WordNet

a complex consisting of an organic base in association with hydrogen chloride

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1. 過敏性腸症候群に対するアロセトロン塩酸塩（Lotronex） alosetron hydrochloride lotronex for irritable bowel syndrome
2. 変形性関節症の初回薬物療法 initial pharmacologic therapy of osteoarthritis
3. クリンダマイシン：概要 clindamycin an overview
4. 成人における急性咽頭炎の対症療法 symptomatic treatment of acute pharyngitis in adults
5. 慢性非アレルギー性鼻炎 chronic nonallergic rhinitis

English Journal

Metabolic effects of various beta-adrenoceptor blocking agents in rats and dogs.

Traunecker W.AbstractKoe 3290 (N-[3-cyano-4-[3-[(1, 1-dimethyl-2-propynyl)amino]-2-hydroxypropoxy] phenyl]-2-methyl-propionamide), Koe 4299 (N-[3-cyano-4-(3-tert-butylamino-2-hydroxypropoxy)phenyl]-hexanamide+ ++ hydrochloride), Koe 4302 (N-[3-cyano-4-[3-[(1, 1-dimethyl-2-propynyl)amino]-2-hydroxypropoxy]phenyl]-hexanamid e hydrochloride) and the well-known compounds propranolol, bunitrolol, atenolol and acebutolol inhibit isoprenaline-stimulated increase of the concentration of free fatty acids (FFA) in the plasma of rats and dogs. In rats, most of the cardioselective blockers (Koe 3290, Koe 4299, Koe 4302, acebutolol) diminish isoprenaline-stimulated lactate, after s.c. injection, in a dose range higher than that required to reduce FFA. With the exception of atenolol, these substances show a relative selectivity between antilipolytic and antiglycolytic activity in favour of the antilipolytic effect. The non-cardioselective substances, propranolol and bunitrolol, either do not or only slightly differentiate between the inhibition of FFA and that of lactate. In dogs, after i.v. injection, only Koe 3290 and acebutolol have a relative metabolic selectivity similar to that seen in rats, but the other beta-adrenoceptor antagonists, with and without cardioselectivity, do not differentiate between the inhibition of isoprenaline-stimulated FFA, and that of lactate and glucose. In contrast, a greater antiglycolytic effect is often seen. Interspecies differences between the rat and the dog and variations among the drugs tested are discussed in detail. Koe 3290 is the only highly cardioselective drug with marked antilipolytic activity which markedly differentiates, in both rats and dogs, between the inhibition of FFA and carbohydrates. This substance, therefore, would appear to offer some additional advantages in the therapy of myocardial ischemia.
Arzneimittel-Forschung.Arzneimittelforschung.1985;35(1A):376-82.
Koe 3290 (N-[3-cyano-4-[3-[(1, 1-dimethyl-2-propynyl)amino]-2-hydroxypropoxy] phenyl]-2-methyl-propionamide), Koe 4299 (N-[3-cyano-4-(3-tert-butylamino-2-hydroxypropoxy)phenyl]-hexanamide+ ++ hydrochloride), Koe 4302 (N-[3-cyano-4-[3-[(1, 1-dimethyl-2-propynyl)amino]-2-hydroxypropoxy]phenyl]-hexanam
PMID 2859032

Absence of high-affinity binding sites for beta-adrenergic blockers and lack of adenyl cyclase stimulation to beta-adrenergic stimulators in most normal and adenomatous human thyroid tissues.

Goretzki PE, Wahl RA, Branscheid D, Roeher HD.AbstractTo determine whether the beta-blocking drug propranolol had any physiologic effect on normal (n = 14) and adenomatous (n = 15) human thyroid tissues, experiments were performed to study the binding of the beta-blockers 125I-iodocyanopindolol (125I-ICYP) and 125I-iodohydroxybenzylpindolol (125I-IHYP) and the stimulation of adenyl cyclase (AC) by isoproterenol. 125I-ICYP and 125I-IHYP failed to show high-affinity binding in 27 of 29 specimens, whereas two (one normal and one adenomatous) thyroid tissues demonstrated high-affinity binding (Kd 5.5 +/- 1 X 10(-9) M) for 125I-ICYP. Thyroid-stimulating hormone (0.3 IU/ml), guanosine triphosphate (10(-4) M), and Gpp (NH)p(10(-4) M) stimulated AC in all thyroid tissues, although in two tissues (normal) Gpp (NH)p failed to cause a significant increase. Isoproterenol (10(-4) M), in contrast, had no effect on basal AC activity or on guanosine triphosphate, and Gpp (NH) p stimulated AC activity in 26 of the 29 thyroid tissues. In one of the two tissues that increased AC in response to isoproterenol, the beta-blocking drugs propranolol hydrochloride, bunitrolol hydrochloride, and tolilprolol hydrochloride decreased AC stimulation to isoproterenol at concentrations of 10(-6) M (p less than 0.05). Higher concentrations of propranolol (10(-4) - 10(-2) M) decreased AC stimulation to thyroid-stimulating hormone (p less than 0.01), not only in this responsive tissue but also in tissues that failed to demonstrate high-affinity binding for 125I-ICYP and AC stimulation to isoproterenol (p less than 0.01). Thus most normal and adenomatous human thyroid tissues lack beta-receptors and a functioning beta-receptor AC system. High concentrations of propranolol in vitro decreased AC response by thyroid-stimulating hormone, but this is probably a nonreceptor-mediated effect.
Surgery.Surgery.1984 Dec;96(6):1001-8.
To determine whether the beta-blocking drug propranolol had any physiologic effect on normal (n = 14) and adenomatous (n = 15) human thyroid tissues, experiments were performed to study the binding of the beta-blockers 125I-iodocyanopindolol (125I-ICYP) and 125I-iodohydroxybenzylpindolol (125I-IHYP)
PMID 6150553

Effect of adrenergic neurotransmitters upon the ejaculatory process in the stallion.

Klug E, Deegen E, Lazarz B, Rojem I, Merkt M.AbstractSuccessful empirical treatment of 17 out of 24 stallions, which had failed to ejaculate after normal penile erection, intromission and friction, by chemical blockage of beta-receptors and additional stimulation of alpha-receptors led us to investigate stallions with normal ejaculatory patterns. In an initial experiment one adult half-bred stallion was injected with 4.88 mg noradrenaline hydrochloride (treatment A), 10 mg bunitrolol (treatment B = beta-receptor blockage) and a combination of treatment A and B. Investigations of the same stallion on dated occasions without treatment served as controls. The test criteria were heart rate during copulation by telemetric measurement, volume of ejaculates and sperm concentration per ml and per ejaculate. In a second experiment, 2 stallions were treated after a modified test schedule. In addition to the criteria used in the first experiment seminal citric acid, ergothioneine, and glycerophosphocholine were measured. Administration of the beta-blocker alone or in combination with alpha-receptor stimulation resulted in (a) significant lowering of the maximal heart rate, (b) significant increase of sperm count per ejaculate and (c) significant rise of glycerophosphocholine.
Journal of reproduction and fertility. Supplement.J Reprod Fertil Suppl.1982;32:31-4.
Successful empirical treatment of 17 out of 24 stallions, which had failed to ejaculate after normal penile erection, intromission and friction, by chemical blockage of beta-receptors and additional stimulation of alpha-receptors led us to investigate stallions with normal ejaculatory patterns. In a
PMID 6132008