile response of isolated guinea pig vas deferens at a concentration of 1 μg/mL, and completely abolishes this response at 3 μg/mL^[1].
Bethanidine sulfate (3-300 μg/mL) inhibits the peristaltic reflex of isolated guinea pig ileum; it reduces cholinergic sensitivity at concentrations of 3 to 30 μg/mL, and decreases the sensitivity to acetylcholine and histamine by 10-fold at a concentration of 300 μg/mL^[1].
Bethanidine sulfate (100-300 μg/mL) inhibits serotonin-induced contraction of isolated rat uterus and adrenaline-induced contraction of isolated rabbit uterus^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Bethanidine sulfate (0.1-100 mg/kg; i.v./s.c./p.o.) produces potent, long-lasting adrenergic neuronal blockade in cats, preferentially inhibiting low-frequency sympathetic nerve stimulation, and is accompanied by transient sympathomimetic effects and neuromuscular blockade at high doses^[1].
Bethanidine sulfate (0.3-100 mg/kg; intravenous/oral administration) induces dose-dependent pressor effects, adrenergic neuron blockade, and enhanced amine responses in dogs, and exhibits good tolerance to high oral doses^[1].
Bethanidine sulfate (10 mg/kg; subcutaneous injection) transiently slows gastrointestinal transit in fasted rats, and an accelerated transit rate is observed 4 h after administration^[1].
Bethanidine sulfate reduces motor activity in mice at high doses. When administered intravenously at 12.5 mg/kg, it prolongs pentobarbital-induced hypnotic duration, and exhibits route-dependent toxicity, with an LD₅₀ of 12 mg/kg for intravenous injection and 520 mg/kg for oral administration^[1].
Bethanidine sulfate (300 mg/kg) increases the ventricular fibrillation threshold by 150% in the hearts of normal dogs and by 327% in the hearts of infarcted dogs, with no acute toxicity observed even at doses as high as 300 mg/kg^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Cat (anaesthetized with chloralose, pentobarbitone, or nitrous oxide; unanaesthetized)^[1]
Dosage:	0.1-30 mg/kg (i.v.); 0.5-100 mg/kg (s.c.); 1.25-5 mg/kg (p.o.)
Administration:	i.v.; s.c.; p.o.
Result:	Caused a blood pressure fall of 20-60 mmHg lasting over 1 hour at 0.3 or 1 mg/kg i.v.. Raised blood pressure by 20-50 mmHg with tachycardia lasting 10 minutes at additional 1 mg/kg i.v.. Decreased hind limb vasoconstrictor responses to sympathetic chain stimulation at 0.1-0.5 mg/kg i.v.. Abolished hind limb vasoconstrictor responses to sympathetic chain stimulation and reversed nerve stimulation to increase blood flow at 1 mg/kg i.v.. Decreased pressor responses to 200 μg tyramine at 3-10 mg/kg. Abolished nictitating membrane contractions to pre- or post-ganglionic sympathetic nerve stimulation, while increased responses to adrenaline and noradrenaline. Caused nictitating membrane contractions ≤30% of maximum at 3-10 mg/kg i.v.. Partially relaxed the nictitating membrane at 1.25 mg/kg s.c. or p.o.. Fully relaxed the nictitating membrane with effects persisting 2-3 days at 2.5 mg/kg s.c. or p.o.. Impaired preganglionic nerve responses at 24 hours at 1 mg/kg s.c. or p.o.. Abolished preganglionic nerve responses at 3 mg/kg s.c. or p.o.. Almost abolished spleen contractions to splenic nerve stimulation 30 minutes after 0.3 mg/kg i.v.. Reduced noradrenaline release from the spleen during nerve stimulation to 1/10 of control levels 15 minutes after 0.3 mg/kg i.v.. Abolished rapid pressor responses to splanchnic nerve stimulation or dimethylphenylpiperazinium in adrenalectomized cats for over 1 hour at 0.3-0.5 mg/kg i.v.. Abolished piloerection for at least 30 minutes at 0.5 mg/kg i.v.. Reduced sweat secretion for 10-15 minutes at 3-10 mg/kg i.v.. Did not reduce pressor amine content of cat irises at 24 hours at single subcutaneous doses of 3, 10, or 30 mg/kg. Caused respiratory paralysis and neuromuscular block of gastrocnemius muscle response to indirect stimulation at 10-20 mg/kg i.v..

Animal Model:	Albino mice^[1]
Dosage:	/
Administration:	i.v.; i.p.; p.o.; s.c.
Result:	Did not change motor activity at 50 mg/kg p.o.. Decreased motor activity at 50 mg/kg i.p. and 200 mg/kg p.o.. Prolonged pentobarbitone hypnosis at 12.5 mg/kg i.v.. Did not prolong pentobarbitone hypnosis at 6.25 mg/kg i.v.. Had LD50 values of 12 mg/kg (i.v.), 150 mg/kg (i.p.), 260 mg/kg (s.c.), 520 mg/kg (p.o.).

Molecular Weight

275.32

Formula

C₁₀H₁₇N₃O₄S

CAS No.

114-85-2

SMILES

O=S(O)(O)=O.CN/C(NC)=N/CC1=CC=CC=C1.[0.5]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. BOURA AL, et al. Adrenergic neurone blockade and other acute effects caused by N-benzyl-N'N"-dimethylguanidine and its ortho-chloro derivative. Br J Pharmacol Chemother. 1963;20(1):36-55.

[2]. Bacaner MB, et al. Antiarrhythmic, antifibrillatory, and hemodynamic actions of bethanidine sulfate: an orally effective analog of bretylium for suppression of ventricular tachyarrhythmias. Am J Cardiol. 1982;50(4):728-734.

[3]. Gifford RW. Bethanidine sulfate—a new antihypertensive agent. JAMa. 1965 Sep 13;193(11):901-5.

Bethanidine sulfate Related Classifications

Neurological Disease Cardiovascular Disease

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Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Bethanidine114-85-2BW 467C60Adrenergic ReceptorBeta Receptorventricular fibrillationrabbit ileumadrenergic neurone blockernorepinephrinecatecholamineguinea-pig ductus deferensventricular tachycardiasympathetic postganglionic neuroeffector junctionsadrenergic nerve terminalshypertensionInhibitorinhibitorinhibit

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