VIP and PACAP Receptor Pharmacology | Zendy

DICKSON LOUISE | Zendy; ARAMORI ICHIRO | Zendy; SHARKEY JOHN | Zendy; FINLAYSON KEITH | Zendy

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VIP and PACAP Receptor Pharmacology

Author(s) -

DICKSON LOUISE,

ARAMORI ICHIRO,

SHARKEY JOHN,

FINLAYSON KEITH

Publication year - 2006

Publication title -

annals of the new york academy of sciences

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 1.712

H-Index - 248

eISSN - 1749-6632

pISSN - 0077-8923

DOI - 10.1196/annals.1317.021

Subject(s) - pharmacology , receptor , chemistry , medicine

VIP/PACAP receptor activation stimulates the production of [cAMP] i and [Ca 2+ ] i by coupling to independent G‐protein subunits, although agonist potencies for the different transduction pathways appear to differ. Using CHO‐K1 cells stably expressing the human VIP/PACAP receptors (hVPAC 1 R, hVPAC 2 R, and hPAC 1 R), functional assays ([cAMP] i and [Ca 2+ ] i ) were established and the receptor pharmacology was characterized with five peptide agonists (VIP, PACAP‐27, PACAP‐38, [Ala 11,22,28 ]VIP, and R3P65). The rank order of potency (ROP) was consistent between assays for the individual receptor subtypes, however, higher agonist concentrations (∼100‐fold) were required for stimulating [Ca 2+ ] i when compared to [cAMP] i .

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