• 제목/요약/키워드: A3 agonist

검색결과 496건 처리시간 0.029초

Comparison of follitropin ${\beta}$ administered by a pen device with follitropin ${\beta}$ administered by a conventional syringe in patients undergoing IVF-ET

  • Kang, Hyuk-Jae;Kim, Chung-Hoon;Ahn, Jun-Woo;Lee, Hyang-Ah;Kim, Sung-Hoon;Chae, Hee-Dong;Kang, Byung-Moon
    • Clinical and Experimental Reproductive Medicine
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    • 제38권1호
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    • pp.37-41
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    • 2011
  • Objective: To compare the effectiveness and convenience of a pen device for the self-administration of follitropin ${\beta}$ with a conventional syringe delivering follitropin ${\beta}$ solution in patients undergoing IVF-ET. Methods: GnRH agonist long protocol was used for controlled ovarian stimulation (COS) in all subjects. A total of 100 patients were randomized into the pen device group or the conventional syringe group on the first day of COS. Local tolerance reactions were assessed within 5 minutes, at 1 hour and at 3 hours after each injection. On the day of hCG injection, patients were asked to rate their overall pain and convenience experienced with self-injection on a visual anlaogue scale (VAS). Results: There were no differences in patients' characteristics between the two groups. The duration of COS was significantly shorter in the pen device group than in the conventional syringe group. Patients included in the pen device group needed a significantly smaller amount of follitropin ${\beta}$. However, no differences between the two groups were found in IVF results and pregnancy outcome. The incidence of local pain within 5 minutes, at 1 hour and at 3 hours after the injection was significantly lower in the pen device group. VAS scores indicated that injections using the pen device were significantly less painful and more convenient. Conclusion: The pen device for self-administration of follitropin ${\beta}$ is less painful, safer and more convenient for the patients, and can be more effective because of the shorter duration and smaller dose of follitropin ${\beta}$ when compared with the conventional syringe.

신장기능의 중추 Dopamine성 조절에 미치는 Yohimbine의 영향 (Influence of Yohimbine on the Central Dopaminergic Regulation of Renal Function)

  • 국영종;김경근;조강선;민병갑
    • 대한약리학회지
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    • 제22권2호
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    • pp.79-87
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    • 1986
  • 중추 dopamine(DA)계가 신장기능 조절에 관여하고 있으며 뇌실내로 DA를 투여하면 norepinephrine(NE)처럼 항이뇨와 항Na 배설을 초래함이 보고된 바 있고, 중추 DA작용에 있어서 adrenergic system이 관여한다는 많은 시사가 있다. 따라서 본 연구에서는alpha-2 adrenocopter 차단제인 yohimbine이 측뇌실내 DA의 신장작용에 어떠한 영향을 미치는가를 관찰하였다. Yohimbine $100\;{\mu}g/kg$을 가토측뇌실내로 투여시(icv) 신혈류 및 사구체 여과율의 감소와 함께 현저한 항이뇨 및 Na 배설감소를 초래하였으며, DA $15\;{\mu}g/kg$ icv 역시 항이뇨를 초래하였으나 yohimbine 전 처치후에는 뇨량 및 Na배설의 증가를 초래하였다. 양을 더올려 $150\;{\mu}g/kg$의 DA를 yohimbine 전처치 가토에 투여하면 3배 이상의 Na배설 증가와 함께 현저한 이뇨작용이 나타났으며 이 작용은 약 20분간 지속되었다. 이때 신혈류 역학은 일부 개선되었다. 다른 DA agonist인 apomorphine은 $100\;{\mu}g/kg$ icv로 현저한 이뇨와 Na 배설증가를 나타내며 신혈류역학도 개선하였으나, yohimbine은 이같은 apomoiphine작용을 차단하지 못하였다. NE $10\;{\mu}g/kg$ icv도 항이뇨 작용을 나타냈으나 yohimbine 전처치에 의하여 차단되지 아니하였다. 이 연구결과로, 중추 DA의 신장작용은 NE처럼 단순하지 않고, 이뇨작용은 신혈류역학의 감퇴에 기인한 항이노작용에 의해 은폐되어 있으며, yohimbine은 DA의 항이뇨작용은 차단하나 이뇨작용에는 영향을 미치지 못하며, DA의 항이뇨작용이 지양될때에만 이뇨작용이 발현됨을 알 수 있었다. 또한 중추를 통한 DA의 신장작용에는 adrenergic system이 관여하지 않은 것으로 보인다.

