5-HT3 receptor antagonists(Serotonin 3 (5-HT3) receptor antagonists), κ opioid receptor antagonists(Kappa opioid receptor antagonists), μ opioid receptor agonists(Mu opioid receptor agonists)

Therapeutic Areas

Nervous System DiseasesOther Diseases

Active Indication-

Inactive Indication

Pain, PostoperativePostoperative Nausea and Vomiting

Originator Organization

Camurus AB

Active Organization-

Inactive Organization

Braeburn, Inc.

Camurus AB

Drug Highest PhasePendingPhase 1

First Approval Date-

Regulation-

Structure

Molecular FormulaC18H24N4O

InChIKeyMFWNKCLOYSRHCJ-BTTYYORXSA-N

CAS Registry109889-09-0

View All Structures (2)

100 Clinical Results associated with Buprenorphine Hydrochloride/Granisetron

100 Translational Medicine associated with Buprenorphine Hydrochloride/Granisetron

100 Patents (Medical) associated with Buprenorphine Hydrochloride/Granisetron

Literatures (Medical) associated with Buprenorphine Hydrochloride/Granisetron

01 Jan 1991·Annali dell'Istituto superiore di sanita

Steroid receptor assays: an Italian quality assessment program.

Review

Author: De Bortoli, M ; Catozzi, L ; Giganti, M ; Giovannini, G ; Piffanelli, A ; Pelizzola, D

An Italian Committee for the quality assessment of steroid receptor assay was instituted in 1979; the number of laboratories participating in this program increased from 7 in 1979 to 43 in 1989. The Italian program in collaboration with EORTC (European Organization Research and Treatment of Cancer) initiatives, utilizes as working standards lyophilized samples that tolerate prolonged storage at 4 degrees C. The national representatives agreed, according to EORTC, that all laboratories would perform, for measurement of steroid receptors, the dextran coated charcoal (DCC) method using the same concentration of radioactive ligands (3-H-estradiol, 3-H-ORG-2058) and would determine the non-specific binding with the same compounds (diethylstilbestrol and ORG-2058). The computation method is a potential source of interlaboratory variation; the multipoint Scatchard analysis, though difficult to apply for receptor problems, is the most widely used approach at present. The standardized DCC method is the most common and recognized (Food and Drug Administration) procedure for quantifying hormone receptor in human cancer. Since new technologies are being introduced (receptor enzyme immunoassay, EIA), adequate programs of quality assessment are required; in general, it has demonstrated an excellent correlation between radioligand binding assay (DCC) and immunochemical assay (EIA). Other prognostic factors, such as proteins produced by oncogenes and growth factors of the malignant cells have become more important. Some of these factors, as well as estrogen receptor status, seem the major determinants of recurrence after the first treatment.

01 Feb 1986·Journal of Steroid Biochemistry

Evidence that a non-aromatizable metabolite of norethisterone induces estrogen-dependent pituitary progestin receptors

Article

Author: Gregorio Pérez-Palacios ; Ana E. Pèrez ; Gustavo A. García ; Bertha Ch́avez ; Arturo Angeles ; Felipe Vilchis

Neutral reduced metabolites of norethisterone (NET) specifically interact with intracellular estrogen receptors in target organs. To determine if this interaction can effectively initiate estrogen-dependent cellular responses, the effects of an A-ring-reduced NET derivative upon the induction of cytosol-located pituitary progestin receptors (PR) and uterine growth were studied in adult castrated female rats. Different doses of 17 alpha-ethynyl-5 alpha-estran-3 beta, 17 beta-diol (3 beta, 5 alpha-NET) were s.c. administered to ovariectomized animals for 6 days. 17 beta-Estradiol (E2) and oil-treated rats served as experimental controls. Pituitary PR were labeled in vitro by a post-gradient technique using [3H]ORG-2058 as the ligand. PR binding specificity was determined by the use of an excess of radioinert steroids. The results demonstrated that administration of 3 beta, 5 alpha-NET induced specific 8-9S pituitary cytosol PR in a dose-dependent manner. Binding properties of the 3 beta, 5 alpha-NET-induced progestin binding sites (Kd = 1.0 X 10(-9) M; NBS = 1.2 X 10(-9) M) appear indistinguishable from those induced by E2. In addition, 3 beta, 5 alpha-NET administration resulted in a significant increase in uterine weight at the expense of myometrium and endometrium growth in a similar fashion to that observed in the E2-treated group. When 3 alpha, 5 alpha-epimeric alcohol (3 alpha, 5 alpha-NET) was administered, induction of pituitary PR and uterine growth were also observed although to a lesser extent. Inasmuch as the results demonstrate that neutral non-aromatizable NET metabolites induce biochemical and morphological estrogenic responses, they offer an alternative explanation for the mechanism of estrogen-like action of this synthetic contraceptive progestin.

100 Deals associated with Buprenorphine Hydrochloride/Granisetron

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Pain, Postoperative	Preclinical	-	Braeburn, Inc.	-
Pain, Postoperative	Preclinical	SE	Camurus AB	-
Postoperative Nausea and Vomiting	Preclinical	-	Braeburn, Inc.	-
Postoperative Nausea and Vomiting	Discovery	SE	Camurus AB	-

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Buprenorphine Hydrochloride/Granisetron

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