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| Content Provider | PubMed Central |
|---|---|
| Author | Eglen, R. M. Whiting, R. L. |
| Abstract | 1. Enprostil is composed, in approximately equal proportions, of 4 allenic isomers which are prostanoids structurally related to prostaglandin E2 (PGE2). The isomers are denoted as RS-86505-007, RS-86812-007 which are in the 'natural' R and S configuration (with respect to PGE2) and RS-86505-008 and RS-86812-008 which are in the 'unnatural' R and S configuration. In the present study we have characterized their activity at prostanoid receptors, in vitro. 2. Enprostil acted as a highly potent (-log EC50 = 8.30 +/- 0.08; mean +/- s.e.mean, n = 6) EP3 receptor agonist in the guinea-pig vas deferens, although no activity was observed at guinea-pig tracheal EP2 receptors at concentrations up to and including 10 microM. Attempts to study the action of enprostil at EP1 receptors were complicated by a general increase in the spontaneous activity of the guinea-pig isolated ileum. This response was stereospecific (i.e. observed, with the 'natural' R and S isomers only) and was not mediated through EP1, FP or TP receptors. 3. Enprostil also exhibited a potent agonist effect at FP and TP receptors in the rat colon and guinea-pig aorta (-log EC50 values = 7.34 +/- 0.11 and 6.54 +/- 0.07, mean +/- s.e. mean, n = 4-8 respectively). No activity at concentrations up to and including 10 microM was observed at DP or IP receptors in the guinea-pig platelet mediating inhibition of ADP-induced aggregation.(ABSTRACT TRUNCATED AT 250 WORDS) |
| Starting Page | 1335 |
| File Format | |
| ISSN | 00071188 |
| Journal | British Journal of Pharmacology |
| Issue Number | 4 |
| Volume Number | 98 |
| Language | English |
| Publisher Date | 1989-12-01 |
| Access Restriction | Open |
| Subject Keyword | Research in Higher Education |
| Content Type | Text |
| Resource Type | Article |
| Subject | Pharmacology |
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