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가토(家兎) 및 Rat에서 Norepinephrine, Phenylephrine 및 Clonidine의 승압반응(昇壓反應)에 대한 Verapamil의 영향(影響) (Effects of Verapamil on Norepinephrine-, Phenylephrine- and Clonidine-induced Pressor Response in Rabbits and Rats)

  • 신동호;최수형
    • 대한수의학회지
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    • 제28권1호
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    • pp.29-36
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    • 1988
  • To examine the selectivity of verapamil, used in the cardiovascular diseases, on alpha-1 and alpha-2 adrenoceptor-induced pressor rsponses, effects of verapamil on alpha-adrenoceptor agonist-induced pressor responses were investigated in urethane-anesthetized rabbits, spinal rabbits, rats and pithed rats. To evaluate the effects of verapamil on each pressor response induced by norepinephrine, phenylephrine and clonidine, these agonists were previously injected into a ear vein, and then same procedures were performed 1~2 min after treatment with intravenous verapamil. The results are summarized as follows: 1. Intravenous verapamil produced dose-dependent depressor response in rabbits and rats. 2. Pressor responses to intravenous norepinephrine($10{\mu}g/kg$) and phenylphrine($30{\mu}g/kg$) were inhibited by pretreatment with intravenous verapamil in rabbits and no difference was noted between the degree of both inhibitions of the pressor response by verapamil. 3. Pressor responses to intravenous norepinephrine($3{\mu}g/kg$), phenylephrine($20{\mu}g/kg$) and clonidine ($300{\mu}g/kg$) were inhibited by pretreatment with intravenous verapamil in spinal rabbits. No difference was noted between the inhibition of norepinephrine-induced pressor response and that of phenylephrine-induced pressor response by verapamil. The inhibition of clonidine-induced pressor response by verapamil was more prominent than that of norepinephrine- or phenylephrine-induced pressor response. 4. Pressor responses to intravenous norepinephrine($3{\mu}g/kg$) and phenylephrine($10{\mu}g/kg$) were inhibited by pretreatment with intravenous verapairlil in rats and no difference was noted between the degree of both inhibitions of the pressor response by verapamil. 5. Pressor responses to intravenous norepinephrine ($3{\mu}g/kg$), phenylephrine($30{\mu}g/kg$) and clonidine($100{\mu}g/kg$) were inhibited by pretreatment with intravenous verapamil in pithed rats. No difference was noted between the inhibition of norepinephrine-induced pressor response and that of phenylephrine-induced pressor response by verapamil. The inhibition of clonidine-induced pressor response by verapamil was more prominent than that of norepinephrine- or phenylephrine-induced pressor response. These results suggest that verapamil significantly inhibits both pressor responses mediated by alpha-1 and alpha-2 adrenoceptors and the inhibition is greater in alpha-2 adrenoceptor-induced response than in alpha-1 adrenoceptor-induced one, and calcium channel takes part in the process of the pressor response mediated by alpha-1 adrenoceptors as well as alpha-2 adrenoceptors.

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Seven-Day Continuous Abstinence Rate from Smoking at 1, 2, or 3 Years after the Use of Varenicline

