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- bufetolol hydrochloride
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出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2018/04/16 13:57:27」(JST)
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Bufetolol
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Names |
IUPAC name
1-(tert-Butylamino)-3-[2-(oxolan-2-ylmethoxy)phenoxy]propan-2-ol
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Identifiers |
CAS Number
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3D model (JSmol)
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ChEMBL |
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ChemSpider |
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KEGG |
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UNII |
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InChI
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InChI=1S/C18H29NO4/c1-18(2,3)19-11-14(20)12-22-16-8-4-5-9-17(16)23-13-15-7-6-10-21-15/h4-5,8-9,14-15,19-20H,6-7,10-13H2,1-3H3
Key: AKLNLVOZXMQGSI-UHFFFAOYSA-N
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InChI=1/C18H29NO4/c1-18(2,3)19-11-14(20)12-22-16-8-4-5-9-17(16)23-13-15-7-6-10-21-15/h4-5,8-9,14-15,19-20H,6-7,10-13H2,1-3H3
Key: AKLNLVOZXMQGSI-UHFFFAOYAN
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SMILES
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CC(C)(C)NCC(COC1=CC=CC=C1OCC2CCCO2)O
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Properties |
Chemical formula
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C18H29NO4 |
Molar mass |
323.43 g·mol−1 |
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
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Infobox references |
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Bufetolol is a beta-adrenoceptor antagonist.[1]
References
- ^ Sada, H; Harada, S; Ban, T (1983). "Effects of beta-adrenoceptor blocking agents of N-tertiary butyl derivatives on maximum upstroke velocity of action potential in guinea-pig papillary muscles". Naunyn-Schmiedeberg's archives of pharmacology. 324 (1): 50–7. doi:10.1007/bf00647838. PMID 6138715.
Adrenergic receptor modulators
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α1 |
- Agonists: 6-FNE
- Amidephrine
- Anisodine
- Buspirone
- Cirazoline
- Corbadrine
- Desglymidodrine
- Dexisometheptene
- Dipivefrine
- Dopamine
- Droxidopa (L-DOPS)
- Ephedrine
- Epinephrine
- Etilefrine
- Etilevodopa
- Ethylnorepinephrine
- Indanidine
- Isometheptene
- L-DOPA (levodopa)
- L-Phenylalanine
- L-Tyrosine
- Melevodopa
- Metaraminol
- Methoxamine
- Methyldopa
- Midodrine
- Naphazoline
- Norepinephrine
- Octopamine (drug)
- Oxymetazoline
- Phenylephrine
- Phenylpropanolamine
- Pseudoephedrine
- Synephrine
- Tetryzoline
- Tiamenidine
- XP21279
- Xylometazoline
- Antagonists: Abanoquil
- Adimolol
- Ajmalicine
- Alfuzosin
- Amosulalol
- Anisodamine
- Arotinolol
- Atiprosin
- Atypical antipsychotics (e.g., brexpiprazole, clozapine, olanzapine, quetiapine, risperidone)
- Benoxathian
- Buflomedil
- Bunazosin
- Carvedilol
- Corynanthine
- Dapiprazole
- Domesticine
- Doxazosin
- Ergolines (e.g., ergotamine, dihydroergotamine, lisuride, terguride)
- Etoperidone
- Eugenodilol
- Fenspiride
- Hydroxyzine
- Indoramin
- Ketanserin
- L-765,314
- Labetalol
- mCPP
- Mepiprazole
- Metazosin
- Monatepil
- Moxisylyte
- Naftopidil
- Nantenine
- Neldazosin
- Niaprazine
- Nicergoline
- Niguldipine
- Pardoprunox
- Pelanserin
- Perlapine
- Phendioxan
- Phenoxybenzamine
- Phentolamine
- Phenylpiperazine antidepressants (e.g., hydroxynefazodone, nefazodone, trazodone, triazoledione)
- Piperoxan
- Prazosin
- Quinazosin
- Quinidine
- Ritanserin
- Silodosin
- Spiperone
- Talipexole
- Tamsulosin
