hv-723 and 5-methylurapidil

hv-723 has been researched along with 5-methylurapidil* in 3 studies

Other Studies

3 other study(ies) available for hv-723 and 5-methylurapidil

ArticleYear
Binding and functional characterization of alpha1-adrenoceptor subtypes in the rat prostate.
    European journal of pharmacology, 1999, Jan-29, Volume: 366, Issue:1

    The alpha1-adrenoceptor subtypes of rat prostate were characterized in binding and functional experiments. In binding experiments, [3H]tamsulosin bound to a single class of binding sites with an affinity (pKD) of 10.79+/-0.04 and Bmax of 87+/-2 fmol mg(-1) protein. This binding was inhibited by prazosin, 2-(2,6-dimethoxy-phenoxyethyl)-aminomethyl-1,4-benzodioxane hydrochloride (WB4101), 5-methylurapidil, alpha-ethyl-3,4,5,-trimethoxy-alpha-(3-((2-(2-methoxyphenoxy)ethyl)-amin o)-propyl)benzeneacetonitrile fumarate (HV723) and oxymetazoline with high efficacy, resulting in a good correlation with the binding characteristics of cloned alpha1a but not alpha1b and alpha1d-adrenoceptor subtypes. In functional studies, noradrenaline and oxymetazoline produced concentration-dependent contractions. These contractions were antagonized by tamsulosin, prazosin, WB4101 and 5-methylurapidil with an efficacy lower than that exhibited by these agents for inhibition of [3H]tamsulosin binding. The relationship between receptor occupancy and contractile amplitude revealed the presence of receptor reserve for noradrenaline, but the contraction induced by oxymetazoline was not in parallel with receptor occupation and developed after predicted receptor saturation. From these results, it is suggested that alpha1A-adrenoceptors are the dominant subtype in the rat prostate which can be detected with [3H]tamsulosin, but that the functional subtype mediating adrenergic contractions has the characteristics of the alpha1L-adrenoceptor subtype, having a lower affinity for prazosin and some other drugs than the alpha1A-adrenoceptor subtype.

    Topics: Acetonitriles; Adrenergic alpha-1 Receptor Antagonists; Adrenergic alpha-Agonists; Adrenergic alpha-Antagonists; Animals; Binding, Competitive; Dioxanes; Dose-Response Relationship, Drug; In Vitro Techniques; Kinetics; Male; Muscle Contraction; Norepinephrine; Oxymetazoline; Piperazines; Prazosin; Prostate; Radioligand Assay; Rats; Rats, Sprague-Dawley; Receptors, Adrenergic, alpha-1; Sulfonamides; Tamsulosin; Tritium

1999
Discrimination of alpha1-adrenoceptor subtypes in rat aorta and prostate.
    Pharmacology, 1998, Volume: 57, Issue:2

    This study was designed to further discriminate alpha1-adrenoceptor subtypes in rat aorta and prostate using functional experiments. Responses induced by phenylephrine were equilibrated in both tissues. The pA2 values and slope factors of several alpha1-antagonists were assessed using concentration-response curves. The antagonists used were prazosin, WB-4101, 5-methylurapidil (5-MU), HV-723, and tamsulosin. In addition, the effects of chloroethylclonidine (CEC) and nifedipine on phenylephrine-induced contractions were investigated. A high pA2 value for prazosin was observed in both tissues (aorta 9.84, prostate 9.19) and the ranking of each drug's pA2 value is as follows: tamsulosin > prazosin > WB-4101 > HV-723 > 5-MU in the aorta, and tamsulosin > prazosin > 5-MU > WB-4101 = HV-723 in the prostate. A significant difference between the pA2 value of each drug except for tamsulosin in the aorta and in prostate was observed (p < 0.01). Inhibition of contraction by pretreatment with CEC was 83.9 +/- 2.42% in the aorta, and 6.17 +/- 0.94% in the prostate. On the other hand, inhibition of maximal response by pretreatment with nifedipine (1 micromol/l) was 35.1 +/- 2.2% in the aorta and 24.5 +/- 3.1% in the prostate. A good correlation between these pA2 values and pKi values for recombinant human alpha1b-adrenoceptor expressed in CHO cells (aorta) and alpha1a-subtypes of CEC pretreated rat hippocampus (prostate) were observed. In conclusion, these results suggest that: (1) the contraction of these two tissues is mediated by alpha1H-adrenoceptor with a high affinity for prazosin; (2) alpha1H-adrenoceptors correspond to alpha1b-(aorta) and alpha1a-subtypes (prostate), and (3) each alpha1-adrenoceptor subtype in the aorta and prostate may be alpha1b-(aorta) and alpha1a-subtypes (prostate), respectively.

    Topics: Acetonitriles; Adrenergic alpha-1 Receptor Antagonists; Adrenergic alpha-Antagonists; Animals; Aorta; Clonidine; Dioxanes; Dose-Response Relationship, Drug; Male; Muscle Contraction; Muscle, Smooth; Nifedipine; Piperazines; Prazosin; Prostate; Rats; Rats, Wistar; Receptors, Adrenergic, alpha-1; Sulfonamides; Tamsulosin; Vasoconstriction; Vasodilator Agents

1998
Identification of alpha 1-adrenoceptor subtypes in the rabbit prostate.
    Journal of autonomic pharmacology, 1995, Volume: 15, Issue:4

    1. The alpha 1-adrenoceptor subtypes of rabbit prostate were characterized in binding and functional experiments. 2. In saturation experiments, [3H]-prazosin bound to two distinct affinity sites in the rabbit prostate (pKD = 11.20 +/- 0.22 and 8.39 +/- 0.11, Bmax = 15.3 and 736 fmol mg protein-1). 3. In the displacement experiments, the binding was inhibited with shallow displacement curves by unlabelled prazosin, WB4101, and 5-methylurapidil, suggesting the presence of two distinct affinity sites for prazosin, WB4101, or 5-methylurapidil. On the other hand, HV723 displaced the [3H]-prazosin binding monophasically with a low affinity. From the results, the presence of two distinct alpha 1-adrenoceptor subtypes was suggested; presumably one is the classical alpha 1A (cloned alpha 1C) subtype with high affinity for prazosin, WB4101 and 5-methylurapidil but not for HV723 and the other corresponds to the alpha 1L subtype, which shows low affinity for the four antagonists. 4. In the functional experiments, prazosin, WB4101, HV723 and 5-methylurapidil competitively antagonized the contractile response to noradrenaline with low affinities close to those for the alpha 1L subtype determined in binding experiments. These results suggest that contractile response to noradrenaline in the rabbit prostate is predominantly mediated through the alpha 1L subtype.

    Topics: Acetonitriles; Adrenergic alpha-Antagonists; Animals; Binding, Competitive; Dioxanes; Male; Muscle Contraction; Norepinephrine; Piperazines; Prazosin; Prostate; Rabbits; Radioligand Assay; Receptors, Adrenergic, alpha-1

1995