Effect of 3-PPP, a putative dopamine autoreceptor agonist, on [3H]ligand binding to dopamine receptors of calf and rat striatum
✍ Scribed by David T. Wong; Penny G. Threlkeld; Leroy R. Reid
- Publisher
- John Wiley and Sons
- Year
- 1983
- Tongue
- English
- Weight
- 467 KB
- Volume
- 3
- Category
- Article
- ISSN
- 0272-4391
No coin nor oath required. For personal study only.
✦ Synopsis
Effect of 3-PPP, a putative dopamine autoreceptor agonist, on [3H]ligand binding to dopamine receptors of calf and rat striatum. Drug Dev. Res. 3:177-184, 1983. 3-(3-Hydroxyphenyl)-N-n-propyliperidine (3-PPP) is most effective in inhibiting I3HJapomorphine binding in rat striatal membranes, with Ki values of 63 nM. 3-PPP was six to 27 times less effective when it competed with the binding of [3H]dopamine or [3H]spiperone in calf and rat striatal membranes. At concentrations up to 10 pM, 3-PPP failed to substitute for dopamine in the activation of adenylate cyclase in rat striatal membranes. 3-PPP at 4.8-5 pM caused 50% inhibition of catecholamine uptake in synaptosomes of corpus striatum and hypothalamus, therefore appearing to be a relatively weak uptake inhibitor. The higher affinity of 3-PPP for [3H]apomorphine binding sites is consistent with its binding to a subset of dopamine receptors which are characterized by a high affinity for both the agonist and antagonist of dopamine.