IMMUNEResearch OnlyNEUROPEPTIDEVASODILATORANTI-INFLAMMATORY

VIP

Also known as: Vasoactive Intestinal Peptide · Vasoactive Intestinal Polypeptide · PHM-27

13 views/week 342 citations 0 edits Updated 6/8/2026

VIP (Vasoactive Intestinal Peptide) is an endogenous 28-amino acid neuropeptide produced throughout the gut, brain, and immune tissues. It activates VPAC1 and VPAC2 receptors to produce potent vasodilation, broad-spectrum anti-inflammatory effects, neuroprotection, and immune regulation. It is the primary pharmacological intervention in the Shoemaker CIRS (Chronic Inflammatory Response Syndrome) protocol and has significant emerging research across autoimmunity, pulmonary hypertension, and neurodegeneration.

STRUCTURE

Molecular Composition

FORMULA
C₁₄₇H₂₃₆N₄₄O₄₃S
MOL. WEIGHT
3,326.8 Da
SEQUENCE LENGTH
28 amino acids
CAS NUMBER
37221-79-7
RECEPTORS
VPAC1 · VPAC2
HALF-LIFE
~1–2 min (IV)
AMINO ACID CHAIN VISUALIZATION
H
Histidine
N-terminal VPAC recognition
NH-CO
F
Phe (pos 6)
key receptor binding contact
NH-CO
T
Thr (pos 7)
receptor selectivity
NH-CO
R
Arg (pos 12)
VPAC1/VPAC2 binding hotspot
NH-CO
M
Met (pos 17)
hydrophobic helix core
NH-CO
K
Lys (pos 20)
electrostatic stabilisation
SEQUENCEH-F-T-R-M-K
MECHANISMS

How It Works

🔬
VPAC1/VPAC2 Agonism — cAMP Anti-Inflammatory Cascade
VIP binds VPAC1 and VPAC2 receptors (Kd ~1 nM) on immune cells, smooth muscle, and neurons, activating Gs/adenylyl cyclase and elevating intracellular cAMP. PKA activation downstream suppresses NF-κB signalling, reducing pro-inflammatory cytokine production (TNF-α, IL-6, IL-1β, IL-12) by 60–90% in activated macrophages. Simultaneously, it upregulates IL-10 — shifting the immune tone from inflammatory toward regulatory across innate and adaptive immune compartments.
🫁
Pulmonary Vasodilation & Bronchoprotection
VIP is one of the most potent endogenous dilators of pulmonary vasculature — acting via cAMP-mediated smooth muscle relaxation. VIP deficiency in pulmonary tissue is a documented feature of pulmonary arterial hypertension. Inhaled VIP reduces pulmonary vascular resistance and bronchodilates airway smooth muscle, underpinning its Phase 2 trial results in PAH and its use in CIRS patients with pulmonary dysfunction and reduced VO₂ max.
🧠
Neuroprotection & Circadian Regulation
VIP acts as a neurotrophic factor in the CNS via VPAC receptors, activating CREB and BDNF expression to support neuronal survival and synaptic plasticity. As the primary neurotransmitter of the suprachiasmatic nucleus (SCN), VIP is the master pacemaker of circadian rhythm entrainment — synchronising peripheral clocks throughout the body. VIP deficiency disrupts sleep architecture and cognitive function, consistent with the brain fog and sleep disturbances seen in CIRS.
⚖️
Treg Induction & Autoimmune Regulation
VIP potently promotes CD4+CD25+FoxP3+ regulatory T-cell (Treg) differentiation from naive T-cells while suppressing Th1 and Th17 inflammatory responses. In autoimmune disease models (rheumatoid arthritis, MS, Crohn's), VIP treatment reduces joint inflammation, CNS demyelination, and intestinal damage through Treg-mediated immune tolerance. This makes VIP one of the most promising endogenous anti-autoimmune peptides under investigation.
OVERVIEW

Research Overview

VIP was first isolated from porcine small intestine in 1970 by Said and Mutt and initially characterised as a vasodilatory peptide. Subsequent decades of research revealed it to be one of the most pleiotropic neuropeptides known — with roles spanning gastrointestinal motility, vasodilation, immune modulation, circadian rhythm regulation, neuroprotection, and reproductive function.

