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A METHOD FOR EVALUATING THE EFFECTS OF LIGANDS UPON G(S) PROTEIN-COUPLED RECEPTORS USING A RECOMBINANT MELANOPHORE-BASED BIOASSAY

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ANALYTICAL BIOCHEMISTRY 1992年第2期206卷 315-322页

作者： POTENZA, MN GRAMINSKI, GF LERNER, MR YALE UNIV SCH MEDDEPT INTERNAL MEDNEW HAVENCT 06510 YALE UNIV SCH MEDDEPT CELL BIOLNEW HAVENCT 06510 YALE UNIV SCH MEDHOWARD HUGHES MED INSTNEW HAVENCT 06510 YALE UNIV SCH MEDBOYER CTR MOLEC MEDDEPT PHARMACOLNEW HAVENCT 06510

As an increasing number of medically important receptors that couple to stimulatory guanine nucleotide (Gs) proteins are isolated and cloned, there is an equally escalating need for methods to rapidly and reproducibly evaluate potential ligands for their properties as agonists or antagonists. Recently, a bioassay that can quickly and accurately determine the effects of numerous chemicals on a beta 1-like adrenergic receptor (AR) endogenous to melanophores derived from Xenopus laevis was developed. Here, the general utility of the melanophore-based pigment dispersion assay is demonstrated by employing it to evaluate the effects of drugs on a human beta 2 AR. Melanophores were both transiently and stably transfected with a plasmid encoding a beta 2 AR. Stimulation of recombinant cells expressing the beta 2 AR, but not wild-type cells, with beta 2-selective agonists induced pigment dispersion and concomitant elevations in intracellular cAMP. Using a microtiter plate reader, it was straightforward to construct reproducible dose-response curves and rapidly determine rank-order potency and EC50 and IC50 values for agonists and antagonists, respectively. The demonstration of functional expression of a human beta 2 AR in the melanophore-based bioassay suggests that the system may be used for the rapid pharmacological characterization of ligands upon any specific Gs-linked receptor for which a cDNA clone is available.

关键词：生物学鉴定法/方法细胞培养的环AMP/代谢 GTP结合蛋白质类/代谢动力学配体黑素细胞刺激激素类/药理学黑素细胞载色体/细胞学黑素细胞载色体/代谢奥西那林/药理学质粒受体肾上腺素能β/药物作用受体肾上腺素能β/代谢受体肾上腺素能β/辐射效应重组蛋白质类/药物作用重组蛋白质类/代谢转染爪蟾光滑动物

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TRANSFORMATION OF AMPHIBIAN IRIDOPHORES INTO MELANOPHORES IN CLONAL CULTURE

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DEVELOPMENTAL BIOLOGY 1976年第2期53卷 297-302页

作者： IDE, H HAMA, T NAGOYA UNIV FAC SCI INST BIOL NAGOYA 464 JAPAN

Iridophores isolated from bullfrog [Rana catesbeiana] tadpoles were successfully cloned. In primary culture the iridophores showed contraction of cell bodies by the addition of alkali-treated ACTH. The disappearance of reflecting platelets occurred in proliferating iridophores and many small black melanin granules were synthesized in the cells. The chromatophores now showed melanin dispersion by the addition of the above hormone. Iridophores may transform into melanophores in vitro.

关键词：细胞分化色素细胞/生理学幼虫/生理学黑素细胞刺激激素类/药理学黑素细胞载色体/生理学黑素细胞载色体/超微结构显微镜检查电子牛蛙皮肤动物

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α-MSH peptides inhibit production of nitric oxide and tumor necrosis factor-α by microglial cells activated with β-amyloid and interferon γ

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BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS 1999年第1期263卷 251-256页

