SB-258719

SB-258719
식별자
	IUPAC 이름 (1R)-3,N-디메틸-N-[1-메틸-3-(4-메틸피페리딘-1-yl)프로필]벤젠설폰아미드;
CAS 번호	195199-95-2 ;
펍켐 CID	5312148;
IUPHAR/BPS	281;
켐스파이더	4471578 ;
켐벨	켐블12264 ;
화학 및 물리적 데이터
공식	C18H32N2O2S
어금질량	340.53 g·190−1
3D 모델(JSmol)	인터랙티브 이미지;
	스마일즈 c1cc(C)cc1S(=O)N(C)CCN(CC2)CC2C;
	인치 InChI=1S/C18H30N2O2S/c1-15-8-11-20(12-9-15)13-10-17(3)19(4)23(21,22)18-7-5-6-16(2)14-18/h5-7,14-15,17H,8-13H2,1-4H3/t17-/m1/s1 ; 키:AGVNHDNTFYHzN-QGZVFFLSA-N ;
	(이게 뭐야?) (iii)

SB-258719는 GlaxoSmithKline이₇ 개발한 약물로 선택적 5-HT 수용체 부분 역작용제 역할을 하며,^[1] 5-HT에서₇ 확인된 리간드로는 최초다.^[2] SB-258719는 여러 가지 다른 시험 모델에 걸쳐 다양한 5-HT₇ 작용제의 진통 효과를 차단하는 능력 때문에 주로 5-HT₇ 작용제의 잠재적 진통제 사용 가능성을 입증하는 데 사용되어 왔다.^[3]^[4]^[5]^[6]

참조

^ Mahé C, Loetscher E, Feuerbach D, Müller W, Seiler MP, Schoeffter P (July 2004). "Differential inverse agonist efficacies of SB-258719, SB-258741 and SB-269970 at human recombinant serotonin 5-HT7 receptors". European Journal of Pharmacology. 495 (2–3): 97–102. doi:10.1016/j.ejphar.2004.05.033. PMID 15249157.
^ Forbes IT, Dabbs S, Duckworth DM, Jennings AJ, King FD, Lovell PJ, et al. (February 1998). "(R)-3,N-dimethyl-N-[1-methyl-3-(4-methyl-piperidin-1-yl) propyl]benzenesulfonamide: the first selective 5-HT7 receptor antagonist". Journal of Medicinal Chemistry. 41 (5): 655–7. doi:10.1021/jm970519e. PMID 9513592.
^ Brenchat A, Romero L, García M, Pujol M, Burgueño J, Torrens A, et al. (February 2009). "5-HT7 receptor activation inhibits mechanical hypersensitivity secondary to capsaicin sensitization in mice". Pain. 141 (3): 239–47. doi:10.1016/j.pain.2008.11.009. PMID 19118950.
^ Yanarates O, Dogrul A, Yildirim V, Sahin A, Sizlan A, Seyrek M, et al. (March 2010). "Spinal 5-HT7 receptors play an important role in the antinociceptive and antihyperalgesic effects of tramadol and its metabolite, O-Desmethyltramadol, via activation of descending serotonergic pathways". Anesthesiology. 112 (3): 696–710. doi:10.1097/ALN.0b013e3181cd7920. PMID 20179508.
^ Brenchat A, Nadal X, Romero L, Ovalle S, Muro A, Sánchez-Arroyos R, et al. (June 2010). "Pharmacological activation of 5-HT7 receptors reduces nerve injury-induced mechanical and thermal hypersensitivity". Pain. 149 (3): 483–94. doi:10.1016/j.pain.2010.03.007. PMID 20399562.
^ Brenchat A, Ejarque M, Zamanillo D, Vela JM, Romero L (August 2011). "Potentiation of morphine analgesia by adjuvant activation of 5-HT7 receptors". Journal of Pharmacological Sciences. 116 (4): 388–91. doi:10.1254/jphs.11039sc. PMID 21778664.

신경계통에 관한 이 약물 기사는 단조롭다. 위키피디아를 확장하여 도울 수 있다.

[pmid15249157-1] Mahé C, Loetscher E, Feuerbach D, Müller W, Seiler MP, Schoeffter P (July 2004). "Differential inverse agonist efficacies of SB-258719, SB-258741 and SB-269970 at human recombinant serotonin 5-HT7 receptors". European Journal of Pharmacology. 495 (2–3): 97–102. doi:10.1016/j.ejphar.2004.05.033. PMID 15249157.

[pmid9513592-2] Forbes IT, Dabbs S, Duckworth DM, Jennings AJ, King FD, Lovell PJ, et al. (February 1998). "(R)-3,N-dimethyl-N-[1-methyl-3-(4-methyl-piperidin-1-yl) propyl]benzenesulfonamide: the first selective 5-HT7 receptor antagonist". Journal of Medicinal Chemistry. 41 (5): 655–7. doi:10.1021/jm970519e. PMID 9513592.

[pmid19118950-3] Brenchat A, Romero L, García M, Pujol M, Burgueño J, Torrens A, et al. (February 2009). "5-HT7 receptor activation inhibits mechanical hypersensitivity secondary to capsaicin sensitization in mice". Pain. 141 (3): 239–47. doi:10.1016/j.pain.2008.11.009. PMID 19118950.

[pmid20179508-4] Yanarates O, Dogrul A, Yildirim V, Sahin A, Sizlan A, Seyrek M, et al. (March 2010). "Spinal 5-HT7 receptors play an important role in the antinociceptive and antihyperalgesic effects of tramadol and its metabolite, O-Desmethyltramadol, via activation of descending serotonergic pathways". Anesthesiology. 112 (3): 696–710. doi:10.1097/ALN.0b013e3181cd7920. PMID 20179508.

[pmid20399562-5] Brenchat A, Nadal X, Romero L, Ovalle S, Muro A, Sánchez-Arroyos R, et al. (June 2010). "Pharmacological activation of 5-HT7 receptors reduces nerve injury-induced mechanical and thermal hypersensitivity". Pain. 149 (3): 483–94. doi:10.1016/j.pain.2010.03.007. PMID 20399562.

[pmid21778664-6] Brenchat A, Ejarque M, Zamanillo D, Vela JM, Romero L (August 2011). "Potentiation of morphine analgesia by adjuvant activation of 5-HT7 receptors". Journal of Pharmacological Sciences. 116 (4): 388–91. doi:10.1254/jphs.11039sc. PMID 21778664.

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SB-258719

네임스페이스

더

참조

식별자

IUPAC 이름 (1R)-3,N-디메틸-N-[1-메틸-3-(4-메틸피페리딘-1-yl)프로필]벤젠설폰아미드
CAS 번호	195199-95-2^N
펍켐 CID	5312148
IUPHAR/BPS	281
켐스파이더	4471578^Y
켐벨	켐블12264^Y
화학 및 물리적 데이터
공식	C₁₈H₃₂N₂O₂S
어금질량	340.53 g·190⁻¹
3D 모델(JSmol)	인터랙티브 이미지
스마일즈 c1cc(C)cc1S(=O)N(C)CCN(CC2)CC2C
인치 InChI=1S/C18H30N2O2S/c1-15-8-11-20(12-9-15)13-10-17(3)19(4)23(21,22)18-7-5-6-16(2)14-18/h5-7,14-15,17H,8-13H2,1-4H3/t17-/m1/s1^Y 키:AGVNHDNTFYHzN-QGZVFFLSA-N^Y
^NY (이게 뭐야?) (iii)