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PubMedDate not supplied

Synthesis, in vitro and in vivo 5-HT1A/5-HT2A serotonin receptor activity of new hybrid 1,2,3,4-tetrahydro-gamma-carbolines with 1-(2-methoxyphenyl)piperazine moiety.

A series of 15 new 2-H- and 2-substituted 5-[omega-[4-(2-methoxyphenyl)-piperazinyl]-alkyl]-1,2,3,4-tetrahydro-gamma-carboline derivatives were prepared, and their affinity for 5-HT1A and 5-HT2A serotonin receptors was determined. Most of those hybrid compounds were found to bind with high affinity to 5-HT1A sites (Ki < 50 nM; 2d, 3a, 3b, 3d, 3e, 4b, 4d, 4e) and moreover two of them (4d, 4e) were mixed 5-HT1A/5-HT2A ligands. The results of a lower lip retraction test in rats indicated that the 2-acetyl derivative with a dimethylene spacer (2d) had features of a postsynaptic 5-HT1A receptor agonist, whereas its analogues with longer chains (3d and 4d) behaved like antagonists. Both 5-HT2A receptor ligands (4d, 4e) at high doses inhibited the (+/-)-DOI-induced head twitches in mice and were classified as weak antagonists of those receptors.

Animals↗
PubMedDate not supplied

Anticonvulsant properties of N-(4-methylpiperazin-1-yl)- and N-[3-(4-methyl-piperazin-1-yl)propyl] derivatives of 3-aryl- and 3-spirocycloalkyl-pyrrolidine-2,5-dione.

Two series of N-(4-methylpiperazin-1-yl)- and N-[3-(4-methylpiperazin-1-yl)-propyl]-3-aryl- and 3-spirocycloalkyl-pyrrolidine-2,5-dione derivatives were synthesized and tested for anticonvulsant activity in the maximum electroshock (MES) seizure and pentetrazole (sc PTZ) seizure threshold tests. Compounds with an aromatic ring at position-3 of pyrrolidine-2,5-dione exhibited anticonvulsant activity in the MES test. For that series of compounds, ED50 values were determined. The most potent in the series were derivatives and with a chlorine atom at position-3 or 4 of the aromatic ring. Those compounds exhibited strong anticonvulsant activity, and their ED50 values ranged from 29 to 48 mg/kg. Introduction of the spirocycloalkyl ring into the position-3 of pyrrolidine-2,5-dione made those compounds inactive.

Animals↗
PubMedDate not supplied

IP66 (1[2-ethoxy-2-(3'-pyridyl)ethyl]-4-(2'-methoxy-phenyl)piperazine) enhances beta-adrenoceptor-induced vasodilatation in rat mesenteric vascular bed.

The effect of the antihypertensive drug IP66 on dopamine-induced vasodilatation has been investigated in isolated perfused rat mesenteric bed. Experiments were carried out in phenoxybenzamine-pretreated preparations to avoid the involvement of alpha-adrenoceptors. Dopamine (1-100 microM) elicited a concentration-dependent relaxation of high-K(+)-induced vasoconstriction, which was resistant to propranolol (3 microM), but antagonized by the DA1-receptor antagonist SCH 23390 (0.1 microM). However, the dopamine-vasodilating component resistant to SCH 23390 (0.1 microM) could be abolished by simultaneous administration of propranolol. Thus, dopamine-induced vasodilatation is mainly ascribable to stimulation of DA1-receptors, although an action on beta 2-adrenoceptors might contribute as well. In presence of IP66 (10 nM), dopamine-induced vasodilatation was significantly enhanced. This amplifying activity was not observed with prazosin and it was blocked by propranolol (3 microM) but unaffected by SCH 23390 (0.1 microM) or by chemical sympathectomy. Furthermore, IP66 (10 nM) also increased, in a significant manner, the amplitude of vasodilatation elicited by the beta 2-adrenoceptor agonist terbutaline, both in rat mesenteric bed and in rat aortic strips. In rat aortic membranes, IP66 (10 nM) enhanced the stimulatory effect of terbutaline (1 microM) on adenylate cyclase activity. In conclusion, IP66 is able to enhance the vasodilatation of rat mesenteric vasculature induced by dopamine or terbutaline. It is proposed that this action might be consequent to an increase in efficiency of the coupling between beta 2-adrenoceptors and membrane adenylate cyclase.

Adenylyl Cyclases↗
PubMed1975

Pharmacological properties of n1-piperonyl-n4-3,7,11-trimethyl-2,6,10-dodecatrienyl-piperazine, a new non-anticholinergic gastric antisecretory agent.

The special and general pharmacology of N1-piperonyl-N4-3,7,11-trimethyl-2,6,10-dodecatrienylpiperazine (U-27) is reported. According to the results of the animal experiments the compound turned out to be a well tolerated gastric antisecretory drug devoid of anticholinergic activity. The compound was able to prevent hypersecretion induced by pylorus ligature in rat and guinea pig. Its duration of action was remarkable and no tolerance occurred after a repeated treatment. The compound displayed also an interesting activity on several experimental ulcers.

Animals↗
PubMed1985

The effects of buspirone, BMY-13805 and 1-(2-pyrimidinyl)-piperazine on cat spinal reflexes.

Buspirone and its analog BMY-13805, clinically effective anxiolytics and their metabolite, 1-PP, were tested on cat spinal reflexes. In the spinal preparation, the monosynaptic reflex and the dorsal root potential were not changed by buspirone, BMY-13805 or 1-PP. Significant changes in the dorsal root potential and monosynaptic reflex were seen after buspirone administration in the intact neuraxis preparation. Generally, these changes had a bimodal pattern, a significant change within 1 hr after buspirone administration, then a period of remittance, followed by a second significant change 3 or more hr later. They included increases in the dorsal root potential and the following changes in the conditioned monosynaptic reflex: an increase in excitatory postsynaptic potential, an increase in postsynaptic inhibition, and decreases in presynaptic inhibition. These data indicate that buspirone does not affect these reflexes directly, but alters supraspinal mechanisms that regulate spinal reflexes.

Animals↗