Published in

General Pharmacology: The Vascular System, 4(26), p. 703-709

DOI: 10.1016/0306-3623(94)00239-j

Links

Tools

Export citation

Search in Google Scholar

Pharmacological properties of MM-706, a new prostacyclin derivative

Journal article published in 1995 by E. Ragazzi ORCID, A. Chinellato, Ü. Lille, U. Lille, M. Lopp, M. G. Doni, Doni Mg, G. Fassina
This paper was not found in any repository, but could be made available legally by the author.
This paper was not found in any repository, but could be made available legally by the author.

Full text: Unavailable

Green circle
Preprint: archiving allowed
Red circle
Postprint: archiving forbidden
Red circle
Published version: archiving forbidden
Data provided by SHERPA/RoMEO

Abstract

. 1. In human platelet-rich plasma, platelet aggregation induced in vitro by collagen (10 μg/ml) or thrombin (50 mU/ml) was dose-dependently inhibited by increasing concentrations of prostacyclin or of the new derivative (±)(5E)-13,14-didehydro-ω-hexanor(1-hydroxycyclohexyl)-9a-carbaprostacyclin (MM-706) with an IC50 of 20–50 nM and 250–500 nM, respectively. In human platelets loaded with fura-2, the intracellular rise of [Ca2+] induced by thrombin was dose-dependently inhibited by MM-706 with an approximate IC50 of 100 μM. 2. 2. In rabbit isolated femoral artery, MM-706 (10nM–10μM) was completely ineffective in relaxing the vessel, which was different to prostacyclin which was able to relax vessels at the same concentrations. 3. 3. In in vitro guinea-pig ileum, prostacyclin produced a contractile effect in the concentration range 1 nM-10μM, but the derivative MM-706 was ineffective at the same concentrations. Preventive addition of MM-706 did not inhibit prostacyclin contraction. 4. 4. On isolated guinea-pig tracheal preparation, prostacyclin induced a concentration-dependent contraction but the new compound MM-706 showed a lower activity, in the concentration range 10nM–10μM. The activity of prostacyclin was not affected by the contemporary presence of MM-706. 5. 5. It is concluded that MM-706 is a prostacyclin analogue with antiaggregating properties but without evident effects on smooth muscle of different regions.