» Articles » PMID: 7834182

Blockade of P2X-purinoceptors by Trypan Blue in Rat Vas Deferens

Overview
Journal Br J Pharmacol
Publisher Wiley
Specialty Pharmacology
Date 1994 Oct 1
PMID 7834182
Citations 8
Authors
Affiliations
Soon will be listed here.
Abstract

1. The possibility of an antagonist effect of trypan blue at P2X-purinoceptors was studied in rat vas deferens. 2. Trypan blue (3.2-320 microM) shifted the concentration-contraction response curve of alpha,beta-methylene ATP (alpha,beta-MeATP) to the right and simultaneously increased the maximum of the curve by up to 40%. The Schild plot had a slope not significantly different from unity and yielded a pA2 value of 5.3 (KB 4.9 microM). 3. Suramin (32 microM) also shifted the concentration-response curve of alpha,beta-MeATP to the right, KB 2.6 microM, and increased the maximum by 31%. In the presence of suramin (32 microM), trypan blue (32 microM) did not change the concentration-response curve of alpha,beta-MeATP. 4. 1-Amino-8-naphthol-3, 6-disulphonate (H-acid) 10 mM, the sulphonic acid-carrying moiety of trypan blue, shifted the concentration-response curve of alpha,beta-MeATP to the right, KB 1.4 mM, and increased the maximum by 33%. 5. Trypan blue did not change contractions elicited by high K+ and noradrenaline. 6. Trypan blue attenuated the purinergic component of neurogenic contractions, IC50 44.9 microM, but did not change the adrenergic component. 7. It is concluded that trypan blue blocks P2X-purinoceptors in rat vas deferens. The increase of the maximum of the alpha,beta-MeATP concentration-response curve is similar in mechanism to the increase produced by suramin.

Citing Articles

P2X receptors as drug targets.

North R, Jarvis M Mol Pharmacol. 2012; 83(4):759-69.

PMID: 23253448 PMC: 3608433. DOI: 10.1124/mol.112.083758.


New insights on P2X purinoceptors.

Humphrey P, Buell G, Kennedy I, Khakh B, Michel A, Surprenant A Naunyn Schmiedebergs Arch Pharmacol. 1995; 352(6):585-96.

PMID: 9053729 DOI: 10.1007/BF00171316.


Evaluation of P2-purinoceptor antagonists at two relaxation-mediating P2-purinoceptors in guinea-pig taenia coli.

Bultmann R, Dudeck O, Starke K Naunyn Schmiedebergs Arch Pharmacol. 1996; 353(4):445-51.

PMID: 8935712 DOI: 10.1007/BF00261442.


P2-purinoceptor antagonists: III. Blockade of P2-purinoceptor subtypes and ecto-nucleotidases by compounds related to suramin.

Bultmann R, Wittenburg H, Pause B, KURZ G, Nickel P, Starke K Naunyn Schmiedebergs Arch Pharmacol. 1996; 354(4):498-504.

PMID: 8897454 DOI: 10.1007/BF00168442.


P2-purinoceptor antagonists: II. Blockade of P2-purinoceptor subtypes and ecto-nucleotidases by compounds related to Evans blue and trypan blue.

Wittenburg H, Bultmann R, Pause B, Ganter C, KURZ G, Starke K Naunyn Schmiedebergs Arch Pharmacol. 1996; 354(4):491-7.

PMID: 8897453 DOI: 10.1007/BF00168441.


References
1.
von Kugelgen I, Bultmann R, Starke K . Interaction of adenine nucleotides, UTP and suramin in mouse vas deferens: suramin-sensitive and suramin-insensitive components in the contractile effect of ATP. Naunyn Schmiedebergs Arch Pharmacol. 1990; 342(2):198-205. DOI: 10.1007/BF00166965. View

2.
Kennedy C . P1- and P2-purinoceptor subtypes--an update. Arch Int Pharmacodyn Ther. 1990; 303:30-50. View

3.
BLAKELEY A, Brockbank J, Kelly S, Petersen S . Effects of suramin on the concentration--response relationship of alpha, beta-methylene ATP on the mouse vas deferens. J Auton Pharmacol. 1991; 11(1):45-9. DOI: 10.1111/j.1474-8673.1991.tb00243.x. View

4.
Lambrecht G, Friebe T, Grimm U, Windscheif U, Bungardt E, Hildebrandt C . PPADS, a novel functionally selective antagonist of P2 purinoceptor-mediated responses. Eur J Pharmacol. 1992; 217(2-3):217-9. DOI: 10.1016/0014-2999(92)90877-7. View

5.
Boland B, Himpens B, Vincent M, Gillis J, Casteels R . ATP activates P2x-contracting and P2y-relaxing purinoceptors in the smooth muscle of mouse vas deferens. Br J Pharmacol. 1992; 107(4):1152-8. PMC: 1907937. DOI: 10.1111/j.1476-5381.1992.tb13422.x. View