- Virtual screening, molecular dynamics and structure-activity relationship studies to identify potent approved drugs for Covid-19 treatment. [Journal Article]
- Computer-aided drug screening by molecular docking, molecular dynamics (MD) and structural-activity relationship (SAR) can offer an efficient approach to identify promising drug repurposing candidates for COVID-19 treatment. In this study, computational screening is performed by molecular docking of 1615 Food and Drug Administration (FDA) approved drugs against the main protease (Mpro) of SARS-Co…
- PMC Free PDF
- Bromocriptine tablet of self-microemulsifying system adsorbed onto porous carrier to stimulate lipoproteins secretion for brain cellular uptake. [Journal Article]Colloids Surf B Biointerfaces. 2015 Jul 01; 131:162-9.CS
- Both low solubility and high hepatic metabolism cause low oral bioavailability of bromocriptine mesylate (BM) leading to very low drug amount in brain. Self-microemulsion (SME) tablets were developed to improve solubility, stimulate lipoprotein synthesis to promote lymphatic transport, avoid hepatic metabolism and target drug to brain. SME liquid containing castor oil, Tween(®) 80 and Cremophor(®…
- Publisher Full Text (DOI)
- Role of subunit interactions in P450 oligomers in the loss of homotropic cooperativity in the cytochrome P450 3A4 mutant L211F/D214E/F304W. [Journal Article]
- The contribution of conformational heterogeneity to cooperativity in cytochrome P450 3A4 was investigated using the mutant L211F/D214E/F304W. Initial spectral studies revealed a loss of cooperativity of the 1-pyrenebutanol (1-PB) induced spin shift (S(50)=5.4 microM, n=1.0) but retained cooperativity of alpha-naphthoflavone binding. Continuous variation (Job's titration) experiments showed the ex…
- Publisher Full TextPMC Free Full TextPMC Free PDF
- Dopamine and nitric oxide interaction on the modulation of prepulse inhibition of the acoustic startle response in the Wistar rat. [Journal Article]
- CONCLUSIONS: Our findings show that L-NOARG interacted with Amph, an indirect DA agonist, but not with the direct DA agonists on PPI, suggesting that NO is involved on the dopaminergic modulation of sensorimotor gating, probably by a presynaptic mechanism.
- The pivotal role of iron in NF-kappa B activation and nigrostriatal dopaminergic neurodegeneration. Prospects for neuroprotection in Parkinson's disease with iron chelators. [Journal Article]
- R-Apomorphine (APO) the catechol-derived dopamine D1-D2 receptor agonist has been shown to be highly potent iron chelator and radical scavenger and inhibitor of membrane lipid peroxidation in vitro, in vivo and in cell culture employing PC12 cells. Its potency has been compared to the prototype iron chelator desferrioxamine (desferal), dopamine, nifedipine and dopamine D2 receptor agonists, bromo…
- Possible sites of dopaminergic inhibition of gonadotropin release from the pituitary of a teleost fish, tilapia. [Journal Article]
- The present study is an attempt to find sites of dopaminergic inhibition along the transduction cascades culminating in gonadotropin (GtH) release in a teleost fish, tilapia. Experiments were carried out on perifused pituitary fragments and in primary culture of trypsinized pituitary cells. Salmon GnRH, chicken GnRH I and II stimulated GtH release in culture with estimated ED50 values of 15.56 pM…
- Effect of BCH 325 (Pro-D-Phe-Pro-Gly) on central dopaminergic functions. [Journal Article]Peptides. 1995; 16(4):635-40.P
- Three behavioral models were used to characterize the pharmacological action of BCH 325 on central dopaminergic transmission. The effect of acute SC treatment with BCH 325 upon dopaminergic mechanisms affecting motor activity was studied on the climbing behavior of mice. It was shown that the beta-casomorphin analogue evoked a dose-dependent increase in apomorphine (APO)-induced hypoactivity that…
- Publisher Full Text
- Ethanol acutely reduces LH and prolactin secretion: possible involvement by dopamine. [Journal Article]
- Ethanol (ETOH) administered acutely to castrate male rats caused a decline in pituitary luteinizing hormone (LH) and prolactin (PRL) secretion. This was associated with an elevation in hypothalamic and median eminence stores of dopamine (DA) that was related to the dose of alcohol given. Pituitary stalk transection (PST) resulted in a significant rise in plasma PRL levels compared to sham control…
- Publisher Full Text
- Different effects of direct and indirect dopamine receptor agonists on immobility time in reserpine-treated mice. [Journal Article]