作者： Galimberti, D Baron, P Meda, L Prat, E Scarpini, E Delgado, R Catania, A Lipton, JM Scarlato, G Univ Milan IRCCS Osped Maggiore Policlin Inst NeurolDino Ferrari Ctr I-20122 Milan Italy Univ Milan IRCCS Osped Maggiore Policlin Div Internal Med 3 I-20122 Milan Italy Univ Texas SW Med Ctr Dept Physiol Dallas TX 75235 USA Univ Texas SW Med Ctr Dept Anesthesiol Dallas TX 75235 USA

alpha-Melanocyte stimulating hormone (alpha-MSH) is an ancient tridecapeptide with potent inhibitory activity in all major forms of inflammation. The anti-inflammatory message sequence of alpha-MSH resides in the COOH-terminal tripeptide alpha-MSH[11-13]. We tested the influence of alpha-MSH[1-13] and of alpha-MSH[11-13] in a cultured murine microglia cell line known to produce nitric oxide (NO2-) and tumor necrosis factor (TNF alpha) when stimulated with beta-amyloid protein (A beta). Melanocortin peptides significantly inhibited release of both NO2- and TNF alpha into cell-free supernatants from microglia stimulated with A beta[1-42] or A beta[25-35] peptides and interferon gamma (IFN gamma). Northern blot analysis demonstrated that alpha-MSH[1-13] and alpha-MSH[11-13] inhibited accumulation of inducible nitric oxide synthase (iNOS) and TNF alpha mRNA was triggered by A beta stimulation. A beta/microglial interaction is believed to promote the progression of inflammatory and neurodegenerative changes in senile plaques in Alzheimer's disease. Our data indicate that alpha-MSH peptides might be used to modulate the local response of the brain to A beta deposition in this neurodegenerative disease. (C) 1999 Academic Press.

关键词：细胞系炎症介导素类/代谢黑素细胞刺激激素类/药理学小神经胶质细胞/药物作用小神经胶质细胞/代谢一氧化氮/生物合成一氧化氮合酶/遗传学一氧化氮合酶/代谢一氧化氮合酶Ⅱ型肽碎片/药理学 RNA 信使/遗传学 RNA 信使/代谢重组蛋白质类肿瘤坏死因子α/生物合成肿瘤坏死因子α/遗传学 α促黑素/药理学动物小鼠

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INFLUENCE OF ACUTE ADMINISTRATION OF HUMAN GROWTH-HORMONE AND ALPHA-MSH ON PLASMA CONCENTRATIONS OF ALDOSTERONE, CORTISOL, CORTICOSTERONE AND GROWTH-HORMONE IN MAN

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ACTA ENDOCRINOLOGICA 1975年第1期79卷 16-24页

作者： BIRKHAUSER, M GAILLARD, R RIONDEL, AM ZAHND, GR UNIV GENEVA DEPT MEDDIV ENDOCRINOLLAB CLIN PHYSIOPATHOL GENEVA SWITZERLAND UNIV GENEVA FDN MED RES GENEVA SWITZERLAND

The effect of acute administration of human growth hormone (HGH) and of alpha-melanocyte stimulating hormone (alpha-MSH) on plasma aldosterone, cortisol, corticosterone and growth hormone has been studied in normal man and in patients with panhypopituitarism. There is no acute effect of exogenous HGH on plasma levels of aldosterone, cortisol and corticosterone in normal man and in patients with panhypopituitarism. The plasma level of immunoreactive HGH measured during acute HGH infusion in man does not seem to be proportional to the doses administered in our study. Alpha-MSH raises the concentration of plasma HGH, but this stimulation is not dose-dependent. Aldosterone, cortisol and corticosterone concentrations are not influenced by the elevation of HGH mediated by alpha-MSH in normal man. Although in some patients with panhypopituitarism an elevation of plasma aldosterone concentration following alpha-MSH infusion is observed, it is unlikely that MSH is directly involved in the acute regulation of aldosterone secretion in healthy subjects.

