Abstract:
:1. In order to further characterize the adenosine binding sites that we previously purified and termed P3 purinergic receptor-like protein (P3LP), a reliable binding assay method was developed using [3H]-5'-N-ethylcarboxamidoadenosine (NECA) as a radioligand and the newly developed high-affinity selective ligand 9-(6,7-dideoxy-beta-D-allo-hept-5-ynofuranosyl) adenine (HAK2701) as a selective displacer. 2. Using this assay method, it was found that rat brain membranes possess high- and low-affinity [3H]-NECA binding sites. The high-affinity binding site showed KD and Bmax values of 19.7+/-2.5 nmol/L and 0.192+/-0.05 pmol/mg protein, respectively, and the KD value for the low-affinity binding site was 4260+/-330 nmol/L. The KD value for the high-affinity site agreed well with that of the [3H]-NECA binding site determined with the partially purified P3LP preparation described previously. 3. The distribution of P3LP in rat tissues was determined using the [3H]-NECA binding method described above. The highest level of P3LP was in the cerebellum followed by the olfactory bulb and the spinal cord. 4. The order of the affinity for various purinergic or related compounds to P3LP in rat brain preparations was also determined by the [3H]-NECA binding method to be HAK2701 > NECA = adenosine 5'-O-(2-thiodiphosphate) > cAMP = beta,gamma-methyleneadenosine 5'-triphosphate > diadenosine tetraphosphate > alpha,beta-methyleneadenosine 5'-triphosphate > 5'-deoxy-5'-methylthioadenosine > N6-cyclopentyladenosine. 5. These studies reveal that the [3H]-NECA binding assay in combination with HAK2701 is successful in the characterization of P3LP, especially the membrane-bound form.
journal_name
Clin Exp Pharmacol Physioljournal_title
Clinical and experimental pharmacology & physiologyauthors
Yoshioka K,Matsuda A,Nakata Hdoi
10.1046/j.1440-1681.2001.03438.xkeywords:
subject
Has Abstractpub_date
2001-04-01 00:00:00pages
278-84issue
4eissn
0305-1870issn
1440-1681pii
cep3438journal_volume
28pub_type
杂志文章abstract::Members of the transient receptor potential (TRP) channel superfamily are present in vascular smooth muscle cells and play important roles in the regulation of vascular contractility. The TRPC3 and TRPC6 channels are activated by stimulation of several excitatory receptors in vascular smooth muscle cells. Activation o...
journal_title:Clinical and experimental pharmacology & physiology
pub_type: 杂志文章,评审
doi:10.1111/j.1440-1681.2007.04855.x
更新日期:2008-09-01 00:00:00
abstract::1. Four, six and eight hours after gavage of rats with alpha-mercapto-beta-(2-furan)acrylic acid (MFA) (25 mg/kg) serum zinc concentration was increased ten-fold over control levels and a mean molar ratio of 1 albumin:0-4 zinc:0-8 MFA was found for seventeen sera. 2. At pH 7-5 a maximum of 1 mole of MFA could be bound...
journal_title:Clinical and experimental pharmacology & physiology
pub_type: 杂志文章
doi:10.1111/j.1440-1681.1977.tb02374.x
更新日期:1977-01-01 00:00:00
abstract::1. In the rectum and distal nephron, sodium reabsorption is mediated by the amiloride-sensitive epithelial sodium channel (ENaC). The ENaC-mediated sodium transport is electrogenic and creates an amiloride-sensitive transepithelial potential difference (PD). 2. We have evaluated the salt- and angiotensin (Ang)II-depen...
journal_title:Clinical and experimental pharmacology & physiology
pub_type: 杂志文章
doi:10.1046/j.1440-1681.2000.03204.x
更新日期:2000-01-01 00:00:00
abstract::1. NBPA is a derivative of 3-n-butylpathalide isolated from Apium granolens Linn. 2. At concentrations ranging from 6 x 10(-6) to 10(-6) mol/L, NBPA inhibited the L-type calcium current in guinea-pig myocardial cells and cultured human neuroblastoma cells. 3. At 10(-6) mol/L, NBPA markedly inhibited calcium-dependent ...
journal_title:Clinical and experimental pharmacology & physiology
pub_type: 杂志文章
doi:10.1046/j.1440-1681.1999.03144.x
更新日期:1999-10-01 00:00:00
abstract::1. The effects of ethacrynic acid were studied on relaxations elicited by nitric oxide (NO), the NO-donors sodium nitroprusside (SNP) and glyceryl trinitrate (GTN), nitrergic nerve stimulation and the NO-independent agent papaverine in isolated preparations of rat anococcygeus muscles. 2. Ethacrynic acid (100 mumol/L)...
journal_title:Clinical and experimental pharmacology & physiology
pub_type: 杂志文章
doi:10.1111/j.1440-1681.1994.tb02515.x
更新日期:1994-04-01 00:00:00
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journal_title:Clinical and experimental pharmacology & physiology
pub_type: 杂志文章
doi:10.1111/j.1440-1681.1993.tb01698.x
更新日期:1993-05-01 00:00:00
abstract::1. The worldwide epidemic of obesity in adults has been mirrored in children in developed and developing countries. 2. Central obesity appears to be driving a cluster of abnormalities often referred to as the metabolic syndrome. 3. The definition of the metabolic syndrome in children is not suited to arbitrary cut-off...
