Peringatan Keamanan

10 mg and 40 mg was well tolerated during clinical trials with Raynaud's patients

OPC-28326

DB05461

small molecule investigational

Deskripsi

At low doses, OPC 28326 selectively vasodilates the femoral arterial bed due to its inhibitory action at alpha-2-adrenoceptors while having minimal action on systemic blood pressure, heart rate and coronary, carotid, vertebral, renal, and mesenteric blood flows. It is the only clinical compound with this profile. It is currently being investigated in the treatment of peripheral vascular diseases and Raynaud's syndrome.

Struktur Molekul 2D

Berat 476.051
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) -
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

Data absorpsi tidak tersedia.

Metabolisme

Data metabolisme tidak tersedia.

Rute Eliminasi

Data eliminasi belum tersedia.

Interaksi Obat

0 Data
Tidak ada data.

Target Protein

5-hydroxytryptamine receptor 2B HTR2B
Alpha-2C adrenergic receptor ADRA2C
Alpha-2B adrenergic receptor ADRA2B

Referensi & Sumber

Artikel (PubMed)
  • PMID: 17223008
    Sumi M, Sata M, Hashimoto A, Imaizumi T, Yanaga K, Ohki T, Mori T, Nagai R: OPC-28326, a selective femoral arterial vasodilator, augments ischemia induced angiogenesis. Biomed Pharmacother. 2007 May;61(4):209-15. Epub 2006 Dec 28.
  • PMID: 15593189
    Wise RA, Wigley FM, White B, Leatherman G, Zhong J, Krasa H, Kambayashi J, Orlandi C, Czerwiec FS: Efficacy and tolerability of a selective alpha(2C)-adrenergic receptor blocker in recovery from cold-induced vasospasm in scleroderma patients: a single-center, double-blind, placebo-controlled, randomized crossover study. Arthritis Rheum. 2004 Dec;50(12):3994-4001.
  • PMID: 11855671
    Orito K, Imaizumi T, Yoshida K, Kishi M, Fujiki H, Mori T: Effect of oral OPC-28326, a selective femoral arterial vasodilator, on hindlimb subcutaneous tissue temperature in conscious dogs under buprenorphine sedation. Jpn J Pharmacol. 2002 Jan;88(1):119-22.
  • PMID: 11606316
    Orito K, Kishi M, Imaizumi T, Nakazawa T, Hashimoto A, Mori T, Kambe T: alpha(2)-adrenoceptor antagonist properties of OPC-28326, a novel selective peripheral vasodilator. Br J Pharmacol. 2001 Oct;134(4):763-70.
  • PMID: 10525078
    Orito K, Imaizumi T, Yoshida K, Fujiki H, Kishi M, Teramoto S, Tanaka M, Shimizu H, Tominaga M, Kimura Y, Kambayashi J, Mori T: Mechanisms of action of OPC-28326, a selective hindlimb vasodilator. J Pharmacol Exp Ther. 1999 Nov;291(2):604-11.
  • PMID: 11602678
    Sun B, Lockyer S, Li J, Chen R, Yoshitake M, Kambayashi JI: OPC-28326, a selective femoral vasodilator, is an alpha2C-adrenoceptor-selective antagonist. J Pharmacol Exp Ther. 2001 Nov;299(2):652-8.

Contoh Produk & Brand

Produk: 0 • International brands: 0
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Sekuens Gen/Protein (FASTA)

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