scholarly journals Repeated subcutaneous administration of PT150 has dose-dependent effects on sign tracking in male Japanese quail.

2019 ◽  
Vol 27 (6) ◽  
pp. 515-521 ◽  
Author(s):  
Beth Ann Rice ◽  
Meredith A. Saunders ◽  
Julia E. Jagielo-Miller ◽  
Mark A. Prendergast ◽  
Chana K. Akins
Keyword(s):  
Japanese Quail ◽  
Subcutaneous Administration ◽  
Sign Tracking ◽  
Dose Dependent

Anticoagulant Activity of Hirulog™, a Direct Thrombin Inhibitor, in Humans

1993 ◽  
Vol 69 (02) ◽  
pp. 157-163 ◽  
Author(s):  
Irving Fox ◽  
Adrian Dawson ◽  
Peter Loynds ◽  
Jane Eisner ◽  
Kathleen Findlen ◽  
...  
Keyword(s):  
Rational Design ◽  
Therapeutic Potential ◽  
Anticoagulant Activity ◽  
Subcutaneous Administration ◽  
Direct Thrombin Inhibitor ◽  
Controlled Study ◽  
Thrombin Inhibitor ◽  
Thrombin Time ◽  
Thrombotic Disease ◽  
Dose Dependent

SummaryHirulog™ (BG8967) is a direct thrombin inhibitor built by rational design using the protein hirudin as a model (Maraganore et al. [1990]; Biochemistry 29: 7095–101). In order to evaluate the therapeutic potential for hirulog in the management of thrombotic disease, the tolerability and anticoagulant activity of the agent were examined in a study of human volunteers.In a randomized, placebo-controlled study (n = 54), the intravenous infusion of hirulog over 15 min showed a rapid, dose-dependent prolongation of activated partial thromboplastin time (APTT), prothrombin time (PT), and thrombin time (TT). There was a corresponding dose-dependent increase in plasma hirulog levels. The peptide was rapidly cleared with a half-life of 36 min and a total body clearance rate for the peptide of 0.43 1 kg−1 h−1. Similar activity was observed following subcutaneous injection but with sustained pharmacodynamic and pharmacokinetic behavior. There was a significant correlation between pharmacokinetic and pharmacodynamic variables for both intravenous (r = 0.8, p <0.001) and subcutaneous administration (r = 0.7, p = 0.002).To evaluate the possible interactions of aspirin on the tolerability and anticoagulant activity of intravenous hirulog, a cross-over design was employed in eight subjects. Aspirin administration did not modify the peptide’s activity. At the administered dose of 0.6 mg kg−1 h−1 for 2 h, hirulog infusion prolonged APTT from 230 to 260% baseline. The infusion of hirulog in subjects who had received aspirin was not associated with any significant changes in the template bleeding time.The final phase of the study examined the activity and tolerability of hirulog in ten subjects during prolonged intravenous infusions for up to 24 h. The peptide (0.3 mg kg−1 h−1) exhibited sustained anticoagulant activity with no evidence for a cumulative effect. During hirulog infusion, APTT was prolonged from 210 to 250% baseline.In all phases of the study, hirulog administration was generally well-tolerated.Our observations show that hirulog is an active antithrombin agent with excellent tolerability in humans. As a direct thrombin inhibitor, hirulog provides a novel approach for the management of thrombotic disease.

Effect of Low-Molecular-Weight Heparin (Tinzaparin) and Unfractionated Heparin on Platelet Aggregation

1996 ◽  
Vol 2 (3) ◽  
pp. 209-212 ◽  
Author(s):  
Hanne B. Ravn ◽  
Claus Bregengaard ◽  
Henrik Vissinger ◽  
Per Østergaard ◽  
Jan Holst ◽  
...  
Keyword(s):  
Molecular Weight ◽  
Platelet Aggregation ◽  
Unfractionated Heparin ◽  
Low Molecular Weight Heparin ◽  
Ex Vivo ◽  
Subcutaneous Administration ◽  
Low Molecular Weight ◽  
Pronounced Difference ◽  
Dose Dependent

A low-molecular-weight heparin (LMWH), when anti-IIa activity was compared. In the ex vivo part Tinzaparin, was compared with unfractionated heparin of the study, a significant enhancement of ADP-induced (UFH) for their effects on platelet aggregation in vitro and platelet aggregation was observed after i.v. administra ex vivo. Both heparins showed a dose-dependent proag- tion of both Tinzaparin and UFH with no difference in gregatory effect on ADP- and collagen-induced platelet potency. Subcutaneous administration of Tinzaparin in aggregation in vitro, but LMWH was less potent. The two different doses did not have any effect on platelet differences in potency between Tinzaparin and UFH de- activity. In conclusion, Tinzaparin appears, like other pended on how the compounds were compared. The most LMWHs, to have less proaggregatory effect on platelets pronounced difference was found when molar concentra- than UFH both in vitro and ex vivo.