journal_title:Clinical and experimental pharmacology & physiology
pub_type: 杂志文章
doi:10.1111/j.1440-1681.2008.04887.x
更新日期:2008-04-01 00:00:00
abstract::1. Tissue plasminogen activator (tPA) has both fibrinolytic and anti-inflammatory activity. These properties may be useful in treating inflammatory lung diseases, such as acute respiratory distress syndrome (ARDS). 2. We have previously demonstrated the feasibility of targeted pulmonary delivery of tPA. As part of our...
journal_title:Clinical and experimental pharmacology & physiology
pub_type: 杂志文章
doi:10.1111/j.1440-1681.2008.05011.x
更新日期:2008-12-01 00:00:00
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pub_type: 杂志文章
doi:10.1111/j.1440-1681.1998.tb02253.x
更新日期:1998-07-01 00:00:00
abstract::1. Activation of bulbospinal neurons projecting from the C1 area of the rostral ventrolateral medulla evokes a pressor response. The nature of the neurotransmitters involved in mediating this response at spinal cord level has not been established. 2. Amino acid antagonists were introduced into the spinal subarachnoid ...
journal_title:Clinical and experimental pharmacology & physiology
pub_type: 杂志文章
doi:10.1111/j.1440-1681.1988.tb01056.x
更新日期:1988-02-01 00:00:00
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journal_title:Clinical and experimental pharmacology & physiology
pub_type: 杂志文章
doi:10.1046/j.1440-1681.2000.03330.x
更新日期:2000-09-01 00:00:00
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journal_title:Clinical and experimental pharmacology & physiology
pub_type: 杂志文章
doi:10.1111/j.1440-1681.2007.04745.x
更新日期:2008-01-01 00:00:00
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journal_title:Clinical and experimental pharmacology & physiology
pub_type: 杂志文章
doi:10.1111/j.1440-1681.1983.tb00172.x
更新日期:1983-01-01 00:00:00
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doi:10.1111/1440-1681.13234
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pub_type: 杂志文章,评审
doi:10.1111/j.1440-1681.2009.05265.x
更新日期:2010-03-01 00:00:00
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journal_title:Clinical and experimental pharmacology & physiology
pub_type: 杂志文章,评审
doi:10.1111/1440-1681.12969
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journal_title:Clinical and experimental pharmacology & physiology
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doi:10.1111/1440-1681.12611
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journal_title:Clinical and experimental pharmacology & physiology
pub_type: 杂志文章
doi:10.1111/j.1440-1681.1977.tb02683.x
更新日期:1977-11-01 00:00:00
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journal_title:Clinical and experimental pharmacology & physiology
pub_type: 杂志文章,随机对照试验
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更新日期:2016-03-01 00:00:00
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journal_title:Clinical and experimental pharmacology & physiology
pub_type: 杂志文章
doi:10.1111/j.1440-1681.2003.03939.x
更新日期:2003-12-01 00:00:00
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journal_title:Clinical and experimental pharmacology & physiology
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doi:10.1111/1440-1681.13332
更新日期:2020-09-01 00:00:00
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journal_title:Clinical and experimental pharmacology & physiology
pub_type: 杂志文章
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更新日期:2010-05-01 00:00:00
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journal_title:Clinical and experimental pharmacology & physiology
pub_type: 杂志文章
doi:10.1111/j.1440-1681.2004.03945.x
更新日期:2004-01-01 00:00:00
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journal_title:Clinical and experimental pharmacology & physiology
pub_type: 杂志文章,评审
doi:10.1111/j.1440-1681.1995.tb01976.x
更新日期:1995-03-01 00:00:00
abstract::1. To investigate the effect of an exercise training programme on antihypertensive drug requirements, 19 sedentary subjects (14 men and five women) with mild essential hypertension (systolic blood pressure greater than 140 mmHg but less than 180 mmHg), aged 29-55 years, were randomly assigned to 16 weeks of moderate i...
journal_title:Clinical and experimental pharmacology & physiology
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1111/j.1440-1681.1991.tb01445.x
更新日期:1991-05-01 00:00:00
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journal_title:Clinical and experimental pharmacology & physiology
pub_type: 杂志文章
doi:10.1111/j.1440-1681.1996.tb02795.x
更新日期:1996-06-01 00:00:00
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journal_title:Clinical and experimental pharmacology & physiology
pub_type: 临床试验,更正并重新发布的文章,杂志文章,随机对照试验
doi:10.1111/j.1440-1681.1998.tb02199.x
更新日期:1998-02-01 00:00:00
abstract::1. Clinical pharmacology requires numerous skills and most activities involve interactions with other specialities, both clinical and experimental. 2. A range of experts has had a major influence on the nature and design of my research, which is illustrated by the evolution of my knowledge of adverse drug reactions an...
journal_title:Clinical and experimental pharmacology & physiology
pub_type:
doi:10.1046/j.1440-1681.2001.03542.x
更新日期:2001-11-01 00:00:00