Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: EC:4.6.1.1 (adenylate cyclase)
 19,190 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The aim of the present work was to explain the mechanism of the stimulating effect of adrenaline (A) on acetylcholine (ACh) synthesis. This action is exerted most probably through the beta- adrenergic receptors, since propranolol and oxprenolol inhibit the stimulating effect of adrenaline on acetylcholine synthesis in the rat cerebral cortex in vitro. Dihydroergotamine does not show such effect. Practolol and phentolamine decrease the spontaneous synthesis of ACh in concentration several times lower than that inhibiting the ACh synthesis stimulated by adrenaline. It is suggested that adrenaline-induced stimulation of ACh synthesis in the rat cerebral cortex is not due to cyclic AMP, because noradrenaline (NA) does not increase ACh synthesis either in vivo or in vitro, although it activates the adenyl cyclase. NA on the other hand activates ACh synthesis in the calcium-free medium, which inhibits activating effect of NA on adenyl cyclase. Moreover it was found that cyclic AMP depresses ACh synthesis in the rat cerebral cortex in vitro.
Acta Physiol Pol
PMID:The effect of adrenaline on acetylcholine synthesis after blockade of alpha- and beta-adrenergic receptors in vitro. 2 84

The influence of haloperidol and propranolol on aggressiveness, motility exploration and general behavior, and the activity or level of adenylate cyclase, cyclic AMP, and protein kinase in the brain of mice treated with LSD was tested. Haloperidol evidently, and propranolol slightly less, inhibited the behavioral and biochemical changes induced by LSD. It is suggested that psychotomimetic effects of LSD depend on complex action of this compound on aminergic receptors in the central nervous system, and the antipsychotic effectiveness of haloperidol and propranolol is related to interaction of these drugs and LSD with the receptors for monoamines participating in the central neuromediation.
Pol J Pharmacol Pharm
PMID:The influence of haloperidol and propranolol on behavior and biochemical changes in the brain of mice treated with LSD. 19 69

The activity of adenylate cyclase (EC 4.6.1.1) in the mouse mammary gland increases during late pregnancy and reaches its maximum value at one day pre partum. In the mouse mammary gland explant culture the adenylate cyclase activity is stimulated by a cooperative action of insulin, prolactin and hydrocortisone. The effect of these hormones can be demonstrated in intact cells, but not in a cell-free system. In the explants, RNA synthesis is stimulated by dibutyryl cyclic AMP, insulin and prolactin. The effects of both protein hormones and cyclic AMP are additive. The results obtained suggest that insulin and prolactin in cooperation with hydrocortisone are involved in the regulation of RNA synthesis in the mammary gland by activation of the adenylate cyclase system, independently of their effect on this process not mediated by cyclic AMP.
Acta Biochim Pol 1978
PMID:Hormonal activation of adenylate cyclase and its role in cyclic AMP mediated regulation of RNA synthesis in the mouse mammary gland. 20 33

Exogenous sialic acid at 3 mM and higher concentrations inhibits the basal adenylate cyclase activity and the activity stimulated by thyrotropin (TSH) and fluoride in the human thyroid membrane fraction; 30 mM-sialic acid acts as an inhibitor of TSH binding. The decrease of these activities at high sialic acid concentrations might be ascribed to changes in membrane conformation caused by acidic character of this sugar.
Acta Biochim Pol 1978
PMID:The effect of sialic acid on adenylate cyclase activity and thyrotropin-receptor binding in human thyroid membranes. 22 Aug 31

Levels of c-AMP in heart and kidney of genetically hypertensive rats (SHR) were significantly lower than in normotensive Wistar animals. PGE2, 10 microgram/kg ip markedly increased the concentration of c-AMP in heart and kidney of SHR animals, but was without effect on this cyclic nucleotide content in normotensive controls. PGF2, in doses up to 100 microgram/kg, did not influence the concentrations of c-AMP in heart and kidney of SHR animals. Alterations in adenylate cyclase--c-AMP system in genetic hypertension are discussed.
Pol J Pharmacol Pharm
PMID:Decreased myocardial and renal content of 3',5'-AMP in genetically hypertensive rats: effects of PGE2 and PGF2 alpha. 23 31

The in vivo effects of GABA-ergic drugs on the activity of serotonin N-acetyltransferase (NAT) and hydroxyindole-O-methyltransferase (HIOMT), two enzymes involved in melatonin biosynthesis, were investigated in light-exposed chicken retina. The ip administration of muscimol and baclofen (direct agonists of GABA-A and GABA-B receptors, respectively), aminooxyacetic acid (an inhibitor of GABA transaminase), and nipecotic acid (an inhibitor of GABA reuptake), significantly increased the retinal NAT activity by 50-100%. Similar rises in NAT activity were observed following intraocular treatment of ether-anesthetized chickens with muscimol, baclofen and GABA. In contrast to NAT, there was no effect of the tested drugs on the retinal HIOMT activity. Aminophylline (a phosphodiesterase inhibitor) markedly elevated the retinal NAT activity, and a combined treatment with the GABA-ergic drugs and aminophylline resulted in additive effects. The actions of both muscimol and baclofen were antagonized by picrotoxin and bicuculline (two GABA-A receptor blockers), whereas the effect of baclofen was not changed by a selective GABA-B receptor blocker, CGP 35,348. Melatonin given ip significantly raised NAT activity, and its combination with muscimol further stimulated the enzyme. Picrotoxin and bicuculline given to chickens during the dark phase of 12 h light--12 h dark illumination cycle significantly suppressed the nocturnal NAT activity in retina. Neither GABA nor muscimol and baclofen significantly affected basal and forskolin (1 microM)-stimulated adenylate cyclase activity in vitro in light-exposed chicken retina. It is concluded that a GABA signal (acting through type A of GABA receptors) plays an important role in a complex mechanism regulating the rhythmic melatonin biosynthesis in vertebrate retina.
Pol J Pharmacol Pharm
PMID:The role of GABA-ergic signal in the regulation of melatonin biosynthesis in vertebrate retina. 130 60