- Terazosin
- Tiodazosin
- Tolazoline
- Tetracyclic antidepressants (e.g., amoxapine, maprotiline, mianserin)
- Tricyclic antidepressants (e.g., amitriptyline, clomipramine, doxepin, imipramine, trimipramine)
- Trimazosin
- Typical antipsychotics (e.g., chlorpromazine, fluphenazine, loxapine, thioridazine)
- Urapidil
- WB-4101
- Zolertine
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α2 |
- Agonists: (R)-3-Nitrobiphenyline
- 4-NEMD
- 6-FNE
- Amitraz
- Apraclonidine
- Brimonidine
- Cannabivarin
- Clonidine
- Corbadrine
- Detomidine
- Dexmedetomidine
- Dihydroergotamine
- Dipivefrine
- Dopamine
- Droxidopa (L-DOPS)
- Etilevodopa
- Ephedrine
- Ergotamine
- Epinephrine
- Etilefrine
- Ethylnorepinephrine
- Guanabenz
- Guanfacine
- Guanoxabenz
- L-DOPA (levodopa)
- L-Phenylalanine
- L-Tyrosine
- Lofexidine
- Medetomidine
- Melevodopa
- Methyldopa
- Mivazerol
- Naphazoline
- Norepinephrine
- Oxymetazoline
- Phenylpropanolamine
- Piperoxan
- Pseudoephedrine
- Rezatomidine
- Rilmenidine
- Romifidine
- Talipexole
- Tasipimidine
- Tetrahydrozoline
- Tiamenidine
- Tizanidine
- Tolonidine
- Urapidil
- Vatinoxan
- XP21279
- Xylazine
- Xylometazoline
- Antagonists: 1-PP
- Adimolol
- Amesergide
- Aptazapine
- Atipamezole
- Atypical antipsychotics (e.g., asenapine, brexpiprazole, clozapine, lurasidone, paliperidone, quetiapine, risperidone, zotepine)
- Azapirones (e.g., buspirone, gepirone, ipsapirone, tandospirone)
- BRL-44408
- Buflomedil
- Cirazoline
- Efaroxan
- Esmirtazapine
- Fenmetozole
- Fluparoxan
- Idazoxan
- mCPP
- Mianserin
- Mirtazapine
- NAN-190
- Olanzapine
- Pardoprunox
- Phentolamine
- Phenoxybenzamine
- Piperoxan
- Piribedil
- Rauwolscine
- Rotigotine
- SB-269970
- Setiptiline
- Spiroxatrine
- Sunepitron
- Tolazoline
- Typical antipsychotics (e.g., chlorpromazine, fluphenazine, loxapine, thioridazine)
- Yohimbine
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β |
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English Journal
- Different effects of various beta-adrenoceptor antagonists on adenylate cyclase, guanylate cyclase and calmodulin-dependent phosphodiesterase in heart.
- Kudo S, Nozawa Y.AbstractA series of six beta-adrenergic blocking drugs including propranolol, bufetolol, bunitrolol, pindolol, labetalol and acebutolol were examined for effects on adenylate cyclase, guanylate cyclase and calmodulin-dependent phosphodiesterase from heart. The adrenergic blocking agents had no apparent effects on basal activities of adenylate cyclase, guanylate cyclase and phosphodiesterase. The drugs blocked the enhancement of adenylate cyclase activity by isoproterenol, but not by guanine nucleotide or fluoride. The inhibitory effects of beta-antagonists were overcome by sufficiently large doses of isoproterenol. Sodium azide specifically required catalase whereas NaNO2 required cysteine to activate myocardial guanylate cyclase. Among beta-adrenergic blocking drugs tested, both pindolol and acebutolol inhibited the stimulation of guanylate cyclase by NaNo2 or N-methyl-N'-nitro-N-nitrosoguanidine (MNNG). However, other beta-blocking drugs did not significantly affect the activation by NaN3, NaNO2 and MNNG. Several beta-antagonists, such as labetalol, bunitrolol, pindolol and acebutolol were also effective in blocking the activation of phosphodiesterase by calmodulin. The inhibitory effects of beta-adrenergic blocking drugs, i.e. pindolol and acebutolol upon either nitroso compound-stimulated guanylate cyclase or calmodulin-activated phosphodiesterase display little correlation with their potency as beta-adrenergic blocking agents. These data suggest that beta-antagonists may have another site of action which is not directly related to the control of catecholamine metabolism.