  • Kim, Jin Se;Jang, Ju Young;Park, Eun Hye;Lee, Joo Young;Gu, Kang Mo;Jung, Jae Woo;Choi, Jae Chol;Shin, Jong Wook;Park, In Won;Choi, Byoung Whui;Kim, Jae Yeol
    • Tuberculosis and Respiratory Diseases
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    • 제78권2호
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    • pp.92-98
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    • 2015
  • Background: Varenicline, a selective partial agonist/antagonist of the ${\alpha}4{\beta}2$ nicotinic receptor, has proven effectiveness for smoking cessation by several randomized, controlled trials. Because few studies have evaluated the long-term efficacy of varenicline, we tried to evaluate the smoking status of varenicline users up to 3 years after the initial prescription of the drug. Methods: We interviewed varenicline users who were prescribed the drug from June 2007 to May 2010 by telephone, from June 2010 to May 2011. Results: One-hundred and thirty-three of 250 varenicline users (53.2%) were available for the survey. Seven-day continuous abstinence from smoking was adhered to by 17 of 39 respondents (43.6%) at 1 year, and 11 of 36 (30.6%) and 19 of 58 (32.8%) at 2 and 3 years since the first use of varenicline, respectively. Compared to current smokers, successful quitters were older (55.0 years vs. 49.9 years, p=0.01), had better compliance to the 12-week course (27.7 vs. 9.3%, p=0.01), and had taken varenicline longer (10.1 vs. 5.9 weeks, p=0.01). Fifty-four of 71 current smokers (76.1%) were willing to stop smoking in the near future. The preferred ways to cease smoking were will-power (48.1%), varenicline (25.9%), nicotine replacement therapy (11.1%), and others (14.9%). Conclusion: Smokers should be encouraged to stick to the proven way for recommended period of time for successful cessation of smoking.

Morphine과 Buprenorphine의 지속적 정주에 의한 술후 통증 억제효과의 비교 (Effects of Morphine and Buprenorphine Intravenous Infusion for Postoperative Pain)

  • 백선기;소상윤;한영진;최훈
    • The Korean Journal of Pain
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    • 제7권1호
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    • pp.78-83
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    • 1994
  • 수술후 통증치료에 morphine과 buprenorphine의 효과를 알아보기 위하여 morphine과 buprenorphinec을 단독 투여하거나(1, 2군) buprenorphine과 ketorolac을 반량씩 혼합하여 지속적으로 정주(3군)하여 다음과 같은 결과를 얻었다. 1) 각군에서 모두 혈압과 맥박의 의의있는 변화는 초래하지 않았다. 2) Visual analogue scale으로 평가한 진통 발현은 각군에서 모두 비슷하였다. 3) Visual analogue scale과 Prince Henry Scale로 평가한 진통효과는 morphine군에서 가장 우수하였고, buprenorphine군과 buprenorphine+ketorolac의 반량 투여군에서는 비슷하였다. 4) 부작용의 발생은 1군과 2군에서 비슷하였으나 3군에서 가장 낮았다. 이상의 결과로 보아 지속적 정주에 의한 술후 통증의 억제에 있어서 buprenorphine은 morphine을 대치할 수는 있으나 morphine보다 우수하지는 못한 것으로 사료되며, buprenorphine 사용시는 ketorolac을 병용하여 사용량을 줄염으로써 부작용을 줄일 수 있을 것으로 사료된다.

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천식 환자에서 $M_2$ 무스카린성 수용체 기능에 관한 연구 (Function of the Neuronal $M_2$ Muscarinic Receptor in Asthmatic Patients)