LUTEINIZING HORMONE RELEASING FACTOR IN THE QUAIL HYPOTHALAMUS

1972 ◽  
Vol 53 (1) ◽  
pp. 131-138 ◽  
Author(s):  
P. M. SMITH ◽  
B. K. FOLLETT
Keyword(s):  
Luteinizing Hormone ◽  
Japanese Quail ◽  
Release Rate ◽  
Initial Period ◽  
Repetitive Stimulation ◽  
Pituitary Glands ◽  
Lh Release ◽  
A Minor ◽  
Dose Dependent ◽  
Stimulation Of

SUMMARY Pituitaries from Japanese quail were superfused continuously for up to 12 h and the luteinizing hormone (LH) in the superfusate was measured by radioimmunoassay. After an initial period the release rate remained low and relatively constant. The introduction of hypothalamic extracts prepared from quail substantially increased immunoreactive LH release. The responses were dose-dependent. Cortical extracts caused a minor but significant response. Dopamine was inactive in the system. The technique is attractive because it allows for repetitive stimulation of the same pituitary glands with treatments being administered every 30–45 min.

scholarly journals BLACK TEA INFUSION AMELIORATES ENZYMATIC CHANGES INDUCED BY SUBCUTANEOUS EXPOSURE OF GASOLINE AND GM-10 IN MICE

2015 ◽  
Vol 3 (9SE) ◽  
pp. 1-5
Author(s):  
Manjeet Dave ◽  
Ramtej Jayram Verma
Keyword(s):  
Low Dose ◽  
Succinic Dehydrogenase ◽  
Subcutaneous Administration ◽  
Black Tea ◽  
High Dose ◽  
Tea Infusion ◽  
Ameliorative Effect ◽  
Cervical Dislocation ◽  
Enzymatic Changes ◽  
Dose Dependent

The present study was carried out to examine the ameliorative effect of black tea infusion on gasoline and GM-10 induced enzymatic changes in kidney of mice. Eighty healthy adult Swiss strain male albino mice weighing 32-35 gm were divided into eight groups including untreated control and various treated groups. Treated groups were subcutaneously administered with gasoline (412 mg/kg/day) and GM-10 low dose (206 mg/kg/day) and high dose (412 mg/kg/day) for 30 days. Black tea infusion (2%) was orally administered alone and along with gasoline and GM-10 through drinking water. All experimental animals were sacrificed on 31st day by cervical dislocation; kidney were isolated and used. Activities of succinic dehydrogenase, adenosine triphosphatase, acid phosphatase and alkaline phosphatase were assayed in kidney.The results revealed that subcutaneous administration of gasoline and GM-10 caused dose-dependent, significant enzymatic alterations in kidney of mice. Oral administration of black tea infusion along with subcutaneous treatment with gasoline and GM-10 significantly ameliorates all enzymatic changes induced by gasoline and GM-10 in kidney of mice.

scholarly journals Reproductive Organ Activities of Morinda lucida Ethanol Root Extract on Male and Female Albino Rats Tramadol HCL Induced Infertility

2021 ◽  
pp. 287-295
Author(s):  
Nkiruka Millicent Amadi ◽  
Peter Uwadiegwu Achukwu ◽  
Nonyelum V. Anoh ◽  
Emmanuel Ifeanyi Obeagu ◽  
Ngozika O. Achukwu ◽  
...  
Keyword(s):  
Body Weight ◽  
Subcutaneous Administration ◽  
Reproductive Organ ◽  
Organ Weight ◽  
Albino Rats ◽  
Root Extract ◽  
Testicular Damage ◽  
Male And Female ◽  
Testicular Cells ◽  
Dose Dependent

Infertility is a serious issue disturbing reproductive ages in all society now and calling for solution for continuity. Infertility were induced on groups of animals with separate sexes; M, M1, M2 and M3; F, F1, F2 andF3 with daily subcutaneous administration of 20 mg/kg body weight tramadol HCl for 42 days before respective ethanol root extract administrations of (500, 1000, 1500) mg/ kg body weight for 10 days. The animals were anaesthetized and sacrificed; uterus, ovaries, testes, epididymis were dissected out for histomorphological studies. There is evidence of dose treatment of infertility among treated groups. From the organ weight study, both the male and the female organ weight in the groups remained significantly unchanged. There are dose dependent treatments with the male and female tramadol treatment. The result is more pronounced in the increased dose of ethanol root extract (1000 mg/kg and 1500 mg/ kg) body weight treated testicular cells. This study indicated that Morinda lucida has a prophylactic effect against tramadol-induced testicular damage.

