AH 6809 is an EP and DP receptor antagonist with nearly equal affinity for the cloned human EP1, EP2, EP3-III, and DP1 receptors.
AH 6809 细胞实验
Cell Line
Concentration
Treated Time
Description
References
mouse bladder smooth muscle cells
10 μM
AH-6809 (10 μM) significantly reduced the PGE2 (50 μM)-induced change in bladder smooth muscle tone (by 23.7 ±4.4%) but had no significant effect on the frequency of phasic contractions (reduced by 9.7 ±4.7%).
Br J Pharmacol. 2012 Jan;165(2):401-13
guinea-pig tracheal smooth muscle
10 μM
30 min
To assess the effect of AH-6809 on insulin-induced contractions, results showed AH-6809 strongly reduced insulin-induced contractions
Br J Pharmacol. 2007 Jan;150(2):136-42
guinea-pig tracheal smooth muscle
0.2-5 μM
15 min pre-incubation
Antagonized contraction by 17-phenyl-ω-trinor PGE2, pA2=7.35
To evaluate the effect of AH 6809 on PGF2a-induced contraction responses, results showed AH 6809 did not exhibit antagonistic effects
Br J Pharmacol. 2003 Aug;139(8):1409-16
adult pig brain microvessel membranes
10 µM
30 min
AH6809, as an EP1 receptor antagonist, significantly inhibited the binding of [3H]-PGE2 to adult pig brain microvessel membranes by 82-91%.
Br J Pharmacol. 1994 May;112(1):59-64
newborn pig brain microvessel membranes
10 µM
30 min
AH6809, as an EP1 receptor antagonist, significantly inhibited the binding of [3H]-PGE2 to newborn pig brain microvessel membranes by 82-91%.
Br J Pharmacol. 1994 May;112(1):59-64
guinea-pig trachea epithelium-intact strips
10 μM
20 min
To evaluate the effect of EP1/EP2 receptor antagonist on bradykinin-induced relaxation, results showed AH 6809 did not significantly affect BK-induced relaxation.
Br J Pharmacol. 2005 Jul;145(6):740-50
Guinea-pig tracheal cholinergic nerves
10 μM
30 min
To evaluate the effect of AH 6809 on the inhibition of EFS-induced [3H]ACh release by 8-iso-PGE1 and 8-iso-PGE2. Results showed AH 6809 itself had no significant inhibitory effect on cholinergic transmission and did not antagonize the inhibitory actions of 8-iso-PGE1 or 8-iso-PGE2.
Br J Pharmacol. 2004 Feb;141(4):600-9
guinea pig tracheal smooth muscle cells
10 µM
30 min
To investigate the effect of AH-6809 on growth factor-induced contractions, results showed AH-6809 almost completely abolished growth factor-induced contractions
Respir Res. 2005 Jul 27;6(1):85
Rabbit pulmonary smooth muscle cells (PSMC)
3 μM
To investigate the antagonistic effect of AH 6809 on EP1 receptors and its impact on iloprost-induced vasodilation. Results showed that AH 6809 significantly enhanced the vasodilatory effect of iloprost.
Respir Res. 2007 Jan 26;8(1):4
AH 6809 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Rats
Freely moving rats
Continuous infusion into the third ventricle
2.1, 6.3, or 21 pmol/min
From 2300 to 0500 hr
During the infusion at 21 pmol/min, wakefulness decreased to 82%, and SWS and PS increased to 122% and 161%, of the respective baseline values. These changes can be explained by AH 6809 antagonizing the endogenous PGE2 that acts to augment wakefulness in the brain.
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