- Biochemical pharmacology.Biochem Pharmacol.1985 May 15;34(10):1659-64.
- A series of six beta-adrenergic blocking drugs including propranolol, bufetolol, bunitrolol, pindolol, labetalol and acebutolol were examined for effects on adenylate cyclase, guanylate cyclase and calmodulin-dependent phosphodiesterase from heart. The adrenergic blocking agents had no apparent effe
- PMID 2860906
- Presynaptic inhibition by serotonin of cardiac sympathetic transmission in dogs.
- Kimura T, Satoh S.AbstractThe effect of serotonin on cardiac sympathetic transmission was investigated in vagotomized and cardiac decentralized dogs. Administration of serotonin in doses of 10-100 micrograms/kg i.v., during the resting unstimulated state caused tachycardia and pressor responses which were inhibited by cyproheptadine but not by guanethidine. The tachycardia was reduced by a beta-adrenoceptor antagonist, bufetolol. Serotonin in doses of 3-100 micrograms/kg depressed the elevated heart rate during maintained electrical stimulation of the cardiac sympathetic nerves. Cyproheptadine did not antagonize the serotonin-induced depression of the stimulation-elevated heart rate, while desipramine attenuated but did not abolish it. Serotonin did not have a significant effect on the heart rate elevated by maintained infusion of noradrenaline. The present results suggest that serotonin-induced depression of heart rate during sympathetic nerve stimulation is due to presynaptic inhibition by serotonin of cardiac sympathetic transmission which is not mediated via 'classic' tryptaminergic receptors.
- Clinical and experimental pharmacology & physiology.Clin Exp Pharmacol Physiol.1983 Sep-Oct;10(5):535-42.
- The effect of serotonin on cardiac sympathetic transmission was investigated in vagotomized and cardiac decentralized dogs. Administration of serotonin in doses of 10-100 micrograms/kg i.v., during the resting unstimulated state caused tachycardia and pressor responses which were inhibited by cyproh
- PMID 6315283
- Effects of beta-adrenoceptor blocking agents of N-tertiary butyl derivatives on maximum upstroke velocity of action potential in guinea-pig papillary muscles.
- Sada H, Harada S, Ban T.AbstractThe effects of bufetolol (27.8-138.9 mumol/l), bunitrolol (70.2-351.1 mumol/l), bupranolol (16.2-100 mumol/l), carteolol (60.7-607 mumol/l), D32 (17.3-100 mumol/l), penbutolol (1.5-29.4 mumol/l) and timolol (115.5 and 231.2 mumol/l) on action potentials were investigated in isolated guinea-pig papillary muscles. All these beta-adrenoceptor blocking agents of teritary butyl aminopropranol derivatives produced a concentration-dependent reduction of Vmax at driving rates of 1 Hz, 0.027 Hz and 4 Hz. The reduction was frequency-dependent but at all the rates penbutolol was highest in potency, as estimated by ED30 (0.027 Hz) and ED 50 values (1 and 4 Hz), followed by bupranolol, D-32, bufetolol and bunitrolol. These were followed in turn by timolol and carteolol in ED30 at 0.027 Hz and ED50 at 1 Hz, but by carteolol and timolol in ED50 at 4 Hz. Each log (1/ED) value is a linear function of log n-octanol/water partition coefficient (log P). The slope and intercept (the value at log P = 0) of the line of log (1/ED50) at 4 Hz are steeper and higher, respectively, than those of the lines at the other frequencies. The time course of recovery of Vmax during diastole was studied by assessing Vmax in premature responses at 0.027 Hz, being approximated by a single exponential function. The time constants of recovery (tau) and intercepts (Ao: the value extrapolated to the time of APD90 of the conditioning responses) at the level of ED50 and at 100 mumol/l of the drugs were thus estimated.(ABSTRACT TRUNCATED AT 250 WORDS)
- Naunyn-Schmiedeberg's archives of pharmacology.Naunyn Schmiedebergs Arch Pharmacol.1983 Sep;324(1):50-7.