  • 권영환;이상엽;박상면;이신형;신철;조재연;심재정;강경호;유세화;인광호
    • Tuberculosis and Respiratory Diseases
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    • 제49권4호
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    • pp.486-494
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    • 2000
  • 연구배경 : 부교감 신경의 자극에 의해 유발된 기관지 수축은 $M_2$ 무스카린성 수용체(muscarinic receptors)에 의해 억제된다. 기관지 과민성을 유발시킨 동물 모델에서는 아세틸콜린 분비를 억제하는 $M_2$ 무스카린성 수용체 기능이 손상되어 아세틸콜린의 분비가 증가되고, 이로 인해 기관지 과민성을 나타낸다. 본 연구에서는 경증, 중등증, 중증 천식 환자를 대상으로 $M_2$ 무스카린성 수용체 기능 이상이 있는지 여부와 천식의 중증도에 따라 $M_2$ 무스카린성 수용체 기능에 차이가 있는지를 알아보고자 연구를 시행하였다. 대상 및 방법 : 고려대학교 안암병원 내과에서 천식으로 진단 받은 27명을 대상으로 하였다. 이 중 경증 천식이 11명, 중등증 천식이 8명, 중증 천식 8명이었다. 천식 발작이 있거나, 2주 이내에 상기도 감염이 있는 환자, 메타콜린 유발 검사에서 음성($PC_{20}{\geq}$16mg/ml)인 환자는 제외하였다. 대상 환자들은 메타콜린 유발 검사를 시행하여 $PC_{20}$을 구하고, 1주일 후에 $M_2$ 무스카린성 수용체 촉진제(agonist) 인 필로카핀(pilocarpine) $180{\mu}g$을 흡입한 후 1차 때와 같은 방법으로 $PC_{20}$을 구해 두 값을 비교하였다. 결과 : 대상 환자의 평균 연령은 39.3$\pm$12.3세였다. 천식의 중증도에 따라 결과를 분석해 보면 경증 천식 환자는 필로카핀 흡입 전 $PC_{20}$은 5.30$\pm$5.23mg/ml(평균$\pm$표준편차)에서 필로카핀 흡입 후 20.82$\pm$22.56mg/ml이었으며(p=0.004), 중등증 천식 환자는 필로카핀 흡입 전 $PC_{20}$은 2.79$\pm$1.51mg/ml에서 필로카핀 흡입 후 4.67$\pm$3.53mg/ml(p=0.012)로 유의하게 증가하였다. 이는 필로카핀에 대한 $M_2$ 무스카린성 수용체 기능이 정상임을 말해준다. 그러나 중증 천식 환자는 필로카핀 흡입 전 $PC_{20}$은 1.76$\pm$1.50mg/ml에서 필로카핀 흡입 후 3.18$\pm$4.03mg/ml(p=0.161)로 필로카핀 흡입 후에 통계적으로 유의한 차이가 없었다. 이는 중증 천식에서는$M_2$ 무스카린성 수용체 기능 이상이 있음을 말해준다. 결론 : 경증, 중등증, 중증을 대상으로 $M_2$ 무스카린성 수용체 기능을 조사해본 결과 경증과 중등증 천식에서는 $M_2$ 무스카린성 수용체 기능 이상이 없었고, 중증 천식에서는 $M_2$ 무스카린성 수용체 기능 이상이 있었다. 이는 천식의 중증도에 따라 $M_2$ 무스카린성 수용체 기능에 차이가 있음을 말해준다.

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흰쥐 해마에서 Acetylcholine 유리에 미치는 $N^6-Cyclopentyladenosine$ 및 Forskolin의 영향 (Interaction of Forskolin with the Effect of $N^6-Cyclopentyladenosine$ on $[^3H]-Acetylcholine$ Release in Rat Hippocampus)

  • 최봉규;박희만;강연욱;국영종
    • 대한약리학회지
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    • 제28권2호
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    • pp.129-136
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    • 1992
  • 흰쥐 해마(hippocampus)에서 acetylcholine(Ach) 유리에 미치는 $A_1-adenosine$ 수용체의 역할과 post-receptor 기전에 있어서 adenylate cyclase 계의 관여여부에 관한 지견을 얻고자 하여 $[^3H]-choline$으로 평형시킨 해마 slice를 사용하여 $[^3H]-ACh$ 유리에 미치는 여러가지 약물들의 영향을 관찰하였다. $A_1-adenosine$ 수용체 흥분제인 $N^6-cyclopentyladenosine(CPA,\;0.1{\sim}10\;{\mu}M)$은 전기자극$(3Hz,\;5\;Vcm^{-1},\;2\;ms,\;rectangular\;pulses)$에 의한 $[^3H]-ACh$ 유리를 용량 의존적으로 감소시켰다. $A_1-adenosine$ 수용체 차단제인 8-cyclopentyl-1, 3-dipropylxanthine$(DPCPX,\;1{\sim}10\;{\mu}M)$은 용량 의존적으로 $[^3H]-ACh$ 유리를 증가시켰으며, 이때 기저(basal)유리 또한 증가됨을 관찰할 수 있었고, $2\;{\mu}M$ DPCPX 전처리는 CPA의 효과를 길항하여 CPA에 의한 용량반응곡선을 우측으로 이동시킴을 볼 수 있었다. G protein 억제제인 N-ethylmaleimide$(NEM,\;10\;&\;30\;{\mu}M)$는 그 자체에 의하여 자극에 의한 ACh 유리를 증가시켰으며, 기저유리 또한 증가함을 볼 수 있었다. NEM 전처리에 의하여 CPA의 효과는 완전히 소실되었다. 한편 adenylate cyclase 활성화제인 forskolin$(0.3{\sim}10\;{\mu}M)$은 기저유리에 변함없이 용량의존적인 $[^3H]-ACh$ 유리의 증가를 초래하였으며 $3\;{\mu}M$ forskolin 전처리는 대량$(10\;{\mu}M)$의 CPA의 효과를 제외하고는 CPA의 효과를 억제시킴을 관찰할 수 있었다. 이상의 실험 결과로 흰쥐 해마의 choline 작동성신경의 presynaptic $A_1-adenosine$ heteroreceptor는 ACh 유리에 중요한 역할을 하고 있으며, ACh 유리의 조절에 Gi-단백질을 통한 adenylate cyclase 계의 관여가 확실하다 하겠다.