- 1. The effects of dopamine agonists on the immobility time in mice were examined. 2. Apomorphine (APO), bupropion (BUP), bromocriptine (BRC) and quinpirole but not SKF 38393 elicited anti-immobility effect. The effect of the agonists was decreased by the D-2 antagonist sulpiride but not by the D-1 antagonist SCH 23390. 3. In animals pretreated with reserpine, the anti-immobility effects of APO an…
- Proopiomelanocortin (POMC)-derived peptides and sleep in the rat. Part 2--Aminergic regulatory processes. [Journal Article]
- Apomorphine (Apo), a D1/D2 Dopamine (DA) agonist, at high doses (500 micrograms/kg) induces a short-lasting insomnia, antagonized by a secondary injection of corticotropin-like intermediate lobe peptide (CLIP, 10 ng); these effects are also observed with hypophysectomized (hypoX) rats. The administration of the serotonin (5-HT) agonist 8-hydroxy-2-di-n-propylamino-tetralin (8-OHDPAT, 0.3 mg/kg) i…
- Bromocriptine induces climbing behaviour: possible D-1 or D-2 dopamine receptor involvement. [Journal Article]
- The ability of bromocriptine (BRC), a dopamine D-2 receptor agonist, to induce climbing behaviour was studied in mice. BRC (2-32 mg/kg IP) evoked climbing behaviour. The maximum effect was obtained with 8 mg/kg, while higher doses of BRC (16 and 32 mg/kg) were less effective. Climbing began about 2 h after injection and was most marked 5 h after bromocriptine administration. Pretreatment of anima…
- Apomorphine: clinical studies on erectile impotence and yawning. [Controlled Clinical Trial]
- 1. The erectile response to the short-acting dopamine (DA) receptor agonist, apomorphine (Apo) HCl (0.25, 0.5, 0.75 and 1.0 mg sc), and placebo was evaluated in 28 impotent patients and penile circumference monitored using a mercury strain gauge and strip chart recording. 2. A full erection (increment in penile circumference greater than 2 cm and lasting at least one minute) occurred in 17 patien…
- Acute effects of direct dopamine agonists in the mouse behavioral despair test. [Journal Article]
- All the dopamine agonists (apomorphine, dipropylamino-5,6-dihydroxytetrahydronaphtalene, piribedil, bromocriptine, CBM 36-733) tested in the 'behavioral despair' test performed in mice had a dose-dependent anti-immobility effect, with the exception of the D-1 dopamine agonist, SKF 38393. This effect occurred at doses that reduced locomotor activity and decreased colonic temperature. A profound hy…
- Enhanced stereotypic behavior by chronic treatment with bromocriptine accompanies increase of D-1 receptor binding. [Journal Article]
- Different effects of chronic treatment with bromocriptine (BRO) on D-1 and D-2 receptors in the rat were studied through behavioral observation and DA receptor binding assays. Chronic BRO led to enhancement of stereotypy to apomorphine (APO), at the same time it increased the density of D-1 receptor binding by 43% and decreased that of D-2 receptor binding by 21%. Our data suggest that BRO has di…
- Apomorphine-induced penile tumescence in impotent patients--preliminary findings. [Controlled Clinical Trial]
- Apomorphine (Apo), a short acting dopamine (DA) receptor agonist induces penile erections in normal subjects. The erectile response to one or more doses of Apo HCl (0.25, 0.5, 0.75, 1.0 mg sc) or placebo was investigated in eight impotent subjects and penile tumescence monitored using a mercury strain gauge and strip chart recording. Four patients showed a full erection with Apo and one a partial…
- Chronic treatment with bromocriptine induces behavioral supersensitivity in rats. [Journal Article]
- Chronic treatment of rotating rats with equipotent doses of the dopamine (DA) agonists apomorphine (APO), 3-(3,4-dihydroxyphenyl)-1-n-propylpyrrolidine hydrobromide (DPPP) and bromocriptine (BRO) for four weeks resulted in marked differences in rotational activity following acute administration of these agonists. Whereas chronic treatment with APO and DPPP failed to produce any significant change…
- Interactions between endogenous dopamine and dopamine agonists at release modulatory receptors: multiple effects of neuronal uptake inhibitors on transmitter release. [Journal Article]
- The authors investigated the mechanisms by which inhibitors of the neuronal uptake (NUI) of dopamine (DA) and prolonged stimulations at high rates antagonize the inhibition of acetylcholine (ACh) release from rabbit striatal slices produced by DA receptor agonists. Nomifensine (1 microM) reduced the potency and efficacy of apomorphine (APO) in inhibiting the evoked release of ACh (0.3 Hz, 39 puls…
- The effects of chronic bromocriptine treatment on behaviour and dopamine receptor binding in the rat striatum. [Journal Article]