The purpose of the study was determination of the perfusion pressure as an expression of the resistance of placental vascular bed after administration of various doses of Salbupart. In a series of 29 experiments with extracorporeal perfusion of the fetal part of the placental from spontaneous labours after physiological pregnancy it was observed that the medicament given in one dose reduced the vascular resistance in the afterbirth. A beneficial spasmolytic effect of Salbupart may be expected in certain cases of pathological pregnancy associated with increased resting tonus of the placental vessels. The pharmacological management for stimulation of placental adenyl cyclase may be treated as supplementation of deficient endogenous catecholamines enhancing the adaptation mechanisms of the fetus and placenta.
Mater Med Pol
PMID:The effect of Salbupart on the value of placental perfusion pressure in extracorporeal experiment. 130 67

In the experimental model of clinical death in rats (Korpachev et al. 1982) cyclic AMP concentrations were evaluated in the brain and plasma at the end of 5-min clinical death, and 5, 15, 30, 60 and 120 min after resuscitation. The cAMP 125I assay system has been used. At the end of clinical death the cAMP level decreased in the brain with normalization 15 min after resuscitation; the second decrease of the cAMP level was observed 30 min post resuscitation with normalization in later periods. In the plasma cAMP concentration did not change at the end of clinical death, followed by a significant increase 5 min after resuscitation. Later the level of plasma cAMP decreased being still above the control value after 2 hours. The possible role of endogenous catecholamines stimulation on adenylate cyclase activity is discussed.
Neuropatol Pol 1991
PMID:Changes of concentration of cyclic AMP in rat brain and plasma in the clinical death model. 166 42

The effect of various dopaminergic agents and related drugs on the activity of the heat-stable inhibitor of cyclic AMP (cAMP)-dependent protein kinase (Walsh inhibitor) and on cAMP accumulation was studied in retinas of light- and dark-adapted rabbits. Both in dark- and light-adapted rabbits low doses of apomorphine increased the retinal Walsh inhibitor activity; high doses of the drug decreased the Walsh inhibitor activity in dark-adapted rabbits, but were without effect in light-adapted animals. S-Sulpiride antagonized the effect of low doses of apomorphine on the Walsh inhibitor activity, and, in contrast to haloperidol (which was effective), did not affect the action of a high apomorphine dose. Selective agonists of dopamine (DA) D2-receptor, quinpirole and bromocriptine, increased the retinal Walsh inhibitor activity in both light- and dark-adapted animals, a selective D1-agonist, SKF 38393, decreased the inhibitor activity in dark- and did not significantly modify it in light-adapted animals. In in vitro experiments, carried out in the presence of theophylline, DA and apomorphine increased cAMP accumulation in pieces of the rabbit retina through activation of D1-receptors. The action of DA, apomorphine, and SKF 38393, was significantly stronger in retinas of dark- than of light-adapted animals. Forskolin stimulated cAMP accumulation in a concentration-dependent manner, producing at 100 microM increases of cAMP levels by approximately 5-fold. DA and SKF 38393 did not significantly modulate the action of 10 microM forskolin, whereas apomorphine slightly decreased the forskolin effect. Of the two selective D2-receptor agonists, bromocriptine slightly decreased, and quinpirole had no effect on the forskolin action. The characteristics of the specific binding of [3H]spiroperidol were essentially the same in the retinas of dark- and light-adapted rabbits. Our data suggest that in light-adapted animals the D1-receptors, or the effector mechanisms for regulation of the Walsh inhibitor activity, may be desensitized. Our results suggest also that in the rabbit retina there are probably no D2-receptors coupled negatively to adenylate cyclase, although a pharmacologically similar class of DA receptors seems to be involved in regulation of the Walsh inhibitor activity (in a way independent on environmental lighting).
Pol J Pharmacol Pharm
PMID:Light modulates dopamine-regulated Walsh inhibitor activity and dopamine-dependent cyclic AMP accumulation in the rabbit retina. 198 30

A series of lumilysergol and lysergol derivatives were studied with a number of neurochemical methods. The compounds investigated showed heterogenous profiles on receptor binding tests. They were mostly active on D-2 receptors, but some alpha-1, alpha-2 and 5-HT-2 affinity could also be demonstrated. None of the drugs showed remarkable D-1 activities tested on basal and DA-stimulated adenylate cyclase (AC) enzyme in vitro. On the basis of the effects of the drugs on the mouse whole brain monoamine neurotransmitter and metabolite levels and neurotransmitter biosynthesis rates along with the receptor binding data we conclude that their actions are mainly related to the central dopaminergic system(s). The 2-halo-lumilysergole derivatives were less potent than the 2-halo-lysergoles with respect to their dopaminergic actions. We found the substitution at position 8 to be substantial to achieve agonistic or antagonistic properties, and, interestingly, 2,8-dihalo-lysergoles have proven to be DA agonists. The neurochemical findings are in good agreement with the behavioral results presented in the accompanying paper. We confirmed the behavioral data in that there are two subgroups among 2-halo-lysergoles possessing antipsychotic activity with opposite effects on DA receptors.
Pol J Pharmacol Pharm
PMID:Substituted ergolines: potential antipsychotics with unique profile. II. Neurochemical characterization. 247 35


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