VIP is produced by neurons throughout the enteric, central, and peripheral nervous systems, as well as by immune cells (T-cells, mast cells, macrophages). It signals through two G-protein coupled receptors: VPAC1 (widely expressed, high affinity) and VPAC2 (brain, pancreas, peripheral tissues). Both couple to Gs proteins, activating adenylyl cyclase and raising intracellular cAMP — the primary signal mediating most of VIP's downstream effects.

In clinical research, VIP has gained significant attention through the work of Ritchie Shoemaker MD, who identified VIP deficiency as a hallmark of Chronic Inflammatory Response Syndrome (CIRS) — a multi-system illness associated with biotoxin exposure (mould, cyanobacteria, Lyme disease). Intranasal VIP supplementation is now a cornerstone of the Shoemaker CIRS treatment protocol. Beyond CIRS, VIP is under investigation for pulmonary arterial hypertension, inflammatory bowel disease, multiple sclerosis, and COVID-19-related inflammation.

Mechanism of Action

// VPAC1/VPAC2 RECEPTOR AGONISM — cAMP SIGNALLING

VIP binds VPAC1 and VPAC2 receptors with high affinity (Kd ~1 nM), activating Gs-coupled adenylyl cyclase and elevating intracellular cAMP. This triggers PKA (protein kinase A) activation, which phosphorylates transcription factors (CREB) and ion channels responsible for smooth muscle relaxation (vasodilation), immune cell modulation, and neurotrophic gene expression. The breadth of VIP's effects reflects the wide tissue distribution of its receptors.

// POTENT ANTI-INFLAMMATORY ACTION

VIP is one of the most potent endogenous anti-inflammatory agents. In activated macrophages and dendritic cells, it suppresses NF-κB signalling, reducing production of pro-inflammatory cytokines (TNF-α, IL-6, IL-12, IL-1β) while promoting IL-10 (anti-inflammatory). It shifts macrophages from M1 (inflammatory) toward M2 (regulatory) phenotype. In T-cells, VIP suppresses Th1 responses and promotes Treg (regulatory T-cell) differentiation — making it broadly immunosuppressive in inflammatory contexts.

// VASODILATION & PULMONARY EFFECTS

VIP is a potent dilator of pulmonary and systemic vasculature, acting directly on vascular smooth muscle via cAMP-mediated Ca²⁺ channel inhibition. Patients with pulmonary arterial hypertension (PAH) have been shown to have reduced pulmonary VIP expression, and inhaled VIP has been trialled in PAH with significant haemodynamic improvements. VIP also reduces pulmonary vascular resistance and bronchodilates airway smooth muscle — contributing to its interest in CIRS and post-COVID respiratory dysfunction.

// NEUROPROTECTION & CNS EFFECTS

VIP acts as a neurotrophic factor in the CNS, promoting neuronal survival, axonal growth, and synaptic plasticity through VPAC receptor-mediated CREB activation and BDNF upregulation. It is produced by interneurons in the cortex and hippocampus and modulates circadian rhythms through the suprachiasmatic nucleus (SCN). VIP deficiency has been linked to neuroinflammatory conditions and disrupted sleep-wake cycles — consistent with the cognitive and sleep symptoms observed in CIRS patients.

DOSAGE

Dosage & Administration

INTRANASAL — SHOEMAKER CIRS PROTOCOL
DOSE
50 µg (1 spray per nostril)
FREQUENCY
4× daily (morning, midday, evening, bedtime)
NOTES
The Shoemaker protocol uses 50 µg intranasal VIP 4 times daily — typically as a 50 µg/mL solution delivering 1 spray per nostril per dose. This route provides localised mucosal effects plus partial systemic absorption. VIP must be compounded by a specialised pharmacy. Prerequisites in the Shoemaker protocol: prior treatment steps (cholestyramine, nasal antifungals, VCS test normalisation) must be completed before VIP is started to avoid triggering an inflammatory flare.
INJECTABLE (SUBCUTANEOUS) — RESEARCH PROTOCOL
DOSE
2–10 µg/kg
FREQUENCY
Once daily or every other day
NOTES
Injectable VIP is used in research settings for systemic anti-inflammatory and cardiopulmonary effects. Doses are weight-based due to the potent vasodilatory effects at higher concentrations (hypotension risk). Start at the lower end (2 µg/kg) and assess cardiovascular tolerance. The extremely short plasma half-life (~1–2 min IV) means SQ injection provides a slower absorption profile more amenable to outpatient use.

