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Context, anatomy, and key evidence

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vasoactive peptide

Bradykinin

Published evidence · coverage incomplete
Anatomical contextAnatomy connections are not mapped yet.

No body region is highlighted until this profile has a supported anatomical connection. This does not mean the peptide has no biological effects.

Read published mechanism findings ↓

At a glance

What is it—and why does it matter?

An introduction is not yet available. The findings below address specific research questions, not a complete account of this peptide.

This published profile is a reference in progress. Findings retain their source context; missing topics are marked below.

What is it?

A molecule, not a product name.

This profile does not yet contain a published summary for this topic. This is a coverage gap, not evidence that no research exists.

How does it work?

Target, response, and disposition.

Mechanism

In this source, the kallikrein-kinin system (KKS) is identified as a major biochemical source pathway for generating bradykinin.

Sources[2]pubmedKallikrein-8 contributes to kallikrein-kinin system dysregulation in Alzheimer's disease.The kallikrein-kinin system (KKS), a major source of bradykinin, has been associated with AD mainly at the peripheral level, but its regulation within the human brain remains largely unexplored.[2]pubmedKallikrein-8 contributes to kallikrein-kinin system dysregulation in Alzheimer's disease.The kallikrein-kinin system (KKS), a major source of bradykinin
Source records
2
Independent studies
1

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “The kallikrein-kinin system (KKS), a major source of bradykinin, has been associated with AD mainly at the peripheral level, but its regulation within the human brain remains largely unexplored.”

    Kallikrein-8 contributes to kallikrein-kinin system dysregulation in Alzheimer's disease. · Abstract

    pubmed:42140379:6b0c0795bec6:6b0c0795bec6
  2. supports · Source-backed record
    “The kallikrein-kinin system (KKS), a major source of bradykinin”

    Kallikrein-8 contributes to kallikrein-kinin system dysregulation in Alzheimer's disease. · Abstract

    pubmed:42140379:6b0c0795bec6:6b0c0795bec6

Mechanism

Icatibant acts as a selective antagonist of the bradykinin B2 receptor, a defined molecular target used for treating acute HAE attacks.

Sources[3]pubmedReal-World Safety and Effectiveness of Icatibant in Patients With Hereditary Angioedema (HAE): Post-Marketing Surveillance in Japan.Icatibant is a selective bradykinin B2 receptor antagonist for treatment of acute attacks of HAE.
Source records
1
Independent studies
1

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Icatibant is a selective bradykinin B2 receptor antagonist for treatment of acute attacks of HAE.”

    Real-World Safety and Effectiveness of Icatibant in Patients With Hereditary Angioedema (HAE): Post-Marketing Surveillance in Japan. · Abstract

    pubmed:42630033:167e09d40262:167e09d40262

Mechanism

Angioedema classification in the source emphasizes differentiating mast cell-mediated from bradykinin-mediated mechanisms.

Sources[4]pubmed[Clinical presentation and diagnosis of bradykinin-mediated angioedema].The most important differentiation to make is between mast cell-mediated and bradykinin-mediated angioedema
Source records
1
Independent studies
1

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “The most important differentiation to make is between mast cell-mediated and bradykinin-mediated angioedema”

    [Clinical presentation and diagnosis of bradykinin-mediated angioedema]. · RESULTS

    pubmed:42640320:8028dd540ab7:8028dd540ab7

Mechanism

In a [3H]-bradykinin radioligand binding assay using CHO cells expressing rat B2 bradykinin receptor, CHEMBL406291 showed Ki 0.46 nM.

Sources[1]chembl-activitiesChEMBL activities for CHEMBL406291Standard result: Ki = 0.46 nM
Reported result
Ki = 0.46 nM
Source records
1
Independent studies
1

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Standard result: Ki = 0.46 nM”

    ChEMBL activities for CHEMBL406291 · Activity 54724

    chembl-activities:chembl406291:a7cf8a298b4b:a7cf8a298b4b

Mechanism

In a cell-based [3H]bradykinin displacement assay using CHO cells expressing human cloned B2 bradykinin receptor, CHEMBL406291 showed very high affinity (Ki 0.065 nM).

Sources[1]chembl-activitiesChEMBL activities for CHEMBL406291Standard result: Ki = 0.065 nM[1]chembl-activitiesChEMBL activities for CHEMBL406291Standard result: Ki = 0.65 nM
Reported result
Ki = 0.065 nM
Source records
2
Independent studies
1

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Standard result: Ki = 0.065 nM”

    ChEMBL activities for CHEMBL406291 · Activity 680171

    chembl-activities:chembl406291:a7cf8a298b4b:a7cf8a298b4b
  2. supports · Source-backed record
    “Standard result: Ki = 0.65 nM”

    ChEMBL activities for CHEMBL406291 · Activity 54723

    chembl-activities:chembl406291:a7cf8a298b4b:a7cf8a298b4b

Mechanism

In a functional cell-based assay measuring inhibition of bradykinin-induced intracellular calcium mobilization at human recombinant bradykinin 2 receptor expressed in CHO cells, CHEMBL406291 had EC50 0.04898 nM.

