Biological Information

Background Information:

Pituitary adenylate cyclase–activating polypeptide (PACAP) is a ubiquitous neuropeptide of the vasoactive intestinal peptide (VIP) family. PACAP exists in 2 forms; one as a 38 aa peptide (PACAP-38) and a C-terminally truncated, 27aa form of the peptide (PACAP-27). PACAP type I receptor has high affinity for both PACAP peptides and is expressed predominantly in the CNS (most abundantly in the olfactory bulb, thalamus, hypothalamus, the dentate gyrus of the hippocampus and in granule cells of the cerebellum. Studies on PAC1 receptor knockout mice point to a role for presynaptic PAC1-mediated signalling at the mossy fibre synapse in long-term potentiation (LTP) and hippocampus-dependent associative learning. The PAC1 receptor is also expressed in brain areas which have been implicated in the emotional control of behavior, such as the amygdala, the hypothalamus, the locus coeruleus and the periaqueductal grey. Consistent with this, mice with a ubiquitous but not with a forebrain-specific deletion of the PAC1 receptor exhibited elevated locomotor activity and strongly reduced anxiety-like behavior. It is also expressed on pancreatic β-cells and has been implicated in the control of pancreatic insulin secretion.

No. of Assays on Panel:

2

Assays on Panel:

Family

GPCR

Name

Item

1843

Protein

PAC1 (PACAP)

Organism

Human

Assay Sub Type

Cell Based

Family

GPCR

Name

Item

1844

Protein

PAC1 (PACAP)

Organism

Human

Assay Sub Type

Cell Based

Family:

GPCR

Sub Family:

VIP and PACAP

Class:

Class B

Protein Name:

PAC1 (PACAP)

Uniprot Number:

P41586

Protein Aliases:

PACAP-R-1|PACAP-R1|PACAP receptor 1

Gene Name:

ADCYAP1R1

Gene ID:

117

Gene Aliases:

PAC1|PACAPR|PAC1R

Organism:

Human

Cell Type:

CHO-K1

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

Agonist & Antagonist

Detection Method:

HTRF

Testing Information

Incubation:

30 min at RT

Control Activator:

PACAP1-38 (0.1 nM)

Test Concentration / Dose:

Eurofins will provide IC/EC50 calculation if 5 or more concentrations are selected.

Test Sample Requirements:

Minimum for 1) Screen: 60 µL of 10 mM stock -OR- 1 mg (pre-weighed) for 10µM finµL testing. 2) Dose Response: 90 µL of 10 mM stock -OR- 1 mg (pre-weighed) for a top concentration at 10 µM.

Minimum Order Quantity:

16

Turnaround Time

Standard:

15 Business Days

Clinical Relevance

Therapeutic Area:

Metabolic Diseases

Adverse / Beneficial Action:

PAC1 receptor deficient mice display impaired insulinotropic response to glucose, reduced glucose tolerance and impaired glucagon response to insulin-induced hypoglycaemia. PAC1 receptor mRNA is constitutively expressed in macrophages and monocytes. PACAP, acting through the PAC1 receptor appears to be protective against endotoxin-induced septic shock, acting at least in part by attenuating lipopolysaccharide-induced production of proinflammatory interleukin-6.

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault

RELATED SOLUTIONS

Item: 1518
Item: 1843
Item: 1844