VIP is an endogenous peptide with a strong physiological safety profile. The primary acute adverse effects at therapeutic doses are vasodilatory: facial flushing, transient drop in blood pressure, and mild tachycardia — dose-dependent and short-lived given the 1–2 minute half-life. Intranasal administration (Shoemaker protocol) is generally well-tolerated with minimal systemic vasodilation at 50 µg doses. VIP requires compounding pharmacy preparation and specialised storage. It degrades rapidly at room temperature — always store cold and use freshly reconstituted preparations. In the CIRS context, VIP should only be used after prior detoxification steps are completed; premature use can worsen inflammatory symptoms.

CYCLING

Cycle Duration Guide

ON CYCLE
3–6 months (CIRS protocol); ongoing with monitoring
OFF CYCLE
Gradual dose reduction rather than abrupt cessation

In the Shoemaker CIRS protocol, VIP is used for extended periods (months) with periodic assessment of inflammatory biomarkers (TGF-β1, MMP-9, VEGF) to guide dosing. Unlike peptides with receptor desensitisation, VIP does not typically cause tachyphylaxis — VPAC1/VPAC2 receptor expression is maintained with continued use. Patients with CIRS often require extended courses as the underlying biotoxin-driven inflammation is a chronic process.

VIP causes vasodilation and blood pressure reduction — use with caution in patients with pre-existing hypotension, cardiac arrhythmias, or on antihypertensive medications. In the Shoemaker protocol, VIP must be the final step after prior treatment phases are complete; skipping protocol steps significantly increases the risk of adverse inflammatory reactions.

NOTES

Research Notes

CIRS (Shoemaker Protocol): Ritchie Shoemaker's research identified low VIP levels in patients with CIRS — a complex multi-system illness following biotoxin exposure. Intranasal VIP (50 µg 4×/day) has been shown to normalise inflammatory markers (TGF-β1, MMP-9), improve VO2 max, restore pulmonary function, and reduce symptom burden in CIRS patients. This remains the most clinically detailed human application of VIP to date, though it lacks large double-blind RCT validation.

Pulmonary arterial hypertension: A Phase 2 trial (Said et al.) of inhaled VIP in PAH showed significant reductions in pulmonary vascular resistance and improvements in exercise capacity. VIP deficiency in pulmonary vasculature is well-documented in PAH pathophysiology.

COVID-19 / post-COVID: VIP's anti-inflammatory profile generated strong interest during the COVID-19 pandemic. Observational data showed VIP levels inversely correlated with COVID severity. Multiple trials of inhaled/IV VIP in severe COVID-19 were conducted; some showed cytokine reduction and clinical improvement. Post-COVID syndrome research continues to explore VIP deficiency as a contributing mechanism to long COVID symptoms.

Autoimmune applications: Preclinical studies demonstrate therapeutic effects of VIP in rheumatoid arthritis, Crohn's disease, multiple sclerosis, and lupus models. Human trials are limited but the anti-inflammatory mechanism is well-validated.

Quick Reference
FORMULAC₁₄₇H₂₃₆N₄₄O₄₃S
MOL. WEIGHT3,326.8 Da
LENGTH28 amino acids
ORIGINEndogenous neuropeptide; expressed in enteric nervous system, CNS, and immune cells. First isolated from porcine intestine by Said & Mutt (1970).
HALF-LIFE~1–2 minutes (IV); intranasal administration provides localised effects with systemic absorption
SOLUBILITYWater-soluble; available as lyophilized powder for reconstitution
CAS NO.37221-79-7
STATUSResearch Only
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TAGS
neuropeptidevasodilatoranti-inflammatoryVPAC1VPAC2CIRSneuroprotectivegut-brain axisautoimmune