A structure–function study of PACAP using conformationally restricted analogs: Identification of PAC1 receptor-selective PACAP agonists

Conformationally Restricted Fentanyl Analogs

Synthesis, analgesic activity and preliminary molecular modeling studies of the cisand trans-fused octahydro-l,2,3,4,4a,5,11,1 la-pyrido[3,4-c][1,5]benzoxazepines 8 and 9, the first rigid fentanyl analogs with a conformationally restricted 4-anilido group that retain antinociceptive properties, are reported. Fentanyl (1) is the prototype of the highly potent 4-anilidopiperidine class of synthet...

Altered Circadian Food Anticipatory Activity Rhythms in PACAP Receptor 1 (PAC1) Deficient Mice

Light signals from intrinsically photosensitive retinal ganglion cells (ipRGCs) entrain the circadian clock and regulate negative masking. Two neurotransmitters, glutamate and Pituitary Adenylate Cyclase Activating Polypeptide (PACAP), found in the ipRGCs transmit light signals to the brain via glutamate receptors and the specific PACAP type 1 (PAC1) receptor. Light entrainment occurs during th...

"PACAP and PAC1 receptor signaling in chronic stress responses: Implications for anxiety-related disorders."

PACAP causes PAC1/VPAC2 receptor mediated hypertension and sympathoexcitation in normal and hypertensive rats.

Pituitary adenylate cyclase-activating polypeptide (PACAP) is an excitatory neuropeptide that plays an important role in hypertension and stress responses. PACAP acts at three G protein-coupled receptors [PACAP type 1 receptor (PAC(1)) and vasoactive intestinal peptide receptor types 1 and 2 (VPAC(1) and VPAC(2))] and is localized to sites involved in cardiovascular control, most significantly ...

Identification of key residues that cause differential gallbladder response to PACAP and VIP in the guinea pig.

Pituitary adenylate cyclase-activating polypeptide (PACAP) and vasoactive intestinal polypeptide (VIP) have opposite actions on the gallbladder; PACAP induces contraction, whereas VIP induces relaxation. Here, we have attempted to identify key residues responsible for their interactions with PACAP (PAC1) and VIP (VPAC) receptors in the guinea pig gallbladder. We synthesized PACAP-27/VIP hybrid ...