关键词：醛固酮/血液生长激素/投药和剂量生长激素/血液生长激素/药理学氢化可的松/血液垂体功能减退症/血液注射静脉内黑素细胞刺激激素类/投药和剂量黑素细胞刺激激素类/药理学刺激化学性时间因素女(雌)性人类男(雄)性

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Mahogany (1377-1428) enters brain by a saturable transport system

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JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS 2000年第2期294卷 633-636页

作者： Kastin, AJ Akerstrom, V Vet Affairs Med Ctr New Orleans LA 70112 USA Tulane Univ Sch Med New Orleans LA 70112 USA

The mouse mahogany gene encodes a protein that is involved in the suppression of diet-induced obesity. We studied the ability of its widely conserved C-terminal fragment to cross the blood-brain barrier (BBB) in mice. Multiple-time regression analysis showed that the entry rate (K-i) of I-125-mahogany (1377-1428) from blood-to-brain was 5.5 X 10(-4) ml/***. After coinjection of unlabeled mahogany (1377-1428), the K-i was significantly decreased, showing the self-inhibition characteristic of a saturable transport mechanism. The excess mahogany (1377-1428) did not change the influx rate of Tc-99m-albumin, the vascular control, indicating a lack of disruption of the BBB. Statistically significant cross-inhibition was not seen with agouti-related protein (83-132), melanin-concentrating hormone, epidermal growth factor, leptin, a melanocortin-4 receptor antagonist, or alpha-melanocyte-stimulating hormone. HPLC showed that most of the injected I-125-mahogany (1377-1428) reached the brain intact, and capillary depletion with washout showed that most of it reached the parenchyma. There was no brain-to-blood efflux system for mahogany (1377-1428) but rather retention after i.c.v. administration, and the octanol/buffer partition coefficient showed low lipophilicity. Thus, the results show that the C-terminal peptide product encoded by the mahogany gene crosses the BBB by a transport mechanism that is saturable. The ability of this system to be regulated indicates the therapeutic potential of mahogany (1377-1428) in the treatment of obesity.

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IODINATION ASSOCIATED INACTIVATION OF BETA-MELANOCYTE STIMULATING HORMONE

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BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS 1979年第1期88卷 266-273页

作者： HEWARD, CB YANG, YCS SAWYER, TK BREGMAN, MD FULLER, BB HRUBY, VJ HADLEY, ME UNIV ARIZONA DEPT GEN BIOL TUCSON AZ 85721 USA UNIV ARIZONA DEPT CHEM TUCSON AZ 85721 USA

Contrary to other reports, iodinated .beta.-melanocyte stimulating hormone (.beta.-MSH) is without biological activity as measured by frog skin bioassay, melanoma (mouse S-91) adenylate cyclase assay, or melanoma tyrosinase assay. Inactivation results in part from oxidation of the Met residue by the chloramine T and sodium metabisulfite used in the iodination reaction. Replacement of the Met of .beta.-MSH with norleucine by solid phase synthesis results in an analog which is more resistant, but not completely resistant, to inactivation. To obtain a biologically active radioligand for radioreceptor studies, further tailoring of the hormone and/or modification of the iodination procedure will be needed.

关键词：无尾目生物学鉴定法细胞系碘化物黑素细胞刺激激素类/类似物和衍生物黑素细胞刺激激素类/药理学黑色素瘤/代谢一元酚单氧酶/代谢肿瘤实验性/代谢豹纹蛙皮肤/药物作用构效关系动物小鼠

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EFFECTS OF ALPHA-MSH ON MOTIVATION, VIGILANCE AND BRAIN RESPIRATION

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PHARMACOLOGY BIOCHEMISTRY AND BEHAVIOR 1976年第Suppl 1期5卷 59-64页

作者： PANKSEPP, J REILLY, P BISHOP, P MEEKER, RB VILBERG, TR KASTIN, AJ BOWLING GREEN STATE UNIV DEPT PSYCHOLBOWLING GREENOH 43403 VET ADM HOSP MED SERVENDOCRINOL SECTNEW ORLEANSLA 70146 TULANE UNIV SCH MEDDEPT MEDNEW ORLEANSLA 70122

In a series of experiments designed to assess the effects of alpha-MSH on various motivational processes, it was observed that the hormone can slightly decrease food intake and increase water consumption during the first hr after administration in rats. alpha-MSH also modified avoidance behavior in 1- and 3-day-old chicks, but there were no reliable effects on activity, distress vocalizations and the tonic immobility response. alpha-MSH appeared to modulate the sleep-waking activity of rats, and the most prominent effect was an increase of slow wave sleep during the 2-3 rd hr after treatment. A possible second effect was a homogenization of sleep patterns--with poor sleepers exhibiting increases of activated sleep and good sleepers a reduction. Measurement of in vitro brain oxygen consumption indicated that mice treated with alpha-MSH exhibit an 18% reduction in respiration of the brain stem section which includes the locus coeruleus, but did not reliably change respiration in forebrain cortices. alpha-MSH also produced a modest 14% increase of plasma glucose. These results are discussed in terms of possible modulation by alpha-MSH of activity in central autonomic cell groups such as the locus coeruleus.

