Catecholamine receptors and cyclic and formation in the central nervous system: Effects of tetrahydroisoquinoline derivatives

Salsolinol Produces Reinforcing Effects in the Nucleus Accumbens Shell of Alcohol‐Preferring (P) Rats

“…Furthermore, within the shell of the nucleus accumbens, the reinforcing doses of SAL are 1000-fold lower than cocaine (Rodd-Henricks et al, 2002a) and 300-fold lower than the D1/D2 agonist combination (Ikemoto et al, 1997a). However, mechanisms other than interactions with the D2 receptor are likely involved in the ICSA of SAL, because quinpirole and dopamine have a 1000-fold higher affinity (Seeman and Van Tol, 1994) than SAL (Nimitkitpaisan and Skolnick, 1978) for the D2-like receptor. One possible mechanism mediating the reinforcing effects of SAL may involve the enhanced release of dopamine and serotonin, because local application of R-SAL can markedly increase the extracellular concentrations of these monoamines (Maruyama et al, 1992(Maruyama et al, , 1993Nakahara et al, 1994).…”

Interaction of catecholamine‐derived alkaloids with central neurotransmitter receptors

“…Receptor binding assays demonstrate that salsolinol is not particularly effective in displacing radioligands from a land 0, -adrenergic receptors or dopaminergic receptor antagonist sites [Nimitkitpaisan and Skolnick, 19781. Although ineffective in interaction with a1 -adrenergic receptors, tetrahydropapaveroline is a potent inhibitor of the binding of PI -adrenergic receptor ligands and also of radioligand binding to dopamine receptor antagonist sites [Nimitkitpaisan and Skolnick, 1978;Brossi et al, 19801. The S-(-) enantiomer of tetrahydropapaveroline is more potent than the R-( +) form in displacing radioligands from ,B1 -adrenergic receptors and dopamine receptor antagonist sites [Nimitkitpaisan and Skolnick, 1978;Brossi et al, 19801.…”

Recent advances in the biochemical aspects of alcohol addiction

“…The possibility that alcohol addiction is related to the formation of alkaloid derivatives in the brain that interact in some way with the endogenous ligand-receptor system, must now be seriously considered. In support of these findings, tetrahydropapaveroline and salsolinol have been shown to affect catecholamine formation in the central nervous system (Nimitkitpaisan & Skolnick, 1978) and using a sensitive radioenzymatic assay, Dean et al, 1980, have detected formation of salsolinol in whole brain homogenates following incubation with physiologic concentrations of acetaldehyde. This behaviour was accompanied by symptoms similar to that of withdrawal and intoxication.…”

“…Only picomoles of the alkaloid were required within the brain to trigger aberrent drinking. In support of these findings, tetrahydropapaveroline and salsolinol have been shown to affect catecholamine formation in the central nervous system (Nimitkitpaisan & Skolnick, 1978) and using a sensitive radioenzymatic assay, Dean et al, 1980, have detected formation of salsolinol in whole brain homogenates following incubation with physiologic concentrations of acetaldehyde.…”