Classification of drugs according to receptor binding profiles
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Summary
The affinity for eight different neurotransmitter receptors of about fourty drugs, used for the treatment of various central nervous system disorders, was determined following in vitro receptor binding assays. Our findings indicate that, in spite of widely varying chemical structures and often poorly understood mechanisms of action, the similarities in the “affinity profiles” permit a clinically meaningful classification of these drugs. Such an approach would thus be useful in the assessment of newly synthesized compounds at an early stage of drug development.
Key words
Ergot alkaloids Antiparkinson agents Neuroleptics Antidepressants CNS-receptors Affinities to multiple binding sitesPreview
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References
- Agid Y, Bonnet AM, Pollak P, Signoret JL, Lhermitte F (1979) Bromocriptine associated with a peripheral dopamine blocking agent in treatment of Parkinson's disease. Lancet 570–572Google Scholar
- Berde B, Schild HO (1978) Ergot-alkaloids and related compounds, Handb Exp Pharmacol, vol 49. Springer, Berlin Heidelberg New YorkGoogle Scholar
- Bevan P, Bradshaw CM, Pun RYK, Slater NT, Szabadi E (1979) The action of microelectrophoretically applied (3,4-dihydroxyphenylamino)-2-imidazoline (DPI) on single cortical neurones. Br J Pharmacol 65:701–706Google Scholar
- Burt DR, Creese I, Snyder SH (1976b) Binding interactions of lysergic acid diethylamide and related agents with dopamine receptors in brain. Mol Pharmacol 12:631–638Google Scholar
- Burt DR, Creese I, Snyder SH (1976b) Properties of [3H]haloperidol and [3H]dopamine binding associated with dopamine receptors of calf brain membranes. Mol Pharmacol 12:800–812Google Scholar
- Caron MG, Beaulieu M, Raymond V, Gagné B, Drouin J, Lefkowitz RJ, Labrie F (1978) Dopaminergic receptors in the pituitary gland. Correlation of [3H]dihydroergocryptine binding with the dopaminergic control of prolactin release. J Biol Chem 253:2244–2253Google Scholar
- Closse A, Frick W, Hauser D, Sauter A (1980) Characterization of [3H]-bromocriptine binding to calf caudate membranes. In: Yamamura HI, Olsen RW, Usdin E (eds) Psychopharmacology and biochemistry of neurotransmitter receptors, developments in neuroscience, vol 11, Elsevier North Holland, New York Amsterdam Oxford, pp 463–474Google Scholar
- Closse A, Bolliger G, Dnavid A, Frick W, Hauser D, Pfäffli P, Sauter A, Tobler HJ (1983) Structural modification of the ergopeptine molecule and their differential influence on the affinities to different receptor binding sites, a structure affinity analysis. In: Segawa T, Yamamura HT, Kuriyama K (eds) Molecular pharmacology of neurotransmitter receptors. Raven Press, New York, pp 269–279Google Scholar
- Creese I, Schneider R, Snyder SH (1977) [3H]Spiroperidol labels dopamine receptors in pituitary and brain. Eur J Pharmacol 46:377–381Google Scholar
- Creese I (1981) Receptors for psychoactive drugs in the central nervous system. In: Cotman W, Poste G, Nicolson GL (eds) The cell surface and neuronal function. Elsevier/North Holland Biomedical Press, New York Amsterdam Oxford, pp 261–301Google Scholar
- Creese I (1981) Dopamine receptors. In: Yamamura HI, Enna SJ (eds) Receptors and recognition ser B., vol. 10, Neurotransmitter receptors, part 2, Biogenic amines. Chapman and Hall, London New York, pp 129–183Google Scholar
- Davis JN, Strittmatter WJ, Hoyler E, Lefkowitz RJ (1977) [3H]Dihydroergocryptine binding in rat brain. Brain Res 132:327–336Google Scholar
- Deakin JFW, Owen F, Cross AJ, Dashwood MJ (1981) Studies of possible mechanisms of action of electroconvulsive therapy; effects of repeated electrically induced seizures on rat brain receptors for monoamines and other neurotransmitters. Psychopharmacology 73:345–349Google Scholar
- Dolphin A, Enjalbert A, Tassin JP, Luas M, Bockaert J (1978) Direct interaction of LSD with central “beta”-adrenergic receptors. Life Sci 22:345–351Google Scholar
- Enna SJ, Kendall DA (1981) Interaction of antidepressants with brain neurotransmitter receptors. J Clin Psychopharmacol 1:(Suppl.) 12–16Google Scholar
- Enna SJ, Mann E, Kendall D, Stancel GM (1981) Effect of chronic antidepressant administration on brain neurotransmitter receptor binding. In: Enna SJ, Malick JB, Richelson E (eds) Antidepressants: Neurochemical, behavioral and clinical perspectives. Raven Press, New York, pp 91–105Google Scholar
- Enz A (1981) Biphasic influence of a 8α-amino ergoline, CU 32-085, on striatal dopamine synthesis and turnover in vivo in the rat. Life Sci 29:2227–2234Google Scholar