scholarly journals Antifungal Activities of R-135853, a Sordarin Derivative, in Experimental Candidiasis in Mice

2005 ◽  
Vol 49 (1) ◽  
pp. 52-56 ◽  
Author(s):  
Yasuki Kamai ◽  
Masayo Kakuta ◽  
Takahiro Shibayama ◽  
Takashi Fukuoka ◽  
Shogo Kuwahara
Keyword(s):  
Subcutaneous Administration ◽  
Viable Cell ◽  
Cell Counts ◽  
Single Oral Administration ◽  
Fluconazole Resistant ◽  
Resistant Strains ◽  
Mucosal Candidiasis ◽  
Dose Dependent

ABSTRACT The activities of R-135853, a novel sordarin derivative that possesses a 1,4-oxazepane ring moiety, were evaluated in vitro and in vivo. R-135853 exhibited potent in vitro activities against Candida albicans (fluconazole-susceptible strains), Candida glabrata, Candida tropicalis, and Cryptococcus neoformans, with MICs at which 90% of isolates were inhibited of 0.03, 1, 0.5, and 0.5 μg/ml, respectively. R-135853 also exhibited potent activities against fluconazole-susceptible dose-dependent and fluconazole-resistant strains of C. albicans, with MICs ranging from 0.03 to 0.06 μg/ml. However, R-135853 exhibited weak or no activity against Candida parapsilosis, Candida krusei, and Aspergillus spp. R-135853 exhibited dose-dependent efficacy against experimental murine hematogenous candidiasis induced by C. albicans when it was administered by both the subcutaneous and the oral routes and reduced viable cell counts in the kidneys significantly when it was administered at 50 mg/kg of body weight/dose (administration three times a day). In this model, R-135853 also exhibited dose-dependent efficacy by single oral administration. Subcutaneous administration of R-135853 exhibited dose-dependent efficacy against experimental murine esophageal candidiasis induced by fluconazole-resistant C. albicans, against which fluconazole at 50 mg/kg/dose was ineffective, and reduced viable cell counts in the esophagus significantly when it was administered at 10 and 50 mg/kg/dose. R-135853 eradicated C. albicans from the esophagi of one and four of five mice when it was administered at 10 and 50 mg/kg/dose, respectively. These results suggest that R-135853 is promising for the treatment of disseminated or mucosal candidiasis, including fluconazole-refractory infections.

scholarly journals Noradrenergic alpha-2A receptor activation suppresses courtship vocalization in male Japanese quail.

2021 ◽  
Author(s):  
Yasuko Tobari ◽  
Ami Masuzawa ◽  
Norika Harada ◽  
Kenta Suzuki ◽  
Simone Meddle
Keyword(s):  
Japanese Quail ◽  
High Frequency ◽  
Adrenergic Receptor ◽  
Receptor Activation ◽  
Early Gene ◽  
Intracerebroventricular Injection ◽  
Receptor Mrna ◽  
Noradrenergic Innervation ◽  
Dose Dependent ◽  
Stimulation Of

Male Japanese quail produce high-frequency crow vocalizations to attract females during the breeding season. The nucleus of intercollicularis (ICo) is the midbrain vocal center in birds and electrical stimulation of the ICo produces calls that include crowing. Noradrenaline plays a significant role in sexual behavior but the contribution of noradrenaline in the control of courtship vocalizations in quail has not been well established. Using dose-dependent intracerebroventricular injection of clonidine, an α2-adrenergic receptor-specific agonist, crowing vocalization was immediately suppressed. At the same time as crow suppression by clonidine there was a reduction of immediate early gene, zenk mRNA, in the ICo; no zenk mRNA expression was detected in the dorsomedial division of the nucleus. Using histochemistry, we determined that the ICo receives noradrenergic innervation and expresses α2A-adrenergic receptor mRNA. Taken together, these data suggest that noradrenaline regulates courtship vocalization in quail, possibly via the alpha2A-adrenergic receptor expressed on ICo neurons.

Sign tracking in Japanese quail: How far will they go?