- Agonist-induced rotation and striatal binding of [3H]spiperone ([3H]SPIP) were assessed in rats with unilateral lesions of the substantia nigra during and after a period of chronic bromocriptine administration. Agonist-induced rotation significantly increased over a three week period of daily administration of bromocriptine (10 mg/kg i.p.); control animals were tested for agonist-induced rotation…
- Differential effects on phrenic output of two dopamine agonists, apomorphine and bromocriptine. [Journal Article]
- Effects of dopamine agonists upon phrenic output were studied in decerebrate, vagotomized, paralyzed, carotid-body denervated dogs. Intravenous administration of dopamine was without effect in these dogs. Apomorphine (APO) increased phrenic minute activity while bromocriptine (BRO) decreased phrenic minute activity following intravenous injection at doses of 100 micrograms/kg for each drug. BRO-i…
- Publisher Full Text
- Dopamine analog-induced hyperglycemia in rats: involvement of the adrenal medulla and the endocrine pancreas. [Journal Article]
- The following synthetic, structural analogs of dopamine (DA) were examined for their ability to produce hyperglycemia in conscious unrestrained rats: APO (apomorphine), RDS-127 (2-di-n-propylamino-4,7-dimethoxyindane), di-n-propyldopamine, 2-di-n-propylamino-5,6-dihydroxytetralin, 2-dimethylamino-6,7-dihydroxytetralin, lergotrile, pergolide, bromocriptine and d-amphetamine. All the compounds demo…
- Publisher Full Text
- Effect of apomorphine, a dopamine receptor agonist, on penile tumescence in normal subjects. [Controlled Clinical Trial]
- Apomorphine HCl (Apo) (0.25, 0.5 or 0.75 mg sc), a dopamine (DA) receptor agonist, induced penile erections (PEs) (monitored by mercury strain gauges and continuous recording on paper strip charts) in 7 out of 9 normal subjects and placebo in 1 of these 9 (p less than 0.05). Apo-induced PEs recurred in each of the 6 subjects retested. Benztropine (2 mg iv) had no effect on Apo-induced penile tume…
- Pharmacological characteristics of dopamine receptors involved in the dual effect of dopamine agonists on yawning behaviour in rats. [Journal Article]
- Increasing doses of apomorphine (APO) induced the dose-dependent appearance of yawns in rats at doses up to 0.1 mg X kg-1 and their disappearance from 0.1 to 0.6 mg X kg-1. A similar biphasic effect on yawning was observed with increasing doses of n-propyl norapomorphine, piribedil, S 584, bromocriptine, lergotrile, lisuride, CQ 32084 and L-DOPA. APO, n-propyl norapomorphine, piribedil and CQ 320…
- Publisher Full Text
- Locomotor hypokinesia in the reserpine-treated rat: drug effects from the corpus striatum and nucleus accumbens. [Journal Article]
- A mechanographic method was used to assess the locomotor performance induced by apomorphine or other dopaminergic drugs in reserpine-treated rats. Reserpine was found to induce locomotor hypokinesia. The hypokinesia was dose-dependently reversed by apomorphine (APO), bromocriptine and pergolide. Locomotion was induced by microinjection of APO into the nucleus accumbens. No locomotor effect was fo…
- Publisher Full Text
- Dopaminergic and serotonergic mediation of the discriminable effects of ergot alkaloids. [Journal Article]
- The involvement of dopamine (DA) and serotonin (5-HT) neuronal systems in the discriminative stimulus effects of various ergot derivatives was assessed by administering four ergots to 36 rats which had been trained to discriminate either apomorphine (APO) or d-lysergic acid diethylamide (LSD) from saline. Lergotrile, lisuride and LSD substituted for APO (0.25 mg/kg) while bromocriptine and ergono…
- Publisher Full Text
- Resumption of prolactin secretion after dopaminergic inhibition: differential effects of dopamine and its agonists. [Journal Article]
- The recovery of prolactin (PRL) secretion following dopaminergic inhibition was studied in vitro using pituitary monolayer cultures. PRL secretion over 4 h was inhibited comparably by 10(-6) M dopamine (DA), 10(-7) M apomorphine (APO), and 10(-10) M bromocriptine (45%, 42%, 51%, respectively) with reciprocal increases in intracellular hormone content. After drug removal, the PRL secretion rate in…
- Publisher Full Text
- Growth hormone hyperresponsiveness to dopaminergic stimulation in Huntington's chorea. [Journal Article]
- The effect of 3 dopamine (DA) mimetic drugs, i.e. bromocriptine (Bro), apomorphine (Apo) and L-3,4-Dihydroxpenylalanine (L-dopa), was evaluated on plasma growth hormone (GH) levels in 18 patients with Huntington's chorea (HC). 27 Nonobese hospitalized patients were used as controls. Mean baseline GH levels were not altered in patients with HC. Oral administration of Bro (2.5 mg po) or L-dopa (500…
- Publisher Full Text