关键词：动物新生回避学习/药物作用行为动物/药物作用脑/药物作用脑干/药物作用脑干/代谢大脑皮质/药物作用大脑皮质/代谢鸡饮行为/药物作用脑电描记术摄食行为/药物作用黑素细胞刺激激素类/药理学动机器官特异性氧耗量/药物作用睡眠/药物作用睡眠期/药物作用觉醒状态/药物作用动物男(雄)性小鼠大鼠

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HORMONES AND REGIONAL BRAIN BLOOD-FLOW

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PHARMACOLOGY BIOCHEMISTRY AND BEHAVIOR 1976年第Suppl 1期5卷 165-169页

作者： GOLDMAN, H SKELLEY, EB SANDMAN, CA KASTIN, AJ MURPHY, S WAYNE STATE UNIV DEPT PHARMACOLDETROITMI 48201 OHIO STATE UNIV DEPT PHARMACOLCOLUMBUSOH 43210 OHIO STATE UNIV DEPT PSYCHOLCOLUMBUSOH 43210 VET ADM HOSP ENDOCRINOL SECTNEW ORLEANSLA 70146 TULANE UNIV SCH MEDDEPT MEDNEW ORLEANSLA 70146

Acute effects of the hormones, estradiol-17beta and alphaMSH, and of neonatal pretreatment with alphaMSH on the flow of blood to regions of the brains of conscious adult rats have been determined with an indicator distribution technique. As previously reported, flows were reduced in most areas within 10 min after intravenous administration of alphaMSH; only the occipital cortex was spared. Though these effects were transitroy for most areas, perfusion of pons and medulla, cerebellum, hippocampus and parietal cortex was still low by 20 min. However, pretreatment with alphaMSH during infancy led to persistent behavioral changes which were not accompanied by flow differences. Assuming that flow changes reflect functional changes, the rapid responses to alphaMSH suggest an explanation for the effects of this hormone on visual learning and on the determination of subsequent learning behavior. By contrast, estradiol, within 10 min after injection, increased flow to most regions of the brain, especially the frontal cortex, hippocampus, basal ganglia and cerebellum; females were more affected than males. Flow changes were greater than those elicited by more obvious behavior-modifying drugs. Compared to alphaMSH, the flow data for estradiol suggest a physiologic basis for a behavioral effect which is likely to be different yet, perhaps, equally profound.

关键词：动物新生行为动物/药物作用脑血管循环/药物作用雌二醇/药理学动情期黑素细胞刺激激素类/药理学性别因素动物女(雌)性男(雄)性妊娠大鼠

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ENKEPHALIN AND A POTENT ANALOG FACILITATE MAZE PERFORMANCE AFTER INTRAPERITONEAL ADMINISTRATION IN RATS

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PHARMACOLOGY BIOCHEMISTRY AND BEHAVIOR 1976年第6期5卷 691-695页

作者： KASTIN, AJ SCOLLAN, EL KING, MG SCHALLY, AV COY, DH VET ADM HOSP MED SERV ENDOCRINOL SECT NEW ORLEANS LA 70146 USA VET ADM HOSP ENDOCRINE & POLYPEPTIDE LABS NEW ORLEANS LA 70146 USA TULANE UNIV SCH MED DEPT MED NEW ORLEANS LA 70146 USA

