Disease relevance of Tetrahydro-beta-naphthylamine

• In vitro metabolism models have been used to determine the relative metabolic stability of novel 2-aminotetralin analogues for the treatment of CNS diseases [1].

Psychiatry related information on Tetrahydro-beta-naphthylamine

• Comparison of the anorectic and motor activity effects of some aminoindanes, 2-aminotetralin and amphetamine in the rat [2].

High impact information on Tetrahydro-beta-naphthylamine

• The fact that 11 (Ki = 206 microM) is more potent than analogues 4 (Ki = 1296 microM) and 5 (Ki = 479 microM), with a half-boat 2AT moiety, suggests that PNMT preferentially binds the half-chair conformation of 2AT at the active site [3].
• The results of the present study show that this bulky functionality is also tolerated by the receptor when incorporated into examples of all other major classes of 5-HT1A agents (e.g., 2-aminotetralin, phenylalklamine, indolylalkylamine, and (aryloxy)alkylamine derivatives) [4].
• The corresponding trans isomer 10 is not a substrate, in spite of enhanced active site interactions with respect to the parent analogue (2-aminotetralin, 4) [5].
• An improved route to 2-aminotetralin systems has been utilized for some of the compounds, which involves Pummerer rearrangement and cyclization of beta-keto sulfoxides and reductive amination of beta-tetralones with a NaBH4-carboxylic acid complex [6].
• In our attempts to elucidate the prolactin release inhibiting pharmacophore within the ergoline structure, we have prepared one indolealkylamine and several 2-aminotetralin derivatives [7].

Biological context of Tetrahydro-beta-naphthylamine

• 2-Aminotetralin, the most flexible of the analogs (capable of assuming both gauche and anticonformations), was the most potent (IC50, 22 microM) [8].
• Substrate selectivity resulted in much faster deamination of 1-aminoindane and 1-aminotetralin than of the corresponding 2-amino compounds, especially in rats [9].
• Antinicotinic activity of some 2-aminotetralin derivatives. A structure-activity relationship study [10].

Anatomical context of Tetrahydro-beta-naphthylamine

• Differential activation by some 2-aminotetralin derivatives of the receptor mechanisms in the nucleus accumbens of rats which mediate hyperactivity and stereotyped biting [11].
• The interactions of 5,6- and 6,7-dihydroxy derivatives of 2-aminotetralin with [3H]clonidine and [3H]prazosin as well as with [3H]spiperone binding sites in rat cerebral cortex membrane preparations were investigated [12].
• The effects of semirigid methoxy analogs of 2-aminotetralin (2-AT) and 2-aminoindane (2-AI) were studied on superfused dog metatarsal veins to investigate postjunctional interactions produced by these agents on sympathetically innervated vascular smooth muscle [13].
• The pharmacological action of a newly synthesized piperazine derivative of 2-aminotetralin (P11) on pre- and postsynaptic alpha-adrenoceptors of isolated rat vas deferens has been investigated [14].

Associations of Tetrahydro-beta-naphthylamine with other chemical compounds

• These findings led us to synthesize a series of polyamine derivatives of 1-aminoindan and 1-aminotetralin and to determine their effects in several in vitro and in vivo models of neurotrauma [15].
• Thus, a series of 35 differently substituted 2-aminotetralin-derived substituted benzamides was synthesized and the compounds were evaluated for their ability to compete for [3H]-raclopride binding to cloned human dopamine D2A and D3 receptors, and for [3H]-8-OH-DPAT binding to rat serotonin 5-HT1A receptors in vitro [16].

Analytical, diagnostic and therapeutic context of Tetrahydro-beta-naphthylamine

• Optimisation of the enantiomeric separation of 12 2-aminotetralin analogues using Chiral AGP high-performance liquid chromatography by simultaneous factorial design [17].
• Circular dichroism curves have been measured for phthaloyl-, maleyl- and itaconyl-derivatives of a number of amines having a general formula R--CH(NH2)--R' (in which R and R' are alkyl-, aryl- or cyclohexyl-groups) and of 1,2,3,4-tetrahydro-1-naphthylamine and 1,2,3,4-tetrahydro-2-naphthylamine [18].

References