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Effect of Pioglitazone on Production of Regulated upon Activation Normal T-cell Expressed and Secreted (RANTES) and IVF Outcomes in Infertile Women with Endometriosis

  • Kim, Chung-Hoon;Lee, You-Jeong;Kim, Jun-Bum;Lee, Kyung-Hee;Kwon, Su-Kyung;Ahn, Jun-Woo;Kim, Sung-Hoon;Chae, Hee-Dong;Kang, Byung-Moon
    • 한국발생생물학회지:발생과생식
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    • 제17권3호
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    • pp.207-213
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    • 2013
  • This study was performed to investigate the effect of peroxisome proliferators activated receptor-${\gamma}$ (PPAR-${\gamma}$) ligand, pioglitazone, on production of regulated upon activation normal T-cell expressed and secreted (RANTES) and in vitro fertilization (IVF) outcome in infertile patients with endometriosis. Sixty-four infertile patients with stage III or IV endometriosis undergoing IVF were randomly allocated to the study or the control group. The long protocol of GnRH agonist (GnRH-a) was used for controlled ovarian stimulation (COS) in all patients. Patients in the study group were treated with pioglitazone at a dose of 15 mg/day orally from the starting day of GnRH-a treatment to the day of hCG injection. Blood samples were drawn for serologic assay of RANTES on the first day of GnRH-a treatment and the day of hCG injection. There were no differences between the study and control groups in patient characteristics. There were also no differences between the two groups in COS duration, and the numbers of retrieved oocytes, fertilized oocytes and embryos transferred. The clinical pregnancy rate per cycle was higher in the study group, but this difference was not statistically significant. However, embryo implantation rate was significantly higher in the study group of 12.5% compared with 8.6% in the control group (P<0.05). The serum RANTES levels after pioglitazone treatment were significantly lower than those before pioglitazone treatmen in the study group (P<0.05). Our data suggest that pioglitazone treatment can suppress RANTES production and improve the embryo implantation rate in patients with endometriosis undergoing IVF.

Cardiac physiologic regulation of sub-type specific adrenergic receptors in transgenic mice overexpressing β1- and β2-adrenergic receptors.