Met-enkephalin and its analog [D-Ala2]-Met-enkephalin-NH2 were administered i.p. at a dose of 80 .mu.g/kg body weight to hungry rats which were tested over 3 days for their ability to run a complex, 12 choice Warden maze for a reward of food. Animals receiving either peptide negotiated the maze significantly (P < 0.01) faster (74.1 and 73.5 vs. 128.8 s) and made significantly (P < 0.01) fewer errors (5.5 and 5.4 vs. 9.1) than animals receiving the diluent vehicle. These findings did not seem to be explained by differences in appetite, thirst, olfaction or general activity. Rats injected in a preliminary study with an analog, [D-Phe4]-Met-enkephalin, which has essentially no opiate activity appeared to run the maze as fast as rats injected with [D-Ala2]-Met-enkephalin-NH2 and with just as few errors. Injection of morphine seemed to result in slower running times and more errors in the maze. Enkephalin and some of its analogs can apparently exert significant behavioral changes after ip administration;these behavioral effects probably can be dissociated from the opiate effects.

关键词：行为动物/药物作用脑啡肽类/投药和剂量脑啡肽类/药理学注射腹腔内学习/药物作用黑素细胞刺激激素类/药理学吗啡/药理学寡肽类/药理学嗅觉/药物作用刺激化学性时间因素动物男(雄)性大鼠

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The melanocortin 4 receptor mediates leptin stimulation of luteinizing hormone and prolactin surges in steroid-primed ovariectomized rats

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BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS 1999年第3期257卷 860-864页

作者： Watanobe, H Schiöth, HB Wikberg, JES Suda, T Hirosaki Univ Sch Med Dept Internal Med 3 Hirosaki Aomori 0368216 Japan Uppsala Univ Dept Pharmaceut Pharmacol S-75124 Uppsala Sweden Melacure Therapeut S-75318 Uppsala Sweden

We have previously reported that leptin, the product of the obese (ob) gene, may play a physiologically relevant role in the generation of estradiol/progesterone-induced luteinizing hormone (LH) and prolactin (PRL) surges in female rats. In the present study, we examined whether the stimulatory effect of leptin on the hormonal surges is mediated through the melanocortin (MC) 4 receptor in the brain, as is leptin's effect on feeding behavior. We also explored whether the MC4 receptor participates in tonic stimulation of steroid-induced LH and PRL surges. Experiments were performed on both normally fed and 3-day starved rats, which were ovariectomized and primed with estradiol and progesterone. At 11:00 h on the day of the experiments, the normally fed rats received an intracerebroventricular administration of artificial cerebrospinal fluid (vehicle), SHU 9119 (a nonselective MC3/MC4 receptor antagonist, 1.0 nmol), or HS014 (a selective MC4 receptor antagonist, 1.0 nmol). The 3-day starved rats were given vehicle, recombinant mouse leptin (0.3 nmol), leptin (0.3 nmol) + SHU9119 (1.0 nmol), or leptin (0.3 nmol) + HS014 (1.0 nmol), From 11:00 to 18:00 h, blood was collected every 30 min to measure LH and PRL. The 3-day starvation completely abolished both LH and PRL surges, but leptin significantly reinstated these hormonal surges. Both SHU9119 and HS014 significantly decreased the magnitude of LH and PRL surges in normally fed rats and also significantly blocked the leptin stimulation of the hormonal surges in starved rats. These results suggest that the MC4 receptor may be the pivotal subtype of MC receptors mediating the leptin stimulation of LH and PRL surges. The data also suggest that endogenous MC(s) may tonically stimulate the hormonal surges in normally fed rats via the MC4 receptor. This is the first report describing a physiological role of a specific MC receptor in regulating the reproductive axis, (C) 1999 Academic Press.

关键词：脑/药物作用雌二醇/药理学食品剥夺瘦素促黄体激素/血液黑素细胞刺激激素类/投药和剂量黑素细胞刺激激素类/药理学卵巢切除术肽类环/投药和剂量肽类环/药理学孕酮/药理学催乳素/血液蛋白质类/投药和剂量蛋白质类/药理学大鼠 Wistar 受体黑皮质素 3型受体黑皮质素 4型受体促肾上腺皮质激素/拮抗剂和抑制剂受体促肾上腺皮质激素/生理学重组蛋白质类/投药和剂量重组蛋白质类/药理学信号传导/药物作用甾类/药理学时间因素动物女(雌)性小鼠大鼠

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