CAS |
137061-48-4 |
English Name |
PACAP-1-38 |
Synonyms |
PituitaryAdenylateCyclaseActivatingPolypeptide38 |
Molecular Formula |
C203H331N63O53S |
Molecular Weight |
4534.26 |
Solubility |
Soluble in Water |
Purity |
≥96% |
Appearance |
White to off-white Solid |
Storage |
Powder:2-8℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year |
MDL |
MFCD00081800 |
SMILES |
--- |
Target Point |
PACAP receptor |
Passage |
Others |
Background |
H-Gly-Gly-Pro-OH is a polypeptide consisting of 3 amino acids. |
Biological Activity |
PACAP (1-38), human, ovine, rat is a neuropeptide with 38 amino acid residues. PACAP (1-38) binds to PACAP type I receptor, PACAP type II receptor VIP1, and PACAP type II receptor VIP2 with IC50s of 4 nM, 2 nM, and 1 nM, respectively.[1-4] |
IC50 |
4nM(PACAP type I receptor);2nM(PACAP type II receptor VIP1);1nM(PACAP type II receptor VIP2)[1] |
In Vitro |
PACAP(1-38),human,ovine,rat is a fragment of pituitary adenylate cyclase activating polypeptide[1]. PACAP(1-38)shows high affinity for PACAP specific(PAC1)receptor in membranes from various tissues including the endocrine pancreas[2]. In vitro,PACAP(1-38)relaxes guinea-pig and rabbit tracheal smooth muscle precontracted by histamine and by acetylcholine. PACAP(1-38)also increases adenosine 3':5'-cyclic monophosphate(cyclic AMP)in tracheal smooth muscle,providing a possible mechanism for the relaxant effect of PACAP(1-38)[3]. |
In Vivo |
PACAP(1-38)alone in sham animals does not result in changes in any of the retinal layers. PACAP(1-38)dissolved in solutio ophthalmica cum benzalkonio leads to significant protection in the retina in bilateral common carotid artery occlusion(BCCAO)-lesioned retinas; retinas treated with PACAP(1-38)eye drops have preserved structure compared to control retinas. OLM-ILM(outer limiting membrane-inner limiting membrane)distance is reduced by 49.7%(p<0.001)in BCCAO retinas compared to sham controls,but it is only 40.6%(p<0.001)in the eyes treated with PACAP(1-38)eye drops. A protection to a similar degree is found in the inner nuclear layer(INL)(BCCAO: 38.5%,PACAP(1-38): 30.5%; p<0.001),and inner plexiform layer(IPL)(BCCAO: 64.8%,PACAP(1-38): 38.2%; p<0.05),while no statistically significant attenuation of the damage is observed in the outer nuclear layer(ONL)(BCCAO: 36.5%,PACAP(1-38): 37.7%)or outer plexiform layer(OPL)(BCCAO: 53.0%,PACAP(1-38): 48.2%). The number of cells in the ganglion cell layer(GCL)is significantly decreased after BCCAO by 52.4%(p<0.05)and is significantly ameliorated by PACAP(1-38)eye drops(decreased by 25.9%; p<0.05)[4]. |
Animal Experiment |
Wistar rats(n=20:n=12 for histological analysis,n=8 for immunohistochemical analysis)weighing 250-300 are fed and watered ad libitum,under light/dark cycles of 12/12 h. Directly after the operation within 1 min,the right eye is treated with PACAP(1-38)eye drops(1 μg/drop). The vehicle used is benzalkonium-chloride in a concentration of 0.005%,as it is the most effective vehicle to achieve neuroprotection with PACAP1-27 eye drops. The left eye serves as a control,treated only with the vehicle. A group of animals serve as the sham-operated group that undergo anesthesia and all steps of the surgical procedure except ligation of the carotid arteries. Rats are treated twice a day with one drop,for 5 consecutive days[4]. |
Data Literature Source |
[1]. Gourlet P,et al. Fragments of pituitary adenylate cyclase activating polypeptide discriminate between type I and II recombinant receptors. Eur J Pharmacol. 1995 Dec 4;287(1):7-11. [2]. Yamaguchi N. Pituitary adenylate cyclase activating polypeptide enhances glucose-evoked insulin secretion in the canine pancreas in vivo. JOP. 2001 Sep;2(5):306-16. [3]. Lindén A,et al. Inhibition of bronchoconstriction by pituitary adenylate cyclase activating polypeptide (PACAP 1-27) in guinea-pigs in vivo. Br J Pharmacol. 1995 Jul;115(6):913-6. [4]. Werling D,et al. Passage through the Ocular Barriers and Beneficial Effects in Retinal Ischemia of Topical Application of PACAP (1-38) in Rodents. Int J Mol Sci. 2017 Mar 21;18(3). pii: E675. |
Unit |
Bottle |
Specification |
1mg |