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Synthesis and biological activities of (R)-5,6-dihydro-N,N-dimethyl-4H-imidazo[4,5,1-ij]quinolin-5-amine and its metabolites.
Efficient syntheses for compounds 3-6 as single enantiomers from quinoline are presented together with information on the biological activities and metabolic stabilities of these compounds.
Pharmacology of U-91356A, an agonist for the dopamine D2 receptor subtype.
In rats, injection of U-91356A produced contralateral turning in rats with unilateral lesions of the substantia nigra, consistent with roles for the dopamine D2 receptor subtype as a dopamine autoreceptor and as a stimulatory, postsynaptic dopamine receptor.
Dopamine D2 receptor binding properties of [3H]U-86170, a dopamine receptor agonist.
This agonist ligand is especially effective in identifying agonists and partial agonists, as well as antagonists, and affords a more precise evaluation of their affinity for the dopamine D2 receptor, without the use of multiple site analysis, than does an antagonist [3H]-ligand.
Analgesic activities of spinal cord substance P antagonists implicate substance P as a neurotransmitter of pain sensation
SP is a natural neurotransmitter for pain and that antagonism of endogenous SP systems causes analgesia, and piperazinone derivatives of substance P's C-terminal hexapeptide are shown to specifically antagonize the scratching induced by i.s. SP.
Dopaminergic and serotonergic activities of imidazoquinolinones and related compounds.
The synthesis of 5-(dipropylamino)-5,6-dihydro-4H-imidazo[4,5,1-ij] quinolin-2(1H)-one (5), a potent dopamine D2 agonist showing high dopamine/serotonin (5HT1A) selectivity, is described.
Cholinergic activity of acetylenic imidazoles and related compounds.
A series of acetylenic imidazoles related to oxotremorine were prepared and evaluated as cholinergic agents with in vitro binding assays and in vivo pharmacological tests in mice, and agonists and antagonists for these compounds at muscarinic receptors are proposed.
Pre- and postsynaptic dopaminergic activities of U-86170F
It is demonstrated that U-86170F is a potent dopamine autoreceptor agonist, with limited activity at the postsynaptic receptor, in the GBL, prolactin, and HVA models.
Medicinal chemistry of imidazoquinolinone dopamine receptor agonists.
(R)-5-(Dipropylamino)-5,6-dihydro-4H-imidazo[4,5,1-ij]-quinolin-2( 1H)-on e (1a), a potent high intrinsic activity dopamine (D2) agonist, has been prepared in eleven steps from quinoline and showed dopamine autoreceptor agonist activity at low doses.