  • Kim, Ka Eul;Tae, Hyun-Jin;Natalia, Petrashevskaya;Lee, Jae-Chul;Ahn, Ji Hyeon;Park, Joon Ha;Kim, In Hye;Ohk, Taek Geun;Park, Chan Woo;Cho, Jun Hwi;Won, Moo-Ho
    • Clinical and Experimental Emergency Medicine
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    • 제3권3호
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    • pp.175-180
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    • 2016
  • Objective Combination of ${\beta}_1-adrenergic$ receptor (AR) blockade and ${\beta}_2-AR$ activation might be a potential novel therapy for treating heart failure. However, use of ${\beta}-AR$ agonists and/or antagonists in the clinical setting is controversial because of the lack of information on cardiac inotropic or chronotropic regulation by AR signaling. Methods In this study, we performed hemodynamic evaluation by examining force frequency response (FFR), Frank-Starling relationship, and response to a non-selective ${\beta}-AR$ agonist (isoproterenol) in hearts isolated from 6-month-old transgenic (TG) mice overexpressing ${\beta}_1-$ and ${\beta}_2-ARs$ (${\beta}_1-$ and ${\beta}_2-AR$ TG mice, respectively). Results Cardiac physiologic consequences of ${\beta}_1-$ and ${\beta}_2-AR$ overexpression resulted in similar maximal response to isoproterenol and faster temporary decline of positive inotropic response in ${\beta}_2-AR$ TG mice. ${\beta}_1-AR$ TG mice showed a pronounced negative limb of FFR, whereas ${\beta}_2-AR$ TG mice showed high stimulation frequencies with low contractile depression during FFR. In contrast, Frank-Starling relationship was equally enhanced in both ${\beta}_1-$ and ${\beta}_2-AR$ TG mice. Conclusion Hemodynamic evaluation performed in the present showed a difference in ${\beta}_1-$ and ${\beta}_2-AR$ signaling, which may be due to the difference in the desensitization of ${\beta}_1-$ and ${\beta}_2-ARs$.

Effect of ciglitazone on adipogenic transdifferentiation of bovine skeletal muscle satellite cells

  • Zhang, Junfang;Li, Qiang;Yan, Yan;Sun, Bin;Wang, Ying;Tang, Lin;Wang, Enze;Yu Jia;Nogoy, Kim Margarette Corpuz;Li, Xiangzi;Choi, Seong-Ho
    • Journal of Animal Science and Technology
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    • 제63권4호
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    • pp.934-953
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    • 2021
  • Ciglitazone is a member of the thiazolidinedione family, and specifically binds to peroxisome proliferator-activated receptor-γ (PPARγ), thereby promoting adipocyte differentiation. We hypothesized that ciglitazone as a PPARγ ligand in the absence of an adipocyte differentiation cocktail would increase adiponectin and adipogenic gene expression in bovine satellite cells (BSC). Muscle-derived BSCs were isolated from six, 18-month-old Yanbian Yellow Cattle. The BSC were cultured for 96 h in differentiation medium containing 5 µM ciglitazone (CL), 10 µM ciglitazone (CM), or 20 µM ciglitazone (CH). Control (CON) BSC were cultured only in a differentiation medium (containing 2% horse serum). The presence of myogenin, desmin, and paired box 7 (Pax7) proteins was confirmed in the BSC by immunofluorescence staining. The CL, CM, and CH treatments produced higher concentrations of triacylglycerol and lipid droplet accumulation in myotubes than those of the CON treatment. Ciglitazone treatments significantly increased the relative expression of PPARγ, CCAAT/enhancer-binding protein alpha (C/EBPα), C/EBPβ, fatty acid synthase, stearoyl-CoA desaturase, and perilipin 2. Ciglitazone treatments increased gene expression of Pax3 and Pax7 and decreased expression of myogenic differentiation-1, myogenin, myogenic regulatory factor-5, and myogenin-4 (p < 0.01). Adiponectin concentration caused by ciglitazone treatments was significantly greater than CON (p < 0.01). RNA sequencing showed that 281 differentially expressed genes (DEGs) were found in the treatments of ciglitazone. DEGs gene ontology (GO) analysis showed that the top 10 GO enrichment significantly changed the biological processes such as protein trimerization, negative regulation of cell proliferation, adipocytes differentiation, and cellular response to external stimulus. Kyoto Encyclopedia of Genes and Genomes pathway analysis showed that DEGs were involved in the p53 signaling pathway, PPAR signaling pathway, biosynthesis of amino acids, tumor necrosis factor signaling pathway, non-alcoholic fatty liver disease, PI3K-Akt signaling pathway, and Wnt signaling pathway. These results indicate that ciglitazone acts as PPARγ agonist, effectively increases the adiponectin concentration and adipogenic gene expression, and stimulates the conversion of BSC to adipocyte-like cells in the absence of adipocyte differentiation cocktail.