- Fillion GMB, Roussell JC, Fillion MP, Beaudoin DM, Goiny MR, Deniau JM, Jacob JJ (1978) High-affinity binding of [3H]5-hydroxytryptamine to brain synaptosomal membranes: Comparison with [3H]lysergic acid diethylamide binding. Mol Pharmacol 14:50–59Google Scholar
- Goldstein M, Lew JY, Engel J (1980) Relevance of dopamine receptor binding studies for evaluation of antiparkinsonian drugs. In: Hanin I, Koslow SH (eds) Physico-chemical methodologies in psychiatric research. Raven Press, New York, pp 103–109Google Scholar
- Green JP, Johnson CL, Weinstein H, Maayani S (1977) Antagonism of histamine activated adenylate cyclase in brain by d-lysergic acid diethylamide. Proc Natl Acad Sci 74:5697–5701Google Scholar
- Greenberg DA, Snyder SH (1978) Pharmacological properties of [3H]dihydroergocryptine binding sites associated with alphanoradrenergic receptors in rat brain membranes. Mol Pharmacol 14:38–49Google Scholar
- Haga T, Haga K (1980) Characterization of alpha-adrenergic receptor subtypes in rat brain: estimation of ability of adrenergic ligands to displace [3H]dihydroergocryptine from the receptor subtypes. Life Sci 26:211–218Google Scholar
- Hall H, Oegren SO (1981) Effect of antidepressant drugs on different receptors in the brain. Eur J Pharmacol 70:393–407Google Scholar
- Hamblin M, Creese I (1980) Phenoxybenzamine discriminates multiple dopamine receptors. Eur J Pharmacol 65:119–121Google Scholar
- Hamon M, Mallat M, Herbet A, Nelson DL, Audinot M, Pichat L, Glowinski J (1981) [3H]Metergoline: a new ligand of serotonin receptors in the rat brain. J Neurochem 36:613–626Google Scholar
- Loew DM, Vigouret JM (1981) Pharmacological approaches to geronto-psychiatry. In: Handbook of experimental pharmacology, vol 55/11. Springer, Berlin Heidelberg New York, pp 435–459Google Scholar
- Ludin HP, Bass-Verrey F (1976) Study of deterioration in long-term treatment of Parkinsonism with l-DOPA plus decarboxylase inhibitor. J Neural Transm 38:249–258Google Scholar
- Marsden CD, Parkes JD (1977) Success and problems of long-term levodopa therapy in Parkinson's disease. Lancet 345–349Google Scholar
- Heyck H (1982) Der Kopfschmerz. Thieme, StuttgartGoogle Scholar
- Parli CJ, Schmidt B, Shaar CJ (1978) Metabolism of lergotrile to 13-hydroxylergotrile, a potent inhibitor of prolactin in vitro. Biochem Pharmacol 27:1405–1408Google Scholar
- Peroutka SJ, Snyder SH (1979) Multiple serotonin receptors: Differential binding of [3H]5-hydroxytryptamine, [3H]lysergic acid diethylamide and [3H]spiroperidol. Mol Pharmacol 16:687–699Google Scholar
- Peroutka SJ, Snyder SH (1980) Relationship of neuroleptic drug effects at brain dopamine, serotonin, α-adrenergic and histamine receptors to clinical potency. Am J Psychiat 137:1518–1522Google Scholar
- Peroutka SJ, Snyder SH (1981) Interactions of antidepressants with neurotransmitter receptor sites. In: Enna SJ, Coyle JT (eds) Antidepressants: Neurochemical, behavioral and clinical perspectives. Raven Press, New York, pp 75–90Google Scholar
- Ringwald E, Hirt D, Markstein R, Vigouret J-M (1982) Dopaminrezeptoren Stimulatoren in der Behandlung der Parkinsonkrankheit. Nervenarzt 53:67–71Google Scholar
- Seeman P (1981) Brain dopamine receptors. Pharmacol Rev 32:229–313Google Scholar
- Stefanini E, Marchisio AM, Devoto P, Vernaleone F, Collu P, Spano PF (1980) Sodium dependent interaction of benzamides with dopamine receptors. Brain Res 198:229–233Google Scholar
- Struyker-Boudier H, Teppema L, Cools A, van Rossum J (1975) (3,4)Dihydroxyphenylamino)-2-imidazoline (DPI), a new potent agonist at dopamine receptors mediating neuronal inhibition. J Pharmacol 27:882–883Google Scholar
- Stuetz P, Stadler P, Vigouret JM, Jaton A (1982) Derivate von (5R,8S,10R)-8-Amino-6-methylergolin als zentral wirksame dopaminerge Stimulantien. Eur J Med Chem — Chim Ther 17:537–541Google Scholar
- Thorner MO, Flückiger E, Calne DB (1980) Bromocriptine, a clinical and pharmacological review. Raven Press, New YorkGoogle Scholar
- Titeler M, Weinreich P, Seeman P (1977) New detection of brain dopamine receptors with [3H]dihydroergocrytpine. Proc Natl Acad Sci 74:3750–3755Google Scholar
- Tran VT, Chang RSL, Snyder SH (1978) Histamine-H1 receptor identified in mammalian brain membranes with [3H]mepyramine. Proc Natl Acad Sci 75:6290–6294Google Scholar
- U'Prichard DC, Greenberg DA, Snyder SH (1977a) Binding characteristics of a radiolabelled agonist and antagonist at central nervous system alpha noradrenergic receptors. Mol Pharmacol 13:454–473Google Scholar
- Wastek GJ, Yamamura HI (1978) Biochemical characterization of the muscarinic cholinergic receptor in human brain: alterations in Hungtington's disease (slightly varied). Mol Pharmacol 14:768–780Google Scholar
- Williams LT, Lefkowitz RJ (1976) Alpha-adrenergic receptor identification by [3H]dihydroergocriptine binding. Science 192:791–793Google Scholar
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