1997 ◽  
Author(s):  
Melissa Burns Hamilton ◽  
Michael Domjan
Keyword(s):  
Japanese Quail ◽  
Sign Tracking

scholarly journals Prolonged Stimulation of Growth Hormone (GH) and Insulin-Like Growth Factor I Secretion by CJC-1295, a Long-Acting Analog of GH-Releasing Hormone, in Healthy Adults

2006 ◽  
Vol 91 (3) ◽  
pp. 799-805 ◽  
Author(s):  
Sam L. Teichman ◽  
Ann Neale ◽  
Betty Lawrence ◽  
Catherine Gagnon ◽  
Jean-Paul Castaigne ◽  
...  
Keyword(s):  
Outcome Measures ◽  
Subcutaneous Administration ◽  
Cumulative Effect ◽  
Healthy Adults ◽  
Pharmacokinetic Parameters ◽  
Double Blind ◽  
Duration Of Action ◽  
Igf I ◽  
Long Acting ◽  
Dose Dependent

Abstract Context: Therapeutic use of GHRH to enhance GH secretion is limited by its short duration of action. Objective: The objective of this study was to examine the pharmacokinetic profile, pharmacodynamic effects, and safety of CJC-1295, a long-acting GHRH analog. Design: The study design was two randomized, placebo-controlled, double-blind, ascending dose trials with durations of 28 and 49 d. Setting: The study was performed at two investigational sites. Participants: Healthy subjects, ages 21–61 yr, were studied. Interventions: CJC-1295 or placebo was administered sc in one of four ascending single doses in the first study and in two or three weekly or biweekly doses in the second study. Main Outcome Measures: The main outcome measures were peak concentrations and area under the curve of GH and IGF-I; standard pharmacokinetic parameters were used for CJC-1295. Results: After a single injection of CJC-1295, there were dose-dependent increases in mean plasma GH concentrations by 2- to 10-fold for 6 d or more and in mean plasma IGF-I concentrations by 1.5- to 3-fold for 9–11 d. The estimated half-life of CJC-1295 was 5.8–8.1 d. After multiple CJC-1295 doses, mean IGF-I levels remained above baseline for up to 28 d. No serious adverse reactions were reported. Conclusions: Subcutaneous administration of CJC-1295 resulted in sustained, dose-dependent increases in GH and IGF-I levels in healthy adults and was safe and relatively well tolerated, particularly at doses of 30 or 60 μg/kg. There was evidence of a cumulative effect after multiple doses. These data support the potential utility of CJC-1295 as a therapeutic agent.

Tolerance and Biological Activity of Pentosan Polysulfate After Intramuscular or Subcutaneous Administration for Ten Days in Human Volunteers

1986 ◽  
Vol 55 (01) ◽  
pp. 086-089 ◽  
Author(s):  
P Sié ◽  
J L Albarede ◽  
M Robert ◽  
C Bouloux ◽  
J Lansen ◽  
...  
Keyword(s):  
Pharmacological Activity ◽  
Subcutaneous Administration ◽  
Daily Injection ◽  
Pentosan Polysulfate ◽  
Drug Injection ◽  
Group I ◽  
Human Volunteers ◽  
The Mean ◽  
Serial Samples ◽  
Dose Dependent

SummaryThis study reports on the tolerance and the pharmacological activity of pentosan polysulfate (PPS) administered to healthy volunteers for 10 days. Three groups of 10 subjects received either one daily injections of 100 mg of PPS by I. M. route (group I), or two daily injection of 50 mg of PPS by I. M. or S. C. route (groups II and III, respectively). In each group two random subjects received a placebo for the 10 days; on day 0, each subject was injected by a placebo. Clinical tolerance was checked by a daily physical examination; biological tolerance was assessed comparing the results of the main biochemical and haematological constants measured before starting the treatment (day 0) and 12 or 24 h after the end of the treatment (day 11). The pharmacological activity was measured on serial samples taken before treatment and between 1 and 6 h after the drug injection on days 1, 3 and 10; the results were compared to those obtained on day 0. Clinical tolerance was good. The biological side effects concern the transaminase levels and the platelet counts. An increase above the upper normal limit was observed in 18/i4 and 3/24 for alanine and aspartic transaminase respectively. The mean platelet reduction ranged between 24 and 34% according to the groups. The drug injection induced a slight Quick time (PT) prolongation, no significant alteration of factors II, VII-X, V levels and of thrombin clotting time. The activated partial thromboplastin time (APTT) was significantly prolonged and there was a weak but significant circulating anti-Xa activity. The fibrinolytic activity was enhanced without increase in the tissue plasminogen activator antigen level. These pharmacological effects were at their maximum between 2 and 4 h after the drug injection and returned to the pre-injection equilibrium between 4 and 6 h except for circulating anti-Xa activity; these effects remained unchanged all over the 10-day therapeutic period. The comparison between group I and II indicates that the PT and APTT effects are dose-dependent while the anti-Xa and the profibrinolytic effects are not; the comparison between group II and III indicates that the S. C. and I. M. route are bioequivalent.

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