Bradyzide
Bradyzide is an orally active non-peptide competitive bradykinin B2 receptor antagonist. The rat Ki for Bradyzide binding to the B2 receptor is 0.5 nM, and the human Ki is 722 nM. Bradyzide can be used for research on inflammatory hyperalgesia and anxiety disorders.
For research use only. We do not sell to patients.
- CAS No.: 263011-13-8
- Formula: C32H42N8O5S2
- Molecular Weight:682.86
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
All Bradykinin Receptor Isoforms
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Biological Activity
Description
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Bradykinin B2 Receptor (B2R) 0.5-722 nM (Ki) |
Bradykinin B2 Receptor (B2R) 0.8-772 nM (IC50) |
In Vitro
Bradyzide antagonizes BK B2 receptor-mediated 45Ca2+ efflux in NG108-15 cells with a pA2 of 8.0[1].
Bradyzide competitively antagonizes BK B2 receptor-mediated contraction of rat uterine smooth muscle, with a pA2 of 8.6[1].
Bradyzide competitively inhibits [3H]BK binding to recombinant rabbit B2 receptors expressed in COS-1 cells, with a Ki of 0.78 nM[4].
Bradyzide ((S)-4) effectively inhibits [3H]BK binding to rodent B2 receptors in NG108-15 membranes, with a Ki of 0.5 nM[5].
Bradyzide weakly inhibits [3H]BK binding to cloned human B2 receptors in Cos-7 membranes with a Ki of 772 nM[5].
Bradyzide binds to rodent B2 receptors in NG108-15 membranes with a KI of 0.51 nM[6].
Bradyzide has low affinity for human B2 receptors in WI-38 membranes, with a KI of 393 nM[6].
Bradyzide is a competitive B2 antagonist in NG108-15 cells with a pKB of 8.0[6].
Bradyzide inhibits rat B2-mediated IP3 generation with an IC50 of 11.8 nM, whereas its effect on the human B2 receptor is much weaker, with an IC50 of 2.4 μM[6].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Bradyzide (0.2-2.0 mg/kg; s.c.; acute administration before behavioral testing) produces a clear anxiolytic-like effect in the open field at 0.7 mg/kg, but this effect is confounded by increased locomotor activity and is not reproduced in the novelty-suppressed feeding or elevated plus maze tests[2].
Bradyzide (p.o.; >4 h) produces oral antihyperalgesic efficacy in FCA-induced mechanical hyperalgesia in rats, with an ED50 of 0.84 µmol/kg and a duration of action exceeding 4 h[5].
Bradyzide (0.1-5 µmol/kg i.v.; 0.75 µmol/kg p.o.; single administration) reverses FCA-induced mechanical hyperalgesia in rats, with a long-lasting effect[6].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:DBA/2NCrl (D2; male; 5-8 weeks old on arrival)[2]
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Dosage:0.2; 0.7; 2.0 mg/kg
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Administration:s.c.; acute administration before behavioral testing
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Result:0.7 mg/kg increased time spent in the open-field centre zone compared with controls.
0.7 and 2.0 mg/kg increased distance travelled in the open field compared with controls.
Adjusting for locomotor activity abolished the apparent centre-zone effect.
0.7 mg/kg did not alter latency to eat in the novelty-suppressed feeding test or time/distance in the open arms of the elevated plus maze.
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Animal Model:Sprague-Dawley (female, 100-120 g)[6]
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Dosage:0.1, 0.5, 0.75, 1, and 5 µmol/kg
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Administration:i.v. or p.o.; single administration after control readings
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Result:Reversed FCA-induced mechanical hyperalgesia with an ED50 of 0.9 µmol/kg i.v. and 0.84 µmol/kg p.o.
Maximal effect was 79% after i.v. dosing and 84% after p.o. dosing, with duration greater than 4 h.
Onset was rapid, with maximum response within 30 min of both i.v. and p.o. administration; duration was greater than 4 h at 0.75 µmol/kg p.o. and above.
Chemical Information
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CAS No. 263011-13-8
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Molecular Weight 682.86
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Formula C32H42N8O5S2
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SMILES
O=S(N1[C@@H](CCC1)C(NCCN(C)CCN(C)C)=O)(C2=CC([N+]([O-])=O)=C(C=C2)NNC(NC(C3=CC=CC=C3)C4=CC=CC=C4)=S)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Heitsch H. Non-peptide antagonists and agonists of the bradykinin B2 receptor. Current medicinal chemistry. 2002 May 1;9(9):913-28. [Content Brief]
[2]. Rouhiainen A, et al. The bradykinin system in stress and anxiety in humans and mice. Scientific reports. 2019 Dec 19;9(1):19437. [Content Brief]
[3]. Valdés G, et al. Administration of angiotensin II and a bradykinin B2 receptor blocker in midpregnancy impairs gestational outcome in guinea pigs. Reproductive biology and endocrinology : RB&E. 2014 Jun 04;12:49. [Content Brief]
[4]. Marceau F, et al. A non-peptide antagonist unusually selective for the human form of the bradykinin B2 receptor. International immunopharmacology. 2003 Oct 1;3(10-11):1529-36. [Content Brief]
[5]. Dziadulewicz EK, et al. Nonpeptide bradykinin B2 receptor antagonists: conversion of rodent-selective bradyzide analogues into potent, orally-active human bradykinin B2 receptor antagonists. Journal of medicinal chemistry. 2002 May 23;45(11):2160-72. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Bradyzide Related Classifications
HY-189089 Related Classifications
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