Sources[1]chembl-activitiesChEMBL activities for CHEMBL406291Standard result: EC50 = 0.04898 nM
Reported result
EC50 = 0.04898 nM
Source records
1
Independent studies
1

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Standard result: EC50 = 0.04898 nM”

    ChEMBL activities for CHEMBL406291 · Activity 2636120

    chembl-activities:chembl406291:a7cf8a298b4b:a7cf8a298b4b

What has been studied?

What the evidence says.

Study findings

In an organism-based rat study reporting percent change in renal vascular resistance, intravenous CHEMBL406291 at 3 ug/kg was associated with a -19.0% change.

Sources[1]chembl-activitiesChEMBL activities for CHEMBL406291Assay: % Change in renal vascular resistance in rats when administered at dose 3 ug/kg intravenously Assay format: organism-based format Standard result: Change = -19.0 %
Reported result
Change = -19.0 %
Source records
1
Independent studies
1

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Assay: % Change in renal vascular resistance in rats when administered at dose 3 ug/kg intravenously Assay format: organism-based format Standard result: Change = -19.0 %”

    ChEMBL activities for CHEMBL406291 · Activity 130445

    chembl-activities:chembl406291:a7cf8a298b4b:a7cf8a298b4b

Study findings

Bradykinin-mediated angioedema is characterized by painful, nonpruritic edema and lack of response to therapies targeting mast cell pathways.

Sources[4]pubmed[Clinical presentation and diagnosis of bradykinin-mediated angioedema].Bradykinin-mediated angioedema is a rare disease causing painful, nonitching edema not responding to mast cell-directed therapy.
Source records
1
Independent studies
1

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Bradykinin-mediated angioedema is a rare disease causing painful, nonitching edema not responding to mast cell-directed therapy.”

    [Clinical presentation and diagnosis of bradykinin-mediated angioedema]. · BACKGROUND

    pubmed:42640320:8028dd540ab7:8028dd540ab7

Study findings

In an organism-based rat assay quantifying percent change in renal vascular resistance, intravenous CHEMBL406291 at 15 ug/kg was associated with a -37.0% change.

Sources[1]chembl-activitiesChEMBL activities for CHEMBL406291Assay: % Change in renal vascular resistance in rats when administered at dose 15 ug/kg intravenously Assay format: organism-based format Standard result: Change = -37.0 %
Reported result
Change = -37.0 %
Source records
1
Independent studies
1

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Assay: % Change in renal vascular resistance in rats when administered at dose 15 ug/kg intravenously Assay format: organism-based format Standard result: Change = -37.0 %”

    ChEMBL activities for CHEMBL406291 · Activity 130446

    chembl-activities:chembl406291:a7cf8a298b4b:a7cf8a298b4b

Study findings

In an organism-based assay measuring agonistic activity on human umbilical vein (HUV) with inhibitors present, CHEMBL406291 potency was reported as pD2 7.9.

Sources[1]chembl-activitiesChEMBL activities for CHEMBL406291Standard result: pD2 = 7.9
Reported result
pD2 = 7.9
Source records
1
Independent studies
1

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Standard result: pD2 = 7.9”

    ChEMBL activities for CHEMBL406291 · Activity 54725

    chembl-activities:chembl406291:a7cf8a298b4b:a7cf8a298b4b

Risks and interactions

Risks, organized for scanning.

This profile does not yet contain a published summary for this topic. This is a coverage gap, not evidence that no research exists.

Products and regulatory status

Same ingredient. Different records.

This profile does not yet contain a published summary for this topic. This is a coverage gap, not evidence that no research exists.

Administration context

The practical clinical context.

This profile does not yet contain a published summary for this topic. This is a coverage gap, not evidence that no research exists.

Research status + gaps

What still needs better answers?

  • No publishable claim yet for: administration, contraindication, identity, interaction, regulatory, safety
  • 106 compiled claim(s) withheld by automated assurance: assurance_score_below_0.58 (82), assurance_score_below_0.72 (21), current_regulatory_source_required (16), extraction_ambiguity (112), high_risk_requires_regulatory_or_two_independent_sources (21), no_direct_support (102), proposal_not_staged (6)

These are the limits of this profile, not an exhaustive list of scientific uncertainties.

References + discovery

Open the records yourself.

  1. ChEMBL activities for CHEMBL406291 ↗

    chembl-activities · published 2026-08-25 · retrieved 2026-08-25T22:58:23Z

  2. Kallikrein-8 contributes to kallikrein-kinin system dysregulation in Alzheimer's disease. ↗

    pubmed · published 2026-09-01 · retrieved 2026-08-25T22:58:23Z

  3. Real-World Safety and Effectiveness of Icatibant in Patients With Hereditary Angioedema (HAE): Post-Marketing Surveillance in Japan. ↗

    pubmed · published 2026-08-21 · retrieved 2026-08-25T22:58:23Z

  4. [Clinical presentation and diagnosis of bradykinin-mediated angioedema]. ↗

    pubmed · published 2026-08-25 · retrieved 2026-08-25T22:58:23Z

Publication history and provenance

Version 2 · Automated assessment · 2026-08-25T22:58:23Z

5cf9deb04580609472ca40b0e3e4f7bc5df8dc5661706319acbf14aa541fd359