- The effects of bufetolol (27.8-138.9 mumol/l), bunitrolol (70.2-351.1 mumol/l), bupranolol (16.2-100 mumol/l), carteolol (60.7-607 mumol/l), D32 (17.3-100 mumol/l), penbutolol (1.5-29.4 mumol/l) and timolol (115.5 and 231.2 mumol/l) on action potentials were investigated in isolated guinea-pig papil
- PMID 6138715
Japanese Journal
- POSSIBLE SIGNIFICANCE OF THE PHARMACOLOGICAL DIFFERENTIATION OF BETA-BLOCKING AGENTS IN HEMODYNAMIC EFFECTS IN ESSENTIAL HYPERTENSION
- TSUKIYAMA HISAICHIRO,OTSUKA KEIKO,HORII MASAKO,YOSHII YUZURU,HATORI YUTAKA,NAKAMURA YUTAKA,NEMOTO EIICHIRO,YAMATO TORAAKI,SAKAI TOSHIKO,YAMAMOTO YOOICHI
- Japanese circulation journal 47(3), 313-322, 1983-03-20
- … Effects of non-cardioselective ones were classified arbitrarily into the following 3 patterns : 1) reduction of CI of more than 0.50 L/min/m^2 and a slight increase of TPRI by more than 150 dyne・sec・cm^<-5>・m^2 (nadolol, propranolol, oxprenolol and penbutolol), 2)reduction TPRI by more than 150 dyne・sec・cm^<-5>・m^2 (pindolol, bunitrolol and labetalol) and 3) the intermediate hemodynamic responses between the two patterns described above (carteolol, bupranolol and bufetolol). …
- NAID 110002577528
- 各種振戦に対するBufetololの臨床応用--効果判定の定量的吟味と文献的考察を中心に
- 過換気症候群とβ受容体機能 : 過換気症候群に対するβ遮断剤の臨床効果(呼吸器心身症の病態と治療(第21回日本心身医学会総会シンポジウム))
- 印東 利勝,安藤 一也
- 心身医学 20(5), 424-428, 1980-10-01
- … In the present study, preventive effect of the hyperventilation attack by β blocker administration was studied for a long period.In 38 cases were administered daily dose of 10 or 15mg of bufetolol hydrochloride only and in 29 cases associated with intense anxiety were administered same amount of bufetolol hydrochloride in combination with anti-anxiety drugs for several months.The following results were obtained.(1) The frequency of HV attacks decreased significantly under each therapeutic method. …
- NAID 110001119572
Related Links
- Bufetololとは?goo Wikipedia (ウィキペディア) 。出典:Wikipedia(ウィキペディア)フリー百科事典。 Bufetololとは - goo Wikipedia (ウィキペディア) gooトップ サイトマップ スタートページに設定 RSS ヘルプ メニューへスキップ 本文へ ...
- Bufetolol(Adobiol)の高血圧症に対する臨床治験 小沢 幸雄 [他] この論文をさがす NDL-OPAC CiNii Books 著者 小沢 幸雄 [他] 収録刊行物 臨牀と研究 臨牀と研究 54(6), p2062-2065, 1977-06 大道学館出版部 Tweet 各種コード NII論文 ...
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