B 4310
B 4310 is a non-organ-selective Bradykinin antagonist. B 4310 induces uterine contraction in rats. B 4310 blocks bradykinin-mediated responses, including substance P release, plasma extravasation, venous contraction, prostaglandin E2 release and trigeminal nerve stimulation, but exerts no effect on angiotensin II, acetylcholine or capsaicin pathways. B 4310 exerts a reversible antagonistic effect on bradykinin-induced nociceptors. B 4310 serves as a tool for investigating the biological effects of bradykinin.
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- No. CAS: 103412-40-4
- Fòrmula: C62H95N19O14S2
- Peso molecular:1394.68
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Almacenamiento:
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Actividad biológica
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Chemical Information
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Actividad biológica
B 4310 acts as an agonist on isolated rat uterine tissues, with a pD2 value of 5.83, and its agonistic activity is approximately 1/500 that of bradykinin[1].
B 4310 (25-200 nM) acts as a competitive antagonist of bradykinin on isolated rat uterine tissues, with a pA2 value of 7.24[1].
B 4310 acts as a competitive antagonist of bradykinin on isolated rat duodenal tissues, with a pA2 value of 7.31[1].
B 4310 (7-60 nmol) dose-dependently and specifically inhibits bradykinin-induced plasma extravasation in ex vivo rabbit skin tissues without agonistic activity, with significant inhibitory effects observed at 20 and 60 nmol[2].
B 4310 (5-500 nM; 5 min) dose-dependently and specifically inhibits bradykinin-induced venous contraction in isolated perfused rabbit ear tissues, exerts significant inhibitory effects starting at a concentration of 5 nM, and does not affect angiotensin Ⅱ-mediated responses[2].
B 4310 (administered in advance at 800 nM) specifically inhibits bradykinin-induced PGE2 release in isolated perfused rabbit ear tissues, with an inhibition rate of 63%, and does not affect basal PGE2 release[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
B 4310 (15 nmol/min; arterial injection; continuous infusion) inhibits Captopril (HY-B0368)-potentiated Bradykinin-induced hypotension in healthy female Sprague-Dawley rats, reducing the blood pressure decrease from 55 mmHg to 23 mmHg during infusion[1].
Co-infusion of B 4310 (15 nmol/min; intra-arterial administration; continuous infusion) with Bacitracin (HY-107193) enhances its acute inhibitory effect on bradykinin-induced hypotension in healthy female Sprague-Dawley rats without prolonging the duration of action[1].
B 4310 (infusion; 50-500 nM) reversibly and competitively inhibits bradykinin-induced nociceptor stimulation in rabbits without affecting acetylcholine-mediated responses[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (female, 180-280 g)[1]
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Dosage:15 nmol/min
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Administration:i.a.; continuous infusion
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Result:Reduced the bradykinin-induced fall in mean arterial blood pressure from 35 mmHg to 9 mmHg.
Restored the bradykinin-induced blood pressure fall to 35 mmHg nine minutes after the end of infusion, matching the control group response of 33 mmHg.\nReduced the captopril-augmented bradykinin-induced blood pressure fall from 55 mmHg to 23 mmHg (P < 0.01), whereas saline infusion had no effect on the captopril-augmented bradykinin response.
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Animal Model:Sprague-Dawley (female, 180-280 g)[1]
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Dosage:15 nmol/min
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Administration:i.a.; continuous infusion
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Result:Reduced the bradykinin-induced blood pressure fall to 4 mmHg, a more pronounced inhibition than the 13 mmHg reduction seen in saline-co-infused controls (P < 0.01).
Equalized bradykinin-induced blood pressure falls in bacitracin and saline groups after stopping infusion.
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Animal Model:Male rabbits (3-4 kg)[2]
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Dosage:50 nM, 500 nM
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Administration:Infusion; administered during bradykinin injections
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Result:Caused a reversible, dose-dependent right shift of the bradykinin-induced reflex hypotension dose-response curve.
Shifted the curve by a factor of 8.7 at 50 nM dose.
Shifted the curve by a factor of 26.4 at 500 nM dose.
Did not alter acetylcholine-induced reflex hypotension.
Chemical Information
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No. CAS 103412-40-4
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Peso molecular 1394.68
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Fòrmula C62H95N19O14S2
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Sequence
Lys-Lys-Arg-Pro-{Hyp}-Gly-{β-3-thienylalanine}-Ser-Phe-{β-3-thienylalanine}-Arg
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Sequence Shortening
KKRP-{Hyp}-G-{β-3-thienylalanine}-SF-{β-3-thienylalanine}-R
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[1]. Griesbacher T, et al. Effects of the bradykinin antagonist B4310 on smooth muscles and blood pressure in the rat, and its enzymatic degradation. British journal of pharmacology. 1989 Mar;96(3):531-8. [Content Brief]
[2]. Griesbacher T, et al. Effect of bradykinin antagonists on bradykinin-induced plasma extravasation, venoconstriction, prostaglandin E2 release, nociceptor stimulation and contraction of the iris sphincter muscle in the rabbit. British journal of pharmacology. 1987 Oct;92(2):333-40. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
B 4310 Related Classifications
HY-P2027 Related Classifications
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