Last update 01 Nov 2024

Bupranolol Hydrochloride

Last update 01 Nov 2024

Overview

R&D Status

Clinical Result

Translational Medicine

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Bupranolol, Bupranolol hydrochloride (JP17), 布拉洛尔

+ [6]

Target

β-adrenoceptors

Mechanism

β-adrenoceptors antagonists(Beta adrenergic receptors antagonists)

Therapeutic Areas

Cardiovascular DiseasesEye Diseases

Active Indication

Cardiovascular DiseasesGlaucoma

Inactive Indication-

Originator Organization-

Active Organization-

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date-

Regulation-

Structure

Molecular FormulaC14H23Cl2NO2

InChIKeyWJUUZHQWGKSLIJ-UHFFFAOYSA-N

CAS Registry15148-80-8

View All Structures (2)

100 Clinical Results associated with Bupranolol Hydrochloride

100 Translational Medicine associated with Bupranolol Hydrochloride

100 Patents (Medical) associated with Bupranolol Hydrochloride

308

Literatures (Medical) associated with Bupranolol Hydrochloride

01 Jan 2021·Gynecologic and Obstetric InvestigationQ4 · MEDICINE

Myometrial Responses to Beta-Adrenoceptor Antagonists in Gynecological Malignancies

Q4 · MEDICINE

Article

Author: Sulkowski, Stanisław ; Kleszczewski, Tomasz ; Modzelewska, Beata ; Jóźwik, Marcin ; Jóźwik, Maciej

Objective: The aim of the study was to determine the influence of beta-adrenoceptor (ADRB) antagonists on contractile activity of the nonpregnant human uterus in patients affected by gynecological malignancies. Design: This was a controlled and prospective ex vivo study. Setting: The work was conducted as a collaboration between 4 academic departments. Materials and Methods: Myometrial specimens were obtained from women undergoing hysterectomy for benign gynecological disorders (reference group; N = 15), and ovarian (N = 15), endometrial (N = 15), synchronous ovarian-endometrial (N = 3), and cervical cancer (N = 10). Contractions of myometrial strips in an organ bath before and after applications of ADRB antagonists (propranolol, bupranolol, SR 59230A, and butoxamine) were studied under isometric conditions. Results: Propranolol and bupranolol attenuated contractions in the endometrial and cervical cancer groups similar to that in the reference group (all p < 0.05), whereas opposite effects were observed in the ovarian and synchronous ovarian-endometrial cancer groups. SR 59230A and butoxamine significantly increased contractions in the ovarian cancer group (both p < 0.001). Limitations: These results require now to be placed into a firm clinical context. Conclusions: Our study indicates that ovarian cancer considerably alters contractile activity of the nonpregnant human uterus in response to ADRB antagonists. This suggests a pathogenetic role of beta-adrenergic pathways in this malignancy. Furthermore, propranolol and bupranolol substantially influence spontaneous uterine contractility.

01 Jan 2020·Life SciencesQ3 · MEDICINE

Pharmacological properties of β-adrenoceptors mediating rat superior mesenteric artery relaxation and the effects of chemical sympathetic denervation

Q3 · MEDICINE

Article

Author: Takahasi, Hiromi ; Iiboshi, Yuri ; Tanaka, Yoshio ; Shigematsu, Mai ; Kasuya, Yoshitoshi ; Obara, Keisuke ; Yoshioka, Kento

AIMSβ-Adrenoceptors (β-ADRs) mediating the relaxation of rat superior mesenteric arteries (SMAs) were pharmacologically identified, and the effects of chemical sympathetic denervation on β-ADR-mediated relaxation were examined.MAIN METHODSThe tension changes of endothelium-denuded SMAs were isometrically recorded and the mRNA of endothelium-denuded SMA β-ADR was detected using RT-PCR.KEY FINDINGSIn endothelium-denuded SMAs contracted with ≥10^-7 M phenylephrine (an α₁-ADR agonist), isoprenaline (a β-ADR agonist)-induced relaxation was competitively inhibited by 3 × 10^-9-10^-8 M propranolol (a β_1,2-ADR antagonist), but not further affected by ≥10^-8 M propranolol. Although isoprenaline-induced relaxation was not affected by ICI-118,551 (10^-9-10^-8 M; a β₂-ADR antagonist), it was competitively inhibited by atenolol (10^-7-3 × 10^-7 M; a β₁-ADR antagonist) in the presence of ICI-118,551. In the presence of 10^-7 M propranolol, isoprenaline- and CGP-12177A (a β₃-ADR partial agonist)-induced relaxation was competitively inhibited by high concentrations of bupranolol (a β_1,2,3-ADR antagonist), with pA₂ values of 6.49 and 5.76, respectively. We detected the mRNA of β₁- and β₃-ADRs in endothelium-denuded SMAs. Treatment with 6-hydroxydopamine (a catecholaminergic neurotoxin) reduced maximal isoprenaline-induced relaxation in the presence and absence of 10^-7 M propranolol, but not CGP-12177A-induced relaxation.SIGNIFICANCEIsoprenaline-induced relaxation of rat SMAs is mediated by β₁- and β₃-ADRs. β-ADR-mediated relaxation of rat SMAs is shown to be attenuated by chemical sympathetic denervation. The differences in the effects of bupranolol and chemical sympathetic denervation on the responses to isoprenaline and CGP-12177A in rat SMAs might be explained by the possible presence of multiple β₃-ADRs with different pharmacological properties.

01 May 2019·Biological and Pharmaceutical BulletinQ4 · MEDICINE

Noradrenaline-Induced Relaxation of Urinary Bladder Smooth Muscle Is Primarily Triggered through the β3-Adrenoceptor in Rats

Q4 · MEDICINE

Article

Author: Suzuki, Serena ; Tanaka, Yoshio ; Yoneyama, Naoki ; Yamaki, Fumiko ; Shibata, Hiroko ; Obara, Keisuke ; Hamamatsu, Shoko ; Higai, Koji

β-Adrenoceptors are subclassified into 3 subtypes (β₁-β₃). Among these, β₃-adrenoceptors are present in various types of smooth muscle and are believed to play a role in relaxation responses of these muscles. β₃-Adrenoceptors are also present in urinary bladder smooth muscle (UBSM), although their expression varies depending on the animal species. To date, there has been little information available about the endogenous ligand that stimulates β₃-adrenoceptors to produce relaxation responses in UBSM. In this study, to determine whether noradrenaline is a ligand of UBSM β₃-adrenoceptors, noradrenaline-induced relaxation was analyzed pharmacologically using rat UBSM. We also assessed whether noradrenaline metabolites were ligands in UBSM. In isolated rat urinary bladder tissues, mRNAs for β₁-, β₂-, and β₃-adrenoceptors were detected using RT-PCR. In UBSM preparations contracted with methacholine (3 × 10^-5 M), noradrenaline-induced relaxation was not inhibited by the following antagonists: atenolol (10^-6 M; selective β₁-adrenoceptor antagonist), ICI-118,551 (3 × 10^-8 M; selective β₂-adrenoceptor antagonist), propranolol (10^-7 M; non-selective β-adrenoceptor antagonist), and bupranolol (10^-7 M; non-selective β-adrenoceptor antagonist). In the presence of propranolol (10^-6 M), noradrenaline-induced relaxation was competitively inhibited by bupranolol (3 × 10^-7-3 × 10^-6 M) or SR59230A (10^-7-10^-6 M; selective β₃-adrenoceptor antagonist), with their pA₂ values calculated to be 6.64 and 7.27, respectively. None of the six noradrenaline metabolites produced significant relaxation of methacholine-contracted UBSM. These findings suggest that noradrenaline, but not its metabolites, is a ligand for β₃-adrenoceptors to produce relaxation responses of UBSM in rats.

100 Deals associated with Bupranolol Hydrochloride

External Link

KEGG	Wiki	ATC	Drug Bank
D01454	Bupranolol Hydrochloride	C07AA19	DB08808

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Cardiovascular Diseases	-	-	-
Glaucoma	-	-	-

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