Pharmacological actions of AH-9700 on micturition reflex in anesthetized rats

Shimizu, Isao; Kawashima, Katsuyoshi; Ishii, Daisuke; Oku, Seiko; Kohayakawa, Hitoshi; Oka, Makoto

doi:10.1016/s0014-2999(00)00937-7

Cited by 5 publications

(7 citation statements)

References 22 publications

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“…The current result of the effect of oxybutynin on RBCs is consistent with previous reports (Doi et al, 2000;Shimizu et al, 2001). In addition, we have performed an in vitro study and found that TRK-130 at 1 mM did not significantly inhibit electrical field stimulation-induced contractions in isolated rat bladder strips (data not shown).…”

Section: A New Drug Candidate For Overactive Bladdersupporting

confidence: 93%

Characteristics of TRK-130 (Naltalimide), a Novel Opioid Ligand, as a New Therapeutic Agent for Overactive Bladder

Fujimura

Izumimoto

Momen

et al. 2014

J Pharmacol Exp Ther

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We characterized 6R,14S)-17-(cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxymorphinan-6-yl]phthalimide; naltalimide), an opioid ligand, to clarify the therapeutic potential for overactive bladder (OAB). In radioligand-binding assays with cells expressing human m-opioid receptors (MORs), d-opioid receptors (DORs), or k-opioid receptors (KORs), TRK-130 showed high selectivity for MORs (K i for MORs, DORs, and KORs 5 0.268, 121, and 8.97 nM, respectively). In a functional assay (cAMP accumulation) with cells expressing each human opioid receptor subtype, TRK-130 showed potent but partial agonistic activity for MORs [EC 50 (E max )

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Section: A New Drug Candidate For Overactive Bladdersupporting

confidence: 93%

Characteristics of TRK-130 (Naltalimide), a Novel Opioid Ligand, as a New Therapeutic Agent for Overactive Bladder

Fujimura

Izumimoto

Momen

et al. 2014

J Pharmacol Exp Ther

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“…Shimizu et al [2000Shimizu et al [ , 2001 showed that (þ)-pentazocine and 1,3-di-o-tolylguanidine (DTG) prolong micturition intervals, indicative of increased bladder capacity, and raised the threshold bladder pressure after either i.v. or i.c.v.…”

Section: Discussionmentioning

confidence: 99%

“…Dextromethorphan also exhibits relatively high a⁄nity for the sigma-1 receptor [Chou et al, 1999] and there is some evidence that sigma-1 receptors mediate its antitussive e⁄cacy [Brown et al, 2004]. Although relatively little is known about the role of sigma receptors in micturition, Shimizu et al [2000Shimizu et al [ , 2001 reported that sigma receptor agonists reduce the frequency of volume-induced bladder contractions, increase bladder capacity and raise the threshold pressure for micturition in anesthetized rats. Interestingly, the sigma receptor agonist 1,3-di-o-tolylguanidine also inhibits electrically stimulated contractions of isolated bladder strips in vitro [Shimizu et al, 2000].…”

Section: Introductionmentioning

confidence: 99%

Effects of dextromethorphan on in vitro contractile responses of mouse and rat urinary bladders

Levin

Whitbeck

Sourial

et al. 2006

Neurourology and Urodynamics

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“…Thus, opiate agonists may offer a therapeutic advantage over other groups of drugs, delaying micturition without inhibiting the micturition reflex itself. Studies in the rat support this hypothesis [123] and suggest that central opiate receptors may prove a very useful target for drug development if the analgesic and addictive actions can be separated from these therapeutic effects. The effect of these agents on micturition interval without affecting detrusor contraction during micturition would offer a possible advantage over other treatments.…”

Section: Opioid Receptorsmentioning

confidence: 90%

Potential therapeutic targets for the treatment of detrusor overactivity

Chess‐Williams¹

2004

Expert Opinion on Therapeutic Targets

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Current treatments for the overactive detrusor are poorly tolerated and can exert significant adverse effects. Possible targets for the development of new treatments are considered. Potential targets in four locations are examined: detrusor smooth muscle, urothelium, peripheral nerves and the CNS. In the detrusor, the role of various muscarinic receptor subtypes is discussed and beta-adrenoceptor agonists, phosphodiesterase inhibitors and potassium channel openers, all of which inhibit detrusor contractility, are considered for drug development. In the urothelium, a number of substances are released that affect bladder function including ATP, acetylcholine and an inhibitory factor that has yet to be identified. All three systems have the potential to be novel targets for drug development. Other possible therapeutic targets are the mechanisms influencing transmitter release in the bladder, for example, prejunctional 5-hydroxytryptamine (5-HT) 4 receptors. Finally, targets within the CNS and spinal cord are considered, including opioid receptors, 5-HT receptors and alpha-adrenoceptors.

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Pharmacological actions of AH-9700 on micturition reflex in anesthetized rats

Cited by 5 publications

References 22 publications

Characteristics of TRK-130 (Naltalimide), a Novel Opioid Ligand, as a New Therapeutic Agent for Overactive Bladder

Characteristics of TRK-130 (Naltalimide), a Novel Opioid Ligand, as a New Therapeutic Agent for Overactive Bladder

Effects of dextromethorphan on in vitro contractile responses of mouse and rat urinary bladders

Potential therapeutic targets for the treatment of detrusor overactivity

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