From: Lamont Granquist
Newsgroups: sci.med.psychobiology,sci.med.pharmacy,alt.psychoactives,alt.drugs
Subject: SSRI Neurochemistry
Date: 10 Sep 1994 23:13:54 GMT
Message-ID: <34teji$f6t@news.u.washington.edu>
As mentioned in the original article, these drugs typically have active
metabolites which may be significant. Thus, actual in vivo activity may
be slightly different.
Receptor Affinities for SSRI drugs
(Values normalized to the IC50 for 5-HT reuptake)
[Data Taken from: Internatn-Clin-Psychopharm, 9 suppl 1: 19-26 (1994)]
Clomiprimine Fluoxetine Sertraline Paroxetine Fluvoxamine
(Prozac) (Zoloft) (Paxil)
5HTRI: 1 5HTRI: 1 5HTRI: 1 5HTRI: 1 5HTRI: 1
NARI: 14 NARI: 54 DARI: 250 NARI: 280 NARI: 160
H1: 36 5HT2A: 100 NARI: 840 ACh: 720 Alpha2: 500
5HT2A 36 5HT2C: 235 ACh: 5,800 DARI: 18,000 Alpha1: 1,300
Alpha1: 40 Beta: 264 Alpha2: 9,500 D1: 52,000 5HT2C: 1,800
ACh: 45 Alpha2: 410 Alpha1: 15,000 5HT2A: 62,000 H1: 2,900
D1: 130 ACh: 445 D1: 33,000 H1: 66,000 5HT2A: 3,200
D2: 290 H1: 470 5HT2A: 45,000 Alpha1: 66,000 ACh: 8,900
Alpha2: 1,200 DARI: 740 H1: 53,000 5HT2C: 69,000 DARI: 11,000
5HT1A: 1,900 D1: 1,500 Beta: 74,000 Beta: 120,000 D2: 17,000
DARI: 2,900 Alpha1: 2,000 D2: 130,000 D2: 180,000 Beta: 23,000
Beta: 15,000 D2: 4,700 5HT1A: >530,000 Alpha2: 300,000 D1: >26,000
5HT2C: NA 5HT1A: 12,000 5HT2C: NA 5HT1A: >340,000 5HT1A: >26,000
Citalopram
5HTRI: 1
H1: 220
5HT2C: 350
Alpha1: 890
Alpha2: 1,000
ACh: 3,100
5HT2A: 3,100
NARI: 3,400
5HT1A: 8,300
D1: 12,000
D2: 18,000
DARI: 22,000
Beta: >56,000
Radioligands used in binding:
D1: SCH23390; D2: Spiperone; 5-HT1A: 5-OH-DPAT; 5-HT2A: Ketanserin;
5-HT2C: Ly278584; Alpha1: Prazosin; Alpha2: Idazoxan; Beta: Dihydroalprenolol;
H1: Mepyramine; ACh: QNB.
--
Lamont Granquist
"In a saner world his [Noam Chomsky's] tireless efforts to promote justice
would have long since won him the Nobel Peace Prize, but the committee keeps
giving it to people like Henry Kissinger." -- Arthur Naiman
