Contralateral turning was produced by unilateral injection of carbachol (0.5, 2.5, 5 micrograms) into the nucleus accumbens, but not into the dorsal or ventral striatum. This behaviour was inhibited by muscarinic M1 acetylcholine receptor blockade in the nucleus accumbens, and less effectively by blockade of muscarinic M2 and nicotinic acetylcholine receptors. Unilateral injection of a mixture ...

A small series of tetrahydroindazoles was prepared, starting from 2-acetylcyclohexanone and different hydrazines using reflux and a focused microwave reactor. Microwave irradiation (MW) favored the formation of the desired products with improved yields and shortened reaction times. This is a simple and green method for the synthesis of substituted tetrahydroindazole derivatives. The in vitro an...

Behavioral studies of chronic CB(1) receptor activation may provide a pharmacological approach to understanding efficacy-related differences among CB(1) ligands as well as mechanistic commonalities between cannabinoid and noncannabinoid drugs. In the present studies, the effects of CB(1) agonists [(6aR,10aR)-3-(1-adamantyl)-6,6,9-trimethyl-6a,7,10,10a-tetrahydrobenzo[c]chromen-1-ol (AM411), 9β-...

Conscious squirrel monkeys were treated i.v. with cocaine and various dopamine agonist drugs. Cocaine produced a dose-dependent increase in blood pressure, heart rate, and the rate-pressure product (RPP). The dopamine D1 receptor agonist (+/-)-6-chloro-3-allyl-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine hydrobromide (SKF 82958) produced effects comparable to cocaine. The D1 agonist (+/-)-6-chl...

R-(+)-7-chloro-8-hydroxy-3-methyl-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine hydrochloride (SCH23390) is a widely used, highly selective antagonist of D1 dopamine receptors. While investigating the crosstalk between D1 and D3 dopamine receptor signaling pathways, we discovered that in addition to being a D1 receptor antagonist, SCH23390 and related compounds inhibit G protein-coupled inwardly...

SKF83959 (3-methyl-6-chloro-7,8-hydroxy-1-[3-methylphenyl]-2,3,4,5-tetrahydro-1H-3-benzazepine), an atypical dopamine receptor-1 (D(1) receptor) agonist, has shown many D(1) receptor-independent effects, such as neuroprotection, blockade of Na(+) channel, and promotion of spontaneous glutamate release, which resemble the effects of the sigma-1 receptor activation. In the present work, we explor...

Chemical investigation of the sponge Callyspongia sp. from the South China Sea afforded one new diketopiperazine, cyclo-(R-Pro-6-hydroxyl-S-Ile) (1), along with six known diketopiperazines: staphyloamide A (2), cyclo(S-Pro-S-Phe) (3), cyclo-(R-Pro-R-Phe) (4), cyclo-(S-Pro-R-Leu) (5), cyclo-(S-Pro-R-Ala) (6), cyclo(R-Tyr-R-Phe) (7), and three known tryptophan-derived alkaloids: C 2 -α-D-mannosyl...

Synthesis and characterization of 6-(hydroxymethyl)-14, 16-dimethyl-13, 14, 16, 17-tetrahydro-6H-13, 17-epiminodibenzo [e, l] [1, 4] dioxacyclotridecin-15 (7H)-oneABSTRACTNew 6-(hydroxymethyl)-14, 16-dimethyl-13, 14, 16, 17-tetrahydro-6H-13, 17-epiminodibenzo [e, l] [1, 4] dioxacyclotridecin-15 (7H)-one (2a) was synthesized in good yield by the Petrenko–Kritchenko reaction of 2, 2'-((3-hydroxyp...

reaction of tryptamine 1 with dimethyl -3-methoxyallylidenemalonate 2 afforded n?-[4,4-bis (methoxycarbonyl)-1,3-butadienyl] tryptamine 3 which in combination with acetylchloride and pyridine in dichloromethane gave n?, n?-[acetyl]-[(4,4-dinethoxycarbonyl) 1,3butadienyl] tryptamine 4. treatment of 3 with sodium hydroxide afforded 2h[n-(3-indolyl) ethyl] 2-oxo-3-methoxycarbonyl-1